Ronald T. Borchardt - Publications

Affiliations: 
Pharmaceutical Chemistry University of Kansas, Lawrence, KS, United States 
Area:
Pharmaceutical Chemistry
Website:
https://pharmchem.ku.edu/ronald-borchardt-0

213 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2013 Trammel AM, Simmons JE, Borchardt RT. An efficient in vitro assay for acetylcholinesterase reactivators using immobilized enzyme. Pharmaceutical Research. 1: 115-20. PMID 24277247 DOI: 10.1023/A:1016323919445  0.32
2012 Nofsinger R, Fuchs-Knotts T, Borchardt RT. Factors that restrict the cell permeation of cyclic prodrugs of an opioid peptide, part 3: Synthesis of analogs designed to have improved stability to oxidative metabolism. Journal of Pharmaceutical Sciences. 101: 3486-99. PMID 22411763 DOI: 10.1002/Jps.23109  0.782
2012 Nofsinger R, Borchardt RT. Factors that restrict the cell permeation of cyclic prodrugs of an opioid peptide, part 4: Characterization of the biopharmaceutical and physicochemical properties of two new cyclic prodrugs designed to be stable to oxidative metabolism by cytochrome P-450 enzymes in the intestinal mucosa. Journal of Pharmaceutical Sciences. 101: 3500-10. PMID 22337204 DOI: 10.1002/Jps.23079  0.791
2012 Wang B, Shan D, Wang W, Zhang H, Gudmundsson O, Borchardt RT. Synthesis of coumarin-based, esterase-sensitive cyclic prodrugs of opioid peptides with enhanced membrane permeability and enzymatic stability. Methods in Molecular Medicine. 23: 71-85. PMID 21380892 DOI: 10.1385/0-89603-517-4:71  0.536
2012 Wang B, Gangwar S, Pauletti G, Siahaan T, Borchardt RT. Synthesis of an esterase-sensitive cyclic prodrug of a model hexapeptide having enhanced membrane permeability and enzymatic stability using a 3-(2'-hydroxy-4',6'-dimethylphenyl)-3,3-dimethyl propionic Acid promoiety. Methods in Molecular Medicine. 23: 53-69. PMID 21380891 DOI: 10.1385/0-89603-517-4:53  0.551
2012 Gangwar S, Pauletti GM, Siahaan TJ, Stella VJ, Borchardt RT. Synthesis of an esterase-sensitive cyclic prodrug of a model hexapeptide having enhanced membrane permeability and enzymatic stability using an acyloxyalkoxy promoiety. Methods in Molecular Medicine. 23: 37-51. PMID 21380890 DOI: 10.1385/0-89603-517-4:37  0.382
2010 Mudra DR, Jin JY, Borchardt RT. Absorption barriers in the rat intestinal mucosa: 2. Application of physiologically based mathematical models to quantify mechanisms of drug permeation and metabolism. Journal of Pharmaceutical Sciences. 99: 999-1015. PMID 19798765 DOI: 10.1002/Jps.21965  0.746
2010 Mudra DR, Borchardt RT. Absorption barriers in the rat intestinal mucosa: 1. Application of an in situ perfusion model to simultaneously assess drug permeation and metabolism. Journal of Pharmaceutical Sciences. 99: 982-98. PMID 19746412 DOI: 10.1002/Jps.21912  0.751
2010 Mudra DR, Borchardt RT. Absorption barriers in the rat intestinal mucosa. 3: Effects of polyethoxylated solubilizing agents on drug permeation and metabolism. Journal of Pharmaceutical Sciences. 99: 1016-27. PMID 19650119 DOI: 10.1002/Jps.21836  0.746
2010 Wang B, Gangwar S, Pauletti G, Siahaan T, Borchardt RT. ChemInform Abstract: Synthesis of an Esterase-Sensitive Cyclic Prodrug of a Model Hexapeptide Having Enhanced Membrane Permeability and Enzymic Stability Using a 3-(2′-Hydroxy-4′,6′-dimethylphenyl)-3,3-Dimethylpropionic Acid Promoiety Cheminform. 31: no-no. DOI: 10.1002/chin.200032252  0.448
2010 Wang B, Shan D, Wang W, Zhang H, Gudmundsson O, Borchardt RT. ChemInform Abstract: Synthesis of Coumarin-Based, Esterase-Sensitive Cyclic Prodrugs of Opioid Peptides with Enhanced Membrane Permeability and Enzymic Stability Cheminform. 31: no-no. DOI: 10.1002/CHIN.200032251  0.455
2010 Wang B, Wang W, Camenisch GP, Elmo J, Zhang H, Borchardt RT. ChemInform Abstract: Synthesis and Evaluation of Novel Coumarin-Based Esterase-Sensitive Cyclic Prodrugs of Peptidomimetic RGD Analogues with Improved Membrane Permeability. Cheminform. 30: no-no. DOI: 10.1002/chin.199930175  0.418
2010 WANG B, LIU S, BORCHARDT RT. ChemInform Abstract: Development of a Novel Redox-Sensitive Protecting Group for Amines Which Utilizes a Facilitated Lactonization Reaction. Cheminform. 26: no-no. DOI: 10.1002/chin.199529091  0.396
2009 Li QS, Cai S, Fang J, Borchardt RT, Kuczera K, Middaugh CR, Schowen RL. Evaluation of NAD(H) analogues as selective inhibitors for Trypanosoma cruzi S-adenosylhomocysteine hydrolase. Nucleosides, Nucleotides & Nucleic Acids. 28: 473-84. PMID 20183597 DOI: 10.1080/15257770903044572  0.314
2009 Ouyang H, Andersen TE, Chen W, Nofsinger R, Steffansen B, Borchardt RT. A comparison of the effects of p-glycoprotein inhibitors on the blood-brain barrier permeation of cyclic prodrugs of an opioid peptide (DADLE). Journal of Pharmaceutical Sciences. 98: 2227-36. PMID 18855917 DOI: 10.1002/Jps.21585  0.785
2009 Ouyang H, Chen W, Andersen TE, Steffansen B, Borchardt RT. Factors that restrict intestinal cell permeation of cyclic prodrugs of an opioid peptide (DADLE): Part II. Role of metabolic enzymes in the intestinal mucosa. Journal of Pharmaceutical Sciences. 98: 349-61. PMID 18537150 DOI: 10.1002/Jps.21424  0.381
2009 Ouyang H, Chen W, Andersen TE, Steffansen B, Borchardt RT. Factors that restrict the intestinal cell permeation of cyclic prodrugs of an opioid peptide (DADLE): Part I. Role of efflux transporters in the intestinal mucosa. Journal of Pharmaceutical Sciences. 98: 337-48. PMID 18537149 DOI: 10.1002/Jps.21428  0.359
2008 Li QS, Cai S, Fang J, Borchardt RT, Kuczera K, Middaugh CR, Schowen RL. Comparative kinetics of cofactor association and dissociation for the human and trypanosomal S-adenosylhomocysteine hydrolases. 2. The role of helix 18 stability. Biochemistry. 47: 4983-91. PMID 18393535 DOI: 10.1021/Bi800175G  0.308
2007 Cai S, Li QS, Borchardt RT, Kuczera K, Schowen RL. The antiviral drug ribavirin is a selective inhibitor of S-adenosyl-L-homocysteine hydrolase from Trypanosoma cruzi. Bioorganic & Medicinal Chemistry. 15: 7281-7. PMID 17845853 DOI: 10.1016/J.Bmc.2007.08.029  0.307
2007 Li QS, Cai S, Borchardt RT, Fang J, Kuczera K, Middaugh CR, Schowen RL. Comparative kinetics of cofactor association and dissociation for the human and trypanosomal S-adenosylhomocysteine hydrolases. 1. Basic features of the association and dissociation processes. Biochemistry. 46: 5798-809. PMID 17447732 DOI: 10.1021/Bi700170M  0.306
2007 Wakankar AA, Liu J, Vandervelde D, Wang YJ, Shire SJ, Borchardt RT. The effect of cosolutes on the isomerization of aspartic acid residues and conformational stability in a monoclonal antibody. Journal of Pharmaceutical Sciences. 96: 1708-18. PMID 17238195 DOI: 10.1002/Jps.20823  0.306
2006 Liederer BM, Borchardt RT. Enzymes involved in the bioconversion of ester-based prodrugs. Journal of Pharmaceutical Sciences. 95: 1177-95. PMID 16639719 DOI: 10.1002/Jps.20542  0.644
2006 Liederer BM, Fuchs T, Vander Velde D, Siahaan TJ, Borchardt RT. Effects of amino acid chirality and the chemical linker on the cell permeation characteristics of cyclic prodrugs of opioid peptides. Journal of Medicinal Chemistry. 49: 1261-70. PMID 16480263 DOI: 10.1021/Jm050277F  0.682
2005 Liederer BM, Phan KT, Ouyang H, Borchardt RT. Significant differences in the disposition of cyclic prodrugs of opioid peptides in rats and guinea pigs following IV administration. Journal of Pharmaceutical Sciences. 94: 2676-87. PMID 16258984 DOI: 10.1002/Jps.20476  0.676
2005 Liederer BM, Borchardt RT. Stability of oxymethyl-modified coumarinic acid cyclic prodrugs of diastereomeric opioid peptides in biological media from various animal species including human. Journal of Pharmaceutical Sciences. 94: 2198-206. PMID 16136552 DOI: 10.1002/Jps.20452  0.681
2005 Li B, O'Meara MH, Lubach JW, Schowen RL, Topp EM, Munson EJ, Borchardt RT. Effects of sucrose and mannitol on asparagine deamidation rates of model peptides in solution and in the solid state. Journal of Pharmaceutical Sciences. 94: 1723-35. PMID 15986465 DOI: 10.1002/Jps.20372  0.308
2004 Tang F, Ouyang H, Yang JZ, Borchardt RT. Bidirectional transport of rhodamine 123 and Hoechst 33342, fluorescence probes of the binding sites on P-glycoprotein, across MDCK-MDR1 cell monolayers. Journal of Pharmaceutical Sciences. 93: 1185-94. PMID 15067695 DOI: 10.1002/Jps.20046  0.328
2003 Parker NB, Yang X, Hanke J, Mason KA, Schowen RL, Borchardt RT, Yin DH. Trypanosoma cruzi: molecular cloning and characterization of the S-adenosylhomocysteine hydrolase. Experimental Parasitology. 105: 149-58. PMID 14969692 DOI: 10.1016/J.Exppara.2003.10.001  0.305
2003 Li B, Borchardt RT, Topp EM, VanderVelde D, Schowen RL. Racemization of an asparagine residue during peptide deamidation. Journal of the American Chemical Society. 125: 11486-7. PMID 13129337 DOI: 10.1021/Ja0360992  0.321
2003 Johnson BM, Chen W, Borchardt RT, Charman WN, Porter CJ. A kinetic evaluation of the absorption, efflux, and metabolism of verapamil in the autoperfused rat jejunum. The Journal of Pharmacology and Experimental Therapeutics. 305: 151-8. PMID 12649363 DOI: 10.1124/Jpet.102.045328  0.335
2003 Yang X, Hu Y, Yin DH, Turner MA, Wang M, Borchardt RT, Howell PL, Kuczera K, Schowen RL. Catalytic strategy of S-adenosyl-L-homocysteine hydrolase: transition-state stabilization and the avoidance of abortive reactions. Biochemistry. 42: 1900-9. PMID 12590576 DOI: 10.1021/Bi0262350  0.328
2003 D'Souza AJ, Schowen RL, Borchardt RT, Salsbury JS, Munson EJ, Topp EM. Reaction of a peptide with polyvinylpyrrolidone in the solid state. Journal of Pharmaceutical Sciences. 92: 585-93. PMID 12587120 DOI: 10.1002/Jps.10316  0.323
2003 Hugger ED, Cole CJ, Raub TJ, Burton PS, Borchardt RT. Automated analysis of polyethylene glycol-induced inhibition of P-glycoprotein activity in vitro. Journal of Pharmaceutical Sciences. 92: 21-6. PMID 12486678 DOI: 10.1002/Jps.10265  0.784
2002 Chen W, Yang JZ, Andersen R, Nielsen LH, Borchardt RT. Evaluation of the permeation characteristics of a model opioid peptide, H-Tyr-D-Ala-Gly-Phe-D-Leu-OH (DADLE), and its cyclic prodrugs across the blood-brain barrier using an in situ perfused rat brain model. The Journal of Pharmacology and Experimental Therapeutics. 303: 849-57. PMID 12388672 DOI: 10.1124/Jpet.102.037143  0.356
2002 Yang JZ, Chen W, Borchardt RT. In vitro stability and in vivo pharmacokinetic studies of a model opioid peptide, H-Tyr-D-Ala-Gly-Phe-D-Leu-OH (DADLE), and its cyclic prodrugs. The Journal of Pharmacology and Experimental Therapeutics. 303: 840-8. PMID 12388671 DOI: 10.1124/Jpet.102.037135  0.385
2002 Hugger ED, Novak BL, Burton PS, Audus KL, Borchardt RT. A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. Journal of Pharmaceutical Sciences. 91: 1991-2002. PMID 12210046 DOI: 10.1002/Jps.10176  0.778
2002 Hugger ED, Audus KL, Borchardt RT. Effects of poly(ethylene glycol) on efflux transporter activity in Caco-2 cell monolayers. Journal of Pharmaceutical Sciences. 91: 1980-90. PMID 12210045 DOI: 10.1002/Jps.10175  0.787
2002 Ouyang H, Tang F, Siahaan TJ, Borchardt RT. A modified coumarinic acid-based cyclic prodrug of an opioid peptide: its enzymatic and chemical stability and cell permeation characteristics. Pharmaceutical Research. 19: 794-801. PMID 12134949 DOI: 10.1023/A:1016148631055  0.353
2002 Tang F, Borchardt RT. Characterization of the efflux transporter(s) responsible for restricting intestinal mucosa permeation of the coumarinic acid-based cyclic prodrug of the opioid peptide DADLE. Pharmaceutical Research. 19: 787-93. PMID 12134948 DOI: 10.1023/A:1016196514217  0.336
2002 Tang F, Borchardt RT. Characterization of the efflux transporter(s) responsible for restricting intestinal mucosa permeation of an acyloxyalkoxy-based cyclic prodrug of the opioid peptide DADLE. Pharmaceutical Research. 19: 780-6. PMID 12134947 DOI: 10.1023/A:1016144530146  0.323
2002 Friedrichsen GM, Chen W, Begtrup M, Lee CP, Smith PL, Borchardt RT. Synthesis of analogs of L-valacyclovir and determination of their substrate activity for the oligopeptide transporter in Caco-2 cells. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation For Pharmaceutical Sciences. 16: 1-13. PMID 12113886 DOI: 10.1016/S0928-0987(02)00047-7  0.354
2002 Ouyang H, Borchardt RT, Siahaan TJ, Vander Velde DG. Synthesis and conformational analysis of a coumarinic acid-based cyclic prodrug of an opioid peptide with modified sensitivity to esterase-catalyzed bioconversion Journal of Peptide Research. 59: 183-195. PMID 11972752 DOI: 10.1034/J.1399-3011.2002.1O983.X  0.348
2001 Gao J, Hugger ED, Beck-Westermeyer MS, Borchardt RT. Estimating intestinal mucosal permeation of compounds using Caco-2 cell monolayers. Current Protocols in Pharmacology / Editorial Board, S.J. Enna (Editor-in-Chief) ... [Et Al.]. Unit 7.2. PMID 22293966 DOI: 10.1002/0471141755.Ph0702S08  0.769
2001 Hu Y, Yang X, Yin DH, Mahadevan J, Kuczera K, Schowen RL, Borchardt RT. Computational characterization of substrate binding and catalysis in S-adenosylhomocysteine hydrolase. Biochemistry. 40: 15143-52. PMID 11735397 DOI: 10.1021/Bi015690D  0.331
2001 Song Y, Schowen RL, Borchardt RT, Topp EM. Formaldehyde production by Tris buffer in peptide formulations at elevated temperature. Journal of Pharmaceutical Sciences. 90: 1198-203. PMID 11536224 DOI: 10.1002/Jps.1073  0.308
2001 Gao J, Murase O, Schowen RL, Aubé J, Borchardt RT. A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells. Pharmaceutical Research. 18: 171-6. PMID 11405287 DOI: 10.1023/A:1011076217118  0.625
2001 Gao J, Winslow SL, Vander Velde D, Aubé J, Borchardt RT. Transport characteristics of peptides and peptidomimetics: II. Hydroxyethylamine bioisostere-containing peptidomimetics as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa. The Journal of Peptide Research : Official Journal of the American Peptide Society. 57: 361-73. PMID 11350596 DOI: 10.1034/J.1399-3011.2001.00830.X  0.657
2001 Gao J, Sudoh M, Aubé J, Borchardt RT. Transport characteristics of peptides and peptidomimetics: I. N-methylated peptides as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa. The Journal of Peptide Research : Official Journal of the American Peptide Society. 57: 316-29. PMID 11328489 DOI: 10.1046/J.1397-002X.2001.00000.X  0.643
2001 Yang X, Borchardt RT. Overexpression, purification, and characterization of S-adenosylhomocysteine hydrolase from Leishmania donovani. Archives of Biochemistry and Biophysics. 383: 272-80. PMID 11185563 DOI: 10.1006/Abbi.2000.2087  0.306
2001 Khossravi M, Borchardt RT. Chemical pathways of peptide degradation. X: effect of metal-catalyzed oxidation on the solution structure of a histidine-containing peptide fragment of human relaxin. Pharmaceutical Research. 17: 851-8. PMID 10990205 DOI: 10.1023/A:1007564410491  0.302
2000 Turner MA, Yang X, Yin D, Kuczera K, Borchardt RT, Howell PL. Structure and function of S-adenosylhomocysteine hydrolase. Cell Biochemistry and Biophysics. 33: 101-25. PMID 11325033 DOI: 10.1385/Cbb:33:2:101  0.306
2000 Yang X, Yin D, Wnuk SF, Robins MJ, Borchardt RT. Mechanisms of inactivation of human S-adenosylhomocysteine hydrolase by 5',5',6',6'-tetradehydro-6'-deoxy-6'-halohomoadenosines. Biochemistry. 39: 15234-41. PMID 11106503 DOI: 10.1021/Bi0015055  0.323
2000 Goolcharran C, Stauffer LL, Cleland JL, Borchardt RT. The effects of a histidine residue on the C-terminal side of an asparaginyl residue on the rate of deamidation using model pentapeptides. Journal of Pharmaceutical Sciences. 89: 818-25. PMID 10824141 DOI: 10.1002/(Sici)1520-6017(200006)89:6<818::Aid-Jps14>3.0.Co;2-8  0.321
2000 Wnuk SF, Valdez CA, Khan J, Moutinho P, Robins MJ, Yang X, Borchardt RT, Balzarini J, De Clercq E. Doubly homologated dihalovinyl and acetylene analogues of adenosine: synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects. Journal of Medicinal Chemistry. 43: 1180-6. PMID 10737751 DOI: 10.1021/Jm990486Y  0.324
2000 Shan D, Zheng A, Ballard CE, Wang W, Borchardt RT, Wang B. A facilitated cyclic ether formation and its potential application in solid-phase peptide and organic synthesis. Chemical & Pharmaceutical Bulletin. 48: 238-44. PMID 10705512 DOI: 10.1248/Cpb.48.238  0.713
2000 Wang W, Borchardt RT, Wang B. Orally active peptidomimetic RGD analogs that are glycoprotein IIb/IIIa antagonists. Current Medicinal Chemistry. 7: 437-53. PMID 10702618 DOI: 10.2174/0929867003375074  0.543
2000 Wang W, Camenisch G, Sane DC, Zhang H, Hugger E, Wheeler GL, Borchardt RT, Wang B. A coumarin-based prodrug strategy to improve the oral absorption of RGD peptidomimetics. Journal of Controlled Release : Official Journal of the Controlled Release Society. 65: 245-51. PMID 10699284 DOI: 10.1016/S0168-3659(99)00241-2  0.785
1999 Borchardt RT. Optimizing oral absorption of peptides using prodrug strategies. Journal of Controlled Release : Official Journal of the Controlled Release Society. 62: 231-8. PMID 10518655 DOI: 10.1016/S0168-3659(99)00042-5  0.39
1999 Gudmundsson OS, Vander Velde DG, Jois SDS, Bak A, Siahaan TJ, Borchardt RT. The effect of conformation of the acyloxyalkoxy-based cyclic prodrugs of opioid peptides on their membrane permeability Journal of Peptide Research. 53: 403-413. PMID 10406218 DOI: 10.1034/J.1399-3011.1999.00077.X  0.344
1999 Bak A, Siahaan TJ, Gudmundsson OS, Gangwar S, Friis GJ, Borchardt RT. Synthesis and evaluation of the physicochemical properties of esterase- sensitive cyclic prodrugs of opioid peptides using an (acyloxy)alkoxy linker Journal of Peptide Research. 53: 393-402. PMID 10406217 DOI: 10.1034/J.1399-3011.1999.00070.X  0.345
1999 Gudmundsson OS, Jois SDS, Vander Velde DG, Siahaan TJ, Wang B, Borchardt RT. The effect of conformation on the membrane permeation of coumarinic acid- and phenylpropionic acid-based cyclic prodrugs of opioid peptides Journal of Peptide Research. 53: 383-392. PMID 10406216 DOI: 10.1034/J.1399-3011.1999.00076.X  0.538
1999 Wang B, Nimkar K, Wang W, Zhang H, Shan D, Gudmundsson O, Gangwar S, Siahaan T, Borchardt RT. Synthesis and evaluation of the physicochemical properties of esterase- sensitive cyclic prodrugs of opioid peptides using coumarinic acid and phenylpropionic acid linkers Journal of Peptide Research. 53: 370-382. PMID 10406215 DOI: 10.1034/J.1399-3011.1999.00071.X  0.56
1999 Wang B, Wang W, Camenisch GP, Elmo J, Zhang H, Borchardt RT. Synthesis and evaluation of novel coumarin-based esterase-sensitive cyclic prodrugs of peptidomimetic RGD analogs with improved membrane permeability. Chemical & Pharmaceutical Bulletin. 47: 90-5. PMID 9987829 DOI: 10.1248/Cpb.47.90  0.491
1999 Bak A, Gudmundsson OS, Friis GJ, Siahaan TJ, Borchardt RT. Acyloxyalkoxy-based cyclic prodrugs of opioid peptides: Evaluation of the chemical and enzymatic stability as well as their transport properties across Caco-2 cell monolayers Pharmaceutical Research. 16: 24-29. PMID 9950274 DOI: 10.1023/A:1018854308829  0.397
1999 Gudmundsson OS, Nimkar K, Gangwar S, Siahaan T, Borchardt RT. Phenylpropionic acid-based cyclic prodrugs of opioid peptides that exhibit metabolic stability to peptidases and excellent cellular permeation Pharmaceutical Research. 16: 16-23. PMID 9950273 DOI: 10.1023/A:1018802324759  0.335
1999 Gudmundsson OS, Pauletti GM, Wang W, Shan D, Zhang H, Wang B, Borchardt RT. Coumarinic acid-based cyclic prodrugs of opioid peptides that exhibit metabolic stability to peptidases and excellent cellular permeability Pharmaceutical Research. 16: 7-15. PMID 9950272 DOI: 10.1023/A:1018828207920  0.58
1999 Yuan CS, Saso Y, Lazarides E, Borchardt RT, Robins MJ. Recent advances in S-adenosyl-L-homocysteine hydrolase inhibitors and their potential clinical applications Expert Opinion On Therapeutic Patents. 9: 1197-1206. DOI: 10.1517/13543776.9.9.1197  0.312
1998 Li J, Tamura K, Lee CP, Smith PL, Borchardt RT, Hidalgo IJ. Structure-affinity relationships of Val-Val and Val-Val-Val stereoisomers with the apical oligopeptide transporter in human intestinal Caco-2 cells. Journal of Drug Targeting. 5: 317-27. PMID 9771614 DOI: 10.3109/10611869808997860  0.302
1998 Robins MJ, Wnuk SF, Yang X, Yuan CS, Borchardt RT, Balzarini J, De Clercq E. Inactivation of S-adenosyl-L-homocysteine hydrolase and antiviral activity with 5',5',6',6'-tetradehydro-6'-deoxy-6'-halohomoadenosine analogues (4'-haloacetylene analogues derived from adenosine). Journal of Medicinal Chemistry. 41: 3857-64. PMID 9748360 DOI: 10.1021/Jm980163M  0.317
1998 Wnuk SF, Yuan CS, Borchardt RT, Robins MJ. Synthesis of homologated halovinyl derivatives from aristeromycin and their inhibition of human placental S-adenosyl-L-homocysteine hydrolase. Nucleosides & Nucleotides. 17: 99-113. PMID 9708344 DOI: 10.1080/07328319808005161  0.304
1998 Camenisch GP, Wang W, Wang B, Borchardt RT. A comparison of the bioconversion rates and the Caco-2 cell permeation characteristics of coumarin-based cyclic prodrugs and methylester-based linear prodrugs of RGD peptidomimetics. Pharmaceutical Research. 15: 1174-81. PMID 9706046 DOI: 10.1023/A:1011975404789  0.481
1998 Wnuk SF, Mao Y, Yuan CS, Borchardt RT, Andrei G, Balzarini J, De Clercq E, Robins MJ. Discovery of type II (covalent) inactivation of S-adenosyl-L-homocysteine hydrolase involving its "hydrolytic activity": synthesis and evaluation of dihalohomovinyl nucleoside analogues derived from adenosine. Journal of Medicinal Chemistry. 41: 3078-83. PMID 9685247 DOI: 10.1021/Jm9801410  0.347
1998 Yuan CS, Wnuk SF, Robins MJ, Borchardt RT. A novel mechanism-based inhibitor (6'-bromo-5', 6'-didehydro-6'-deoxy-6'-fluorohomoadenosine) that covalently modifies human placental S-adenosylhomocysteine hydrolase. The Journal of Biological Chemistry. 273: 18191-7. PMID 9660780 DOI: 10.1074/Jbc.273.29.18191  0.317
1998 Sudoh M, Pauletti GM, Yao W, Moser W, Yokoyama A, Pasternak A, Sprengeler PA, Smith AB, Hirschmann R, Borchardt RT. Transport characteristics of peptidomimetics. Effect of the pyrrolinone bioisostere on transport across Caco-2 cell monolayers Pharmaceutical Research. 15: 719-725. PMID 9619780 DOI: 10.1023/A:1011966918959  0.357
1998 Robins MJ, Neschadimenko V, Ro B, Yuan C, Borchardt RT, Wnuk SF. Nucleic Acid Related Compounds. 101.S-Adenosyl-l-homocysteine Hydrolase Does Not Hydrate (5‘-Fluoro)vinyl or (6‘-Halo)homovinyl Analogues Derived from 3‘-Deoxyadenosine or 3‘-(Chloro or Fluoro)-3‘-deoxyadenosine1 Journal of Organic Chemistry. 63: 1205-1211. DOI: 10.1021/Jo971741U  0.325
1997 Sorensen M, Steenberg B, Knipp GT, Wang W, Steffansen B, Frokjaer S, Borchardt RT. The effect of β-turn structure on the permeation of peptides across monolayers of bovine brain microvessel endothelial cells Pharmaceutical Research. 14: 1341-1348. PMID 9358545 DOI: 10.1023/A:1012104301773  0.336
1997 Knipp GT, Vander Velde DG, Siahaan TJ, Borchardt RT. The effect of β-turn structure on the passive diffusion of peptides across caco-2 cell monolayers Pharmaceutical Research. 14: 1332-1340. PMID 9358544 DOI: 10.1023/A:1012152117703  0.339
1997 Tamura K, Agrios KA, Vander Velde D, Aubé J, Borchardt RT. Effect of stereochemistry on the transport of Aca-linked beta-turn peptidomimetics across a human intestinal cell line. Bioorganic & Medicinal Chemistry. 5: 1859-66. PMID 9354242 DOI: 10.1016/S0968-0896(97)00115-6  0.328
1997 Capdevila A, Decha-Umphai W, Song KH, Borchardt RT, Wagner C. Pancreatic exocrine secretion is blocked by inhibitors of methylation. Archives of Biochemistry and Biophysics. 345: 47-55. PMID 9281310 DOI: 10.1006/Abbi.1997.0249  0.32
1997 Kupczyk-Subotkowska L, Tamura K, Pal D, Sakaeda T, Siahaan TJ, Stella VJ, Borchardt RT. Derivatives of melphalan designed to enhance drug accumulation in cancer cells Journal of Drug Targeting. 4: 359-370. PMID 9239576 DOI: 10.3109/10611869709017893  0.303
1997 Huang H, Yuan CS, Borchardt RT. Effect of limited proteolysis on the stability and enzymatic activity of human placental S-adenosylhomocysteine hydrolase. Protein Science : a Publication of the Protein Society. 6: 1482-90. PMID 9232649 DOI: 10.1002/Pro.5560060712  0.313
1997 Nerurkar MM, Ho NF, Burton PS, Vidmar TJ, Borchardt RT. Mechanistic roles of neutral surfactants on concurrent polarized and passive membrane transport of a model peptide in Caco-2 cells. Journal of Pharmaceutical Sciences. 86: 813-21. PMID 9232522 DOI: 10.1021/Js960483Y  0.349
1997 Shan D, Nicolaou MG, Borchardt RT, Wang B. Prodrug strategies based on intramolecular cyclization reactions Journal of Pharmaceutical Sciences. 86: 765-767. PMID 9232513 DOI: 10.1021/Js970069D  0.501
1997 Huang H, Yuan CS, Wnuk SF, Robins MJ, Borchardt RT. The mechanism of inactivation of human placental S-adenosylhomocysteine hydrolase by (E)-4',5'-didehydro-5'-methoxyadenosine and adenosine 5'-carboxaldehyde oxime. Archives of Biochemistry and Biophysics. 343: 109-17. PMID 9210652 DOI: 10.1006/Abbi.1997.0159  0.321
1997 Wnuk SF, Yuan CS, Borchardt RT, Balzarini J, De Clercq E, Robins MJ. Anticancer and antiviral effects and inactivation of S-adenosyl-L-homocysteine hydrolase with 5'-carboxaldehydes and oximes synthesized from adenosine and sugar-modified analogues. Journal of Medicinal Chemistry. 40: 1608-18. PMID 9171871 DOI: 10.1021/Jm960828P  0.38
1997 Okumu FW, Pauletti GM, Vander Velde DG, Siahaan TJ, Borchardt RT. Effect of restricted conformational flexibility on the permeation of model hexapeptides across caco-2 cell monolayers Pharmaceutical Research. 14: 169-175. PMID 9090704 DOI: 10.1023/A:1012092409216  0.313
1997 Pauletti GM, Okumu FW, Borchardt RT. Effect of size and charge on the, passive diffusion of peptides across caco-2 cell monolayers via the paracellular pathway Pharmaceutical Research. 14: 164-168. PMID 9090703 DOI: 10.1023/A:1012040425146  0.316
1997 Pauletti GM, Gangwar S, Wang B, Borchardt RT. Esterase-sensitive cyclic prodrugs of peptides: Evaluation of a phenylpropionic acid promoiety in a model hexapeptide Pharmaceutical Research. 14: 11-17. PMID 9034215 DOI: 10.1023/A:1012091014242  0.537
1997 Wang B, Gangwar S, Pauletti GM, Siahaan TJ, Borchardt RT. Synthesis of a novel esterase-sensitive cyclic prodrug system for peptides that utilizes a 'trimethyl lock'-facilitated lactonization reaction Journal of Organic Chemistry. 62: 1363-1367. DOI: 10.1021/Jo961778Z  0.535
1997 Gangwar S, Pauletti GM, Siahaan TJ, Stella VJ, Borchardt RT. Synthesis of a novel esterase-sensitive cyclic prodrug of a hexapeptide using an (acyloxy)alkoxy promoiety Journal of Organic Chemistry. 62: 1356-1362. DOI: 10.1021/Jo961696A  0.361
1997 Gangwar S, Pauletti GM, Wang B, Siahaan TJ, Stella VJ, Borchardt RT. Prodrug strategies to enhance the intestinal absorption of peptides Drug Discovery Today. 2: 148-155. DOI: 10.1016/S1359-6446(97)01011-8  0.528
1997 Okumu FW, Cleland JL, Borchardt RT. The effect of size, charge and cyclization of model peptides on their in vitro release from dl–PLGA microspheres Journal of Controlled Release. 49: 133-140. DOI: 10.1016/S0168-3659(97)00065-5  0.304
1997 Gangwar S, Pauletti GM, Wang B, Siahaan TJ, Stella VJ, Borchardt RT. Novel esterase-sensitive cyclic prodrugs of a model hexapeptide having enhanced membrane permeability and enzymatic stability Pharmacochemistry Library. 28: 27-34. DOI: 10.1016/S0165-7208(97)80050-5  0.553
1996 Nicolaou MG, Wolfe JL, Schowen RL, Borchardt RT. Facilitated Intramolecular Conjugate Addition of Amides of 3-(3',6'-Dioxo-2',4'-dimethyl-1',4'-cyclohexadienyl)-3,3-dimethylpropionic Acid. 2. Kinetics of Degradation. The Journal of Organic Chemistry. 61: 6633-6638. PMID 11667533 DOI: 10.1021/Jo961069L  0.323
1996 Burton PS, Conradi RA, Ho NF, Hilgers AR, Borchardt RT. How structural features influence the biomembrane permeability of peptides. Journal of Pharmaceutical Sciences. 85: 1336-40. PMID 8961149 DOI: 10.1021/Js960067D  0.371
1996 Pauletti GM, Gangwar S, Okumu FW, Siahaan TJ, Stella VJ, Borchardt RT. Esterase-sensitive cyclic prodrugs of peptides: Evaluation of an acyloxyalkoxy promoiety in a model hexapeptide Pharmaceutical Research. 13: 1615-1623. PMID 8956324 DOI: 10.1023/A:1016472119387  0.34
1996 Yuan CS, Ault-Riché DB, Borchardt RT. Chemical modification and site-directed mutagenesis of cysteine residues in human placental S-adenosylhomocysteine hydrolase. The Journal of Biological Chemistry. 271: 28009-16. PMID 8910410 DOI: 10.1074/Jbc.271.45.28009  0.328
1996 Wnuk SF, Liu S, Yuan CS, Borchardt RT, Robins MJ. Inactivation of S-adenosyl-L-homocysteine hydrolase by amide and ester derivatives of adenosine-5'-carboxylic acid. Journal of Medicinal Chemistry. 39: 4162-6. PMID 8863793 DOI: 10.1021/Jm960313Y  0.339
1996 Nerurkar MM, Burton PS, Borchardt RT. The use of surfactants to enhance the permeability of peptides through Caco-2 cells by inhibition of an apically polarized efflux system. Pharmaceutical Research. 13: 528-34. PMID 8710741 DOI: 10.1023/A:1016033702220  0.341
1996 Liu S, Yuan CS, Borchardt RT. Aristeromycin-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase. Journal of Medicinal Chemistry. 39: 2347-53. PMID 8691429 DOI: 10.1021/Jm950916U  0.314
1996 Nicolaou MG, Yuan C, Borchardt RT. Phosphate Prodrugs for Amines Utilizing a Fast Intramolecular Hydroxy Amide Lactonization The Journal of Organic Chemistry. 61: 8636-8641. DOI: 10.1021/Jo961477P  0.349
1996 Yuan CS, Liu S, Wnuk SF, Robins MJ, Borchardt RT. Design and synthesis of S-adenosylhomocysteine hydrolase inhibitors as broad-spectrum antiviral agents Advances in Antiviral Drug Design. 2: 41-88. DOI: 10.1016/S1075-8593(96)80103-1  0.323
1996 Pauletti GM, Gangwar S, Knipp GT, Nerurkar MM, Okumu FW, Tamura K, Siahaan TJ, Borchardt RT. Structural requirements for intestinal absorption of peptide drugs Journal of Controlled Release. 41: 3-17. DOI: 10.1016/0168-3659(96)01352-1  0.363
1996 Liu S, Wang B, Nicolaou MG, Borchardt RT. “Trimethyl lock” facilitated spirocyclizations: A structural analysis Journal of Chemical Crystallography. 26: 209-214. DOI: 10.1007/Bf01673672  0.472
1996 Wang B, Nicolaou MG, Liu S, Borchardt RT. Structural Analysis of a Facile Lactonization System Facilitated by a “Trimethyl Lock” Bioorganic Chemistry. 24: 39-49. DOI: 10.1006/Bioo.1996.0005  0.47
1995 Gupta RA, Yuan CS, Ault-Riché DB, Borchardt RT. Limited proteolysis of S-adenosylhomocysteine hydrolase: implications for the three-dimensional structure. Archives of Biochemistry and Biophysics. 319: 365-71. PMID 7786017 DOI: 10.1006/Abbi.1995.1306  0.348
1995 Chikhale EG, Chikhale PJ, Borchardt RT. Carrier-mediated transport of the antitumor agent acivicin across the blood-brain barrier Biochemical Pharmacology. 49: 941-945. PMID 7741766 DOI: 10.1016/0006-2952(95)00005-K  0.319
1995 Li S, Schöneich C, Borchardt RT. Chemical pathways of peptide degradation. VIII. Oxidation of methionine in small model peptides by prooxidant/transition metal ion systems: influence of selective scavengers for reactive oxygen intermediates. Pharmaceutical Research. 12: 348-55. PMID 7617519 DOI: 10.1023/A:1016240115675  0.307
1995 Yuan CS, Borchardt RT. Photoaffinity labeling of human placental S-adenosylhomocysteine hydrolase with [2-3H]8-azido-adenosine. The Journal of Biological Chemistry. 270: 16140-6. PMID 7608178 DOI: 10.1074/Jbc.270.27.16140  0.346
1995 Yuan C, Liu S, Wnuk S, Robins M, Borchardt R. Rational Approaches to the Design of Mechanism-Based Inhibitors of S-Adenosylhomocysteine Hydrolase Nucleosides, Nucleotides and Nucleic Acids. 14: 439-447. DOI: 10.1080/15257779508012403  0.341
1995 Wang B, Liu S, Borchardt RT. Development of a Novel Redox-Sensitive Protecting Group for Amines Which Utilizes a Facilitated Lactonization Reaction The Journal of Organic Chemistry. 60: 539-543. DOI: 10.1021/Jo00108A013  0.462
1994 Gray RA, Vander Velde DG, Burke CJ, Manning MC, Middaugh CR, Borchardt RT. Delta-sleep-inducing peptide: solution conformational studies of a membrane-permeable peptide. Biochemistry. 33: 1323-31. PMID 8312250 DOI: 10.1021/Bi00172A006  0.34
1994 Stevenson CL, Friedman AR, Kubiak TM, Donlan ME, Borchardt RT. Effect of secondary structure on the rate of deamidation of several growth hormone releasing factor analogs. International Journal of Peptide and Protein Research. 42: 497-503. PMID 8307680 DOI: 10.1111/J.1399-3011.1993.Tb00356.X  0.317
1994 Kim DC, Burton PS, Borchardt RT. A correlation between the permeability characteristics of a series of peptides using an in vitro cell culture model (Caco-2) and those using an in situ perfused rat ileum model of the intestinal mucosa. Pharmaceutical Research. 10: 1710-4. PMID 8302755 DOI: 10.1023/A:1018961828510  0.334
1994 Oliyai C, Borchardt RT. Chemical pathways of peptide degradation. VI. Effect of the primary sequence on the pathways of degradation of aspartyl residues in model hexapeptides. Pharmaceutical Research. 11: 751-8. PMID 8058648 DOI: 10.1023/A:1018944800691  0.319
1994 Chikhale EG, Ng KY, Burton PS, Borchardt RT. Hydrogen bonding potential as a determinant of the in vitro and in situ blood-brain barrier permeability of peptides. Pharmaceutical Research. 11: 412-9. PMID 8008709 DOI: 10.1023/A:1018969222130  0.358
1994 Miller DW, Keller BT, Borchardt RT. Identification and distribution of insulin receptors on cultured bovine brain microvessel endothelial cells: Possible function in insulin processing in the Blood-Brain barrier Journal of Cellular Physiology. 161: 333-341. PMID 7962117 DOI: 10.1002/Jcp.1041610218  0.441
1994 Yuan CS, Wnuk SF, Liu S, Robins MJ, Borchardt RT. (E)-5',6'-didehydro-6'-deoxy-6'-fluorohomoadenosine: a substrate that measures the hydrolytic activity of S-adenosylhomocysteine hydrolase. Biochemistry. 33: 12305-11. PMID 7918452 DOI: 10.1021/Bi00206A038  0.306
1994 Borchardt RT. Rational Delivery Strategies for the Design of Peptides with Enhanced Oral Delivery Drug Development and Industrial Pharmacy. 20: 469-483. DOI: 10.3109/03639049409038313  0.352
1994 Robins MJ, Wnuk SF, Mullah KB, Dalley NK, Yuan C, Lee Y, Borchardt RT. Nucleic Acid Related Compounds. 80. Synthesis of 5'-S-(Alkyl and aryl)-5'-fluoro-5'-thioadenosines with Xenon Difluoride or (Diethylamido)sulfur Trifluoride, Hydrolysis in Aqueous Buffer, and Inhibition of S-Adenosyl-L-homocysteine hydrolase by derived "Adenosine 5'-Aldehyde" Species The Journal of Organic Chemistry. 59: 544-555. DOI: 10.1021/Jo00082A010  0.31
1993 Liu S, Wnuk SF, Yuan C, Robins MJ, Borchardt RT. Adenosine-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase. Journal of Medicinal Chemistry. 36: 883-7. PMID 8464042 DOI: 10.1021/Jm00059A013  0.306
1993 Oliyai C, Borchardt RT. Chemical pathways of peptide degradation. IV. Pathways, kinetics, and mechanism of degradation of an aspartyl residue in a model hexapeptide. Pharmaceutical Research. 10: 95-102. PMID 8430066 DOI: 10.1023/A:1018981231468  0.307
1993 Stevenson CL, Donlan ME, Friedman AR, Borchardt RT. Solution conformation of Leu27 hGRF(1-32)NH2 and its deamidation products by 2D NMR. International Journal of Peptide and Protein Research. 42: 24-32. PMID 8370640 DOI: 10.1111/J.1399-3011.1993.Tb00345.X  0.316
1993 Tang AS, Chikhale PJ, Shah PK, Borchardt RT. Utilization of a Human Intestinal Epithelial Cell Culture System (Caco-2) for Evaluating Cytoprotective Agents Pharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists. 10: 1620-1626. PMID 8290475 DOI: 10.1023/A:1018976804403  0.314
1993 Li S, Schöneich C, Wilson GS, Borchardt RT. Chemical pathways of peptide degradation. V. Ascorbic acid promotes rather than inhibits the oxidation of methionine to methionine sulfoxide in small model peptides. Pharmaceutical Research. 10: 1572-9. PMID 8290469 DOI: 10.1023/A:1018960300769  0.345
1993 Schöneich C, Zhao F, Wilson GS, Borchardt RT. Iron-thiolate induced oxidation of methionine to methionine sulfoxide in small model peptides. Intramolecular catalysis by histidine. Biochimica Et Biophysica Acta. 1158: 307-22. PMID 8251532 DOI: 10.1016/0304-4165(93)90030-C  0.325
1993 Kim DC, Harrison AW, Ruwart MJ, Wilkinson KF, Fisher JF, Hidalgo IJ, Borchardt RT. Evaluation of the bile acid transporter in enhancing intestinal permeability to renin-inhibitory peptides. Journal of Drug Targeting. 1: 347-59. PMID 8069578 DOI: 10.3109/10611869308996094  0.355
1993 Stevenson CL, Williams TD, Anderegg RJ, Borchardt RT. Identification and quantitation of tetrapeptide deamidation products by mass spectrometry. Journal of Pharmaceutical and Biomedical Analysis. 10: 567-75. PMID 1463791 DOI: 10.1016/0731-7085(92)80082-X  0.303
1993 Hasobe M, Liang H, Ault-Riche DB, Borcherding DR, Wolfe MS, Borchardt RT. (1′R, 2′S, 3′R)-9-(2′, 3′-Dihydroxycyclopentan-1′-yl)-Adenine and −3-Deaza-Adenine: Analogues of Aristeromycin Which Exhibit Potent Antiviral Activity with Reduced Cytotoxicity: Antiviral Chemistry & Chemotherapy. 4: 245-248. DOI: 10.1177/095632029300400408  0.335
1993 Ishii H, Hasobe M, McKee JG, Ault-Riché DB, Borchardt RT. Synergistic Antiviral Activity of Inhibitors of S-Adenosylhomocysteine Hydrolase and Ribavirin Antiviral Chemistry & Chemotherapy. 4: 127-130. DOI: 10.1177/095632029300400207  0.321
1992 Hu M, Borchardt RT. Transport of a large neutral amino acid in a human intestinal epithelial cell line (Caco-2): uptake and efflux of phenylalanine. Biochimica Et Biophysica Acta. 1135: 233-44. PMID 1623010 DOI: 10.1016/0167-4889(92)90226-2  0.319
1992 Robins MJ, Samano V, Zhang W, Balzarini J, De Clercq E, Borchardt RT, Lee Y, Yuan CS. Nucleic acid related compounds. 74. Synthesis and biological activity of 2'(and 3')-deoxy-2'(and 3')-methylenenucleoside analogues that function as mechanism-based inhibitors of S-adenosyl-L-homocysteine hydrolase and/or ribonucleotide reductase. Journal of Medicinal Chemistry. 35: 2283-93. PMID 1613752 DOI: 10.1021/Jm00090A020  0.329
1992 Wolfe MS, Lee Y, Bartlett WJ, Borcherding DR, Borchardt RT. 4'-modified analogues of aristeromycin and neplanocin A: synthesis and inhibitory activity toward S-adenosyl-L-homocysteine hydrolase. Journal of Medicinal Chemistry. 35: 1782-91. PMID 1588558 DOI: 10.1021/Jm00088A013  0.338
1992 Wolfe JL, Vander Velde D, Borchardt RT. Facilitated intramolecular conjugate addition of N-(p-methoxyphenyl)-3-(3',6'-dioxo-2',4'-dimethylcyclohexa-1',4'-dienyl)-3,3-dimethylpropionamide. 1. Product characterization The Journal of Organic Chemistry. 57: 6138-6142. DOI: 10.1021/Jo00049A018  0.315
1992 Miller DW, Audus KL, Borchardt RT. Application of cultured endothelial cells of the brain microvasculature in the study of the blood-brain barrier Journal of Tissue Culture Methods. 14: 217-224. DOI: 10.1007/Bf01409014  0.46
1991 Hu M, Borchardt RT. Mechanism of L-alpha-methyldopa transport through a monolayer of polarized human intestinal epithelial cells (Caco-2). Pharmaceutical Research. 7: 1313-9. PMID 2095572 DOI: 10.1023/A:1015906409585  0.304
1991 Shah PK, Borchardt RT. A comparison of peptidase activities and peptide metabolism in cultured mouse keratinocytes and neonatal mouse epidermis. Pharmaceutical Research. 8: 70-5. PMID 2014210 DOI: 10.1023/A:1015882323677  0.309
1991 Yeh JC, Borchardt RT, Vedani A. A molecular model for the active site of S-adenosyl-L-homocysteine hydrolase. Journal of Computer-Aided Molecular Design. 5: 213-34. PMID 1919618 DOI: 10.1007/Bf00124340  0.318
1991 Baranczyk-Kuzma A, Garren JA, Hidalgo IJ, Borchardt RT. Substrate specificity and some properties of phenol sulfotransferase from human intestinal Caco-2 cells. Life Sciences. 49: 1197-206. PMID 1910139 DOI: 10.1016/0024-3205(91)90568-V  0.324
1991 Sufrin JR, Spiess AJ, Kramer DL, Libby PR, Miller JT, Bernacki RJ, Lee YH, Borchardt RT, Porter CW. Targeting 5'-deoxy-5'-(methylthio)adenosine phosphorylase by 5'-haloalkyl analogues of 5'-deoxy-5'-(methylthio)adenosine. Journal of Medicinal Chemistry. 34: 2600-6. PMID 1908523 DOI: 10.1021/Jm00112A039  0.326
1990 Patel K, Borchardt RT. Chemical pathways of peptide degradation. II. Kinetics of deamidation of an asparaginyl residue in a model hexapeptide. Pharmaceutical Research. 7: 703-11. PMID 2395797 DOI: 10.1023/A:1015807303766  0.32
1990 Patel K, Borchardt RT. Chemical pathways of peptide degradation. III. Effect of primary sequence on the pathways of deamidation of asparaginyl residues in hexapeptides. Pharmaceutical Research. 7: 787-93. PMID 2235875 DOI: 10.1023/A:1015999012852  0.337
1990 Hidalgo IJ, Borchardt RT. Transport of a large neutral amino acid (phenylalanine) in a human intestinal epithelial cell line: Caco-2. Biochimica Et Biophysica Acta. 1028: 25-30. PMID 2207118 DOI: 10.1016/0005-2736(90)90261-L  0.31
1990 Audus KL, Bartel RL, Hidalgo IJ, Borchardt RT. The Use of Cultured Epithelial and Endothelial Cells for Drug Transport and Metabolism Studies Pharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists. 7: 435-451. PMID 2195492 DOI: 10.1023/A:1015800312910  0.313
1990 Bhatt NP, Patel K, Borchardt RT. Chemical pathways of peptide degradation. I. Deamidation of adrenocorticotropic hormone. Pharmaceutical Research. 7: 593-9. PMID 2164192 DOI: 10.1023/A:1015862026539  0.322
1990 Borchardt RT. Assessment of Transport Barriers Using Cell and Tissue Culture Systems Drug Development and Industrial Pharmacy. 16: 2595-2612. DOI: 10.3109/03639049009058549  0.326
1989 Shah MV, Audus KL, Borchardt RT. The Application of Bovine Brain Microvessel Endothelial-Cell Monolayers Grown onto Polycarbonate Membranes in Vitro to Estimate the Potential Permeability of Solutes Through the Blood–Brain Barrier Pharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists. 6: 624-627. PMID 2798313 DOI: 10.1023/A:1015913817221  0.302
1989 Baranczyk-Kuzma A, Audus KL, Borchardt RT. Substrate specificity of phenol sulfotransferase from primary cultures of bovine brain microvessel endothelium Neurochemical Research. 14: 689-691. PMID 2779729 DOI: 10.1007/Bf00964880  0.328
1989 Smith KR, Borchardt RT. Permeability and Mechanism of Albumin, Cationized Albumin, and Glycosylated Albumin Transcellular Transport Across Monolayers of Cultured Bovine Brain Capillary Endothelial Cells Pharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists. 6: 466-473. PMID 2762222 DOI: 10.1023/A:1015960205409  0.312
1989 Scriba GK, Borchardt RT. Metabolism of catecholamine esters by cultured bovine brain microvessel endothelial cells. Journal of Neurochemistry. 53: 610-5. PMID 2746238 DOI: 10.1111/J.1471-4159.1989.Tb07377.X  0.336
1989 Borchardt R, Mazer N, Rytting J, Shek E, Ziv E, Touitou E, Higuchi W. The delivery of peptides Journal of Pharmaceutical Sciences. 78: 883-892. DOI: 10.1002/Jps.2600781102  0.317
1988 Smith KR, Kato A, Borchardt RT. Characterization of specific receptors for atrial natriuretic factor on cultured bovine brain capillary endothelial cells Biochemical and Biophysical Research Communications. 157: 308-314. PMID 2848519 DOI: 10.1016/S0006-291X(88)80048-2  0.309
1988 van Nispen JW, Hichens M, Sauter A, Lingeman H, Cubbins DC, McMartin C, Webb RL, Wennogle LP, Wysowskyi HE, Zimmerman MB, Lee VHL, Sandow J, Seidel H, Schmiedel R, Keller BT, ... ... Borchardt RT, et al. Abstracts of lectures symposium disposition and delivery of peptide drugs Pharmaceutisch Weekblad. 10: 30-50. DOI: 10.1007/Bf01966433  0.303
1987 Matuszewska B, Borchardt RT. The mechanism of inhibition of Alcaligenes faecalis S-adenosylhomocysteine hydrolase by neplanocin A. Archives of Biochemistry and Biophysics. 256: 50-5. PMID 3606132 DOI: 10.1016/0003-9861(87)90424-3  0.305
1987 Fisher EW, Decedue CJ, Keller BT, Borchardt RT. Neplanocin A inhibition of S-adenosylhomocysteine hydrolase in Alcaligenes faecalis has no effect on growth of the microorganism. The Journal of Antibiotics. 40: 873-81. PMID 3112082 DOI: 10.7164/Antibiotics.40.873  0.308
1987 Hasobe M, McKee JG, Borcherding DR, Borchardt RT. 9-(trans-2',trans-3'-Dihydroxycyclopent-4'-enyl)-adenine and -3-deazaadenine: analogs of neplanocin A which retain potent antiviral activity but exhibit reduced cytotoxicity. Antimicrobial Agents and Chemotherapy. 31: 1849-51. PMID 2449123 DOI: 10.1128/Aac.31.11.1849  0.316
1987 Ramakrishnan V, Borchardt RT. Adenosine dialdehyde and neplanocin A: Potent inhibitors of S-adenosylhomocysteine hydrolase in neuroblastoma N2a cells Neurochemistry International. 10: 423-431. DOI: 10.1016/0197-0186(87)90068-4  0.329
1986 Patel-Thombre U, Borchardt RT. Adenine nucleoside dialdehydes: potent inhibitors of bovine liver S-adenosylhomocysteine hydrolase. Biochemistry. 24: 1130-6. PMID 4096893 DOI: 10.1021/Bi00326A010  0.326
1986 Bartel RL, Borchardt RT. Quantitation of S-adenosylhomocysteine hydrolase in mouse L929 cells using the inhibitor neplanocin A. Analytical Biochemistry. 149: 191-6. PMID 4073475 DOI: 10.1016/0003-2697(85)90494-4  0.336
1986 Audus KL, Borchardt RT. Characteristics of the large neutral amino acid transport system of bovine brain microvessel endothelial cell monolayers Journal of Neurochemistry. 47: 484-488. PMID 3734791 DOI: 10.1111/J.1471-4159.1986.Tb04527.X  0.32
1986 Baranczyk-Kuzma A, Audus KL, Borchardt RT. Catecholamine-metabolizing enzymes of bovine brain microvessel endothelial cell monolayers Journal of Neurochemistry. 46: 1956-1960. PMID 2871135 DOI: 10.1111/J.1471-4159.1986.Tb08519.X  0.308
1986 Audus KL, Borchardt RT. Characterization of an In Vitro Blood–Brain Barrier Model System for Studying Drug Transport and Metabolism Pharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists. 3: 81-87. DOI: 10.1023/A:1016337202335  0.321
1985 Porter PA, Osiecka I, Borchardt RT, Fix JA, Frost L, Gardner C. In Vitro Drug Absorption Models. II. Salicylate, Cefoxitin, α-Methyldopa and Theophylline Uptake in Cells and Rings: Correlation with In Vivo Bioavailability. Pharmaceutical Research. 2: 293-8. PMID 24271126 DOI: 10.1023/A:1016393618111  0.313
1985 Osiecka I, Porter PA, Borchardt RT, Fix JA, Gardner CR. In vitro drug absorption models. I. Brush border membrane vesicles, isolated mucosal cells and everted intestinal rings: characterization and salicylate accumulation. Pharmaceutical Research. 2: 284-93. PMID 24271125 DOI: 10.1023/A:1016341601273  0.332
1985 Matuszewska B, Borchardt RT. Rat kidney histamine N-methyltransferase: purification and partial characterization. Preparative Biochemistry. 15: 145-57. PMID 4059182 DOI: 10.1080/10826068508062268  0.311
1985 Houston DM, Matuszewska B, Borchardt RT. Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 10. Base- and amino acid modified analogues of S-aristeromycinyl-L-homocysteine. Journal of Medicinal Chemistry. 28: 478-82. PMID 3981540 DOI: 10.1002/Chin.198531335  0.325
1985 Houston DM, Dolence EK, Keller BT, Patel-Thombre U, Borchardt RT. Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 9. 2',3'-Dialdehyde derivatives of carbocyclic purine nucleosides as inhibitors of S-adenosylhomocysteine hydrolase. Journal of Medicinal Chemistry. 28: 471-7. PMID 3981539 DOI: 10.1002/Chin.198531336  0.324
1985 Houston DM, Dolence EK, Keller BT, Patel-Thombre U, Borchardt RT. Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 8. Molecular dissections of carbocyclic 3-deazaadenosine as inhibitors of S-adenosylhomocysteine hydrolase. Journal of Medicinal Chemistry. 28: 467-71. PMID 3981538 DOI: 10.1002/Chin.198531233  0.315
1984 Keller BT, Borchardt RT. Metabolic conversion of neplanocin A to S-neplanocylmethionine by mouse L 929 cells. Biochemical and Biophysical Research Communications. 120: 131-7. PMID 6712684 DOI: 10.1016/0006-291X(84)91423-2  0.338
1984 Liang NY, Chandra A, Tessel RE, Grunewald GL, Borchardt RT. Inhibitors of phenylethanolamine-N-methyltransferase: effects on brain catecholamine content and blood pressure in DOCA-salt hypertensive rats. Research Communications in Chemical Pathology and Pharmacology. 46: 319-29. PMID 6515125 DOI: 10.1016/S0022-5347(17)49412-2  0.605
1983 Borchardt RT, Schasteen CS, Wu SE. Phenol sulfotransferase. II. Inactivation by phenylglyoxal, N-ethylmaleimide and ribonucleotide 2',3'-dialdehydes. Biochimica Et Biophysica Acta. 708: 280-93. PMID 6959651 DOI: 10.1016/0167-4838(82)90438-1  0.337
1983 Borchardt RT, Schasteen CS. Phenol sulfotransferase. I. Purification of a rat liver enzyme by affinity chromatography. Biochimica Et Biophysica Acta. 708: 272-9. PMID 6959650 DOI: 10.1016/0167-4838(82)90437-X  0.324
1982 Rafferty MF, Krass P, Borchardt RT, Grunewald GL. Importance of the aromatic ring in adrenergic amines. 8. 2-(Aminomethyl)-trans-2-decalols as inhibitors of norepinephrine N-methyltransferase. Journal of Medicinal Chemistry. 25: 1250-2. PMID 7143367 DOI: 10.1002/Chin.198311323  0.318
1982 Grunewald GL, Monn JA, Rafferty MF, Borchardt RT, Krass P. Probes of the active site of norepinephrine N-methyltransferase: effect of hydrophobic and hydrophilic interactions on side-chain binding of amphetamine and alpha-methylbenzylamine. Journal of Medicinal Chemistry. 25: 1248-50. PMID 7143366 DOI: 10.1002/Chin.198311322  0.312
1982 Rafferty MF, Borchardt RT, Grunewald GL. Directional probes of the hydrophobic component of the aromatic ring binding site of norepinephrine N-methyltransferase. Journal of Medicinal Chemistry. 25: 1204-8. PMID 7143357 DOI: 10.1002/Chin.198310180  0.309
1982 Rafferty MF, Wilson DS, Monn JA, Krass P, Borchardt RT, Grunewald GL. Importance of the aromatic ring in adrenergic amines. 7. Comparison of the stereoselectivity of norepinephrine N-methyltransferase for aromatic vs. nonaromatic substrates and inhibitors. Journal of Medicinal Chemistry. 25: 1198-204. PMID 7143356 DOI: 10.1002/Chin.198310168  0.328
1982 Borchardt RT, Huber JA. Catechol O-methyltransferase. 11. Inactivation by 5-hydroxy-3-mercapto-4-methoxybenzoic acid Journal of Medicinal Chemistry. 25: 321-323. PMID 7069707 DOI: 10.1021/Jm00345A017  0.323
1982 Borchardt RT, Bhatia P. Catechol O-methyltransferase. 12. Affinity labeling the active site with the oxidation products of 5,6-dihydroxyindole Journal of Medicinal Chemistry. 25: 263-271. PMID 7069705 DOI: 10.1002/Chin.198233173  0.338
1982 Borchardt RT, Huber JA, Houston M. Catechol o-methyltransferase. 10. 5-Substituted 3-hydroxy-4-methoxybenzoic acids (isovanillic acids) and 5-substituted 3-hydroxy-4-methoxybenzaldehydes (isovanillins) as potential inhibitors Journal of Medicinal Chemistry. 25: 258-263. PMID 7069704 DOI: 10.1002/Chin.198233149  0.316
1981 Pegg AE, Borchardt RT, Coward JK. Effects of inhibitors of spermidine and spermine synthesis on polyamine concentrations and growth of transformed mouse fibroblasts. The Biochemical Journal. 194: 79-89. PMID 7305994 DOI: 10.1042/Bj1940079  0.307
1981 Davis DP, Borchardt RT, Grunewald GL. Importance of the aromatic ring in adrenergic amines. 6. Nonaromatic analogues of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: role of pi-electronic and steric interactions. Journal of Medicinal Chemistry. 24: 12-6. PMID 7205869 DOI: 10.1002/Chin.198123180  0.301
1980 Hibasami H, Borchardt RT, Chen SY, Coward JK, Pegg AE. Studies of inhibition of rat spermidine synthase and spermine synthase. The Biochemical Journal. 187: 419-28. PMID 7396856 DOI: 10.1042/Bj1870419  0.326
1978 Borchardt RT, Wu YS, Wu BS. Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 7. Role of the ribosyl moiety in enzymatic binding of S-adenosyl-L-homocysteine and S-adenosyl-L-methionine. Journal of Medicinal Chemistry. 21: 1307-10. PMID 722739 DOI: 10.1002/Chin.197918371  0.3
1978 Borchardt RT, Wu YS, Wu BS. Affinity labeling of histamine N-methyltransferase by 2',3'-dialdehyde derivatives of S-adenosylhomocysteine and S-adenosylmethionine. Kinetics of inactivation. Biochemistry. 17: 4145-52. PMID 708699 DOI: 10.1021/Bi00613A007  0.303
1978 Tessel RE, Kennedy LE, Burgess SK, Borchardt RT. Epinephrine in rat hypothalamus: antagonism by desipramine of 6-hydroxydopamine-induced depletion. Brain Research. 153: 615-7. PMID 698800 DOI: 10.1016/0006-8993(78)90347-5  0.593
1978 Leboy PS, Glick JM, Steiner FG, Haney S, Borchardt RT. S-adenosylhomocysteine analogues as inhibitors of specific tRNA methylation Bba Section Nucleic Acids and Protein Synthesis. 520: 153-163. PMID 698227 DOI: 10.1016/0005-2787(78)90016-3  0.355
1978 Borchardt RT, Wu SE, Schasteen CS. Adenosine 5'-diphosphate dialdehyde: an affinity labeling reagent for phenol-sulfotransferase. Biochemical and Biophysical Research Communications. 81: 841-9. PMID 666796 DOI: 10.1016/0006-291X(78)91428-6  0.332
1978 Borchardt RT, Cheng CF. Purification and characterization of rat liver microsomal thiol methyltransferase. Biochimica Et Biophysica Acta. 522: 340-53. PMID 623768 DOI: 10.1016/0005-2744(78)90068-2  0.327
1978 Borchardt R, Cheng CF. Purification and characterization of rat heart and brain catechol methyltransferase. Biochimica Et Biophysica Acta. 522: 49-62. PMID 413582 DOI: 10.1016/0005-2744(78)90321-2  0.313
1977 Borchardt RT, Schasteen CS. Phenol-sulfotransferase inactivation by 2,3-butanedione and phenylglyoxal: evidence for an active site arginyl residue. Biochemical and Biophysical Research Communications. 78: 1067-73. PMID 911328 DOI: 10.1016/0006-291X(77)90529-0  0.318
1977 Borchardt RT, Wu YS, Wu BS. S-adenosyl-L-homocysteine dialdehyde: an affinity labeling reagent for histamine-N-methyltransferase. Biochemical and Biophysical Research Communications. 78: 1025-33. PMID 911324 DOI: 10.1016/0006-291X(77)90524-1  0.331
1977 Borchardt RT, Thakker DR. Labeling of catechol-O-methyltransferase with N-haloacetyl derivatives. Methods in Enzymology. 46: 554-61. PMID 909444 DOI: 10.1016/S0076-6879(77)46068-3  0.32
1976 Borchardt RT, Smissman EE, Nerland D, Reid JR. Catechol O methyltransferase. 7. Affinity labeling with the oxidation products of 6 aminodopamine Journal of Medicinal Chemistry. 19: 30-37. PMID 1246049 DOI: 10.1002/Chin.197617179  0.774
1976 Smissman EE, Reid JR, Walsh DA, Borchardt RT. Synthesis and biological activity of 2- and 4-substituted 6,7-dihydroxy-1,2,3,4-tetrahydroisoquinolines Journal of Medicinal Chemistry. 19: 127-131. PMID 1246034 DOI: 10.1002/Chin.197617239  0.582
1976 Borchardt RT, Reid JR, Thakker DR. Catechol O-methyltransferase. 9. Mechanism of inactivation by 6-hydroxydopamine. Journal of Medicinal Chemistry. 19: 1201-9. PMID 994150 DOI: 10.1002/Chin.197705184  0.351
1976 Borchardt RT, Wu YS, Huber JA, Wycpalek AF. Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 6. Structural modifications of S-adenosylmethionine Journal of Medicinal Chemistry. 19: 1104-1110. PMID 978675 DOI: 10.1002/Chin.197652393  0.332
1976 Borchardt RT, Huber JA, Wu YS. Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 4. Further modifications of the amino acid and base portions of S-adenosyl-L-homocysteine Journal of Medicinal Chemistry. 19: 1094-1099. PMID 978673 DOI: 10.1021/Jm00231A003  0.307
1976 Borchardt RT, Thakker DR, Warner VD, Mirth DB, Sane JN. Catechol O-methyltransferase. 8. Structure-activity relationships for inhibtion by 8-hydroxyquinolines. Journal of Medicinal Chemistry. 19: 558-60. PMID 817025 DOI: 10.1021/Jm00226A025  0.305
1976 Borchardt RT, Thakker DR. Evidence for sulfhydryl groups at the active site of catechol-O-methyltransferase. Biochimica Et Biophysica Acta. 445: 598-609. PMID 9991 DOI: 10.1016/0005-2744(76)90113-3  0.328
1976 SMISSMAN EE, REID JR, WALSH DA, BORCHARDT RT. ChemInform Abstract: SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2- AND 4-SUBSTITUTED 6,7-DIHYDROXY-1,2,3,4-TETRAHYDROISOQUINOLINES Chemischer Informationsdienst. 7: no-no. DOI: 10.1002/chin.197617239  0.513
1976 BORCHARDT RT, SMISSMAN EE, NERLAND D, REID JR. ChemInform Abstract: CATECHOL O-METHYLTRANSFERASE. 7. AFFINITY LABELING WITH THE OXIDATION PRODUCTS OF 6-AMINODOPAMINE Chemischer Informationsdienst. 7: no-no. DOI: 10.1002/chin.197617179  0.734
1975 Borchardt RT, Wu YS. Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 3. Modifications of the sugar portion of S-adenosylhomocysteine. Journal of Medicinal Chemistry. 18: 300-4. PMID 1133821 DOI: 10.1021/Jm00237A018  0.312
1975 Borchardt RT, Cheng CF, Thakker DR. Purification of catechol-O-methyltransferase by affinity chromatography. Biochemical and Biophysical Research Communications. 63: 69-77. PMID 1125027 DOI: 10.1016/S0006-291X(75)80012-X  0.3
1975 Borchardt RT, Thakker DR. Catechol O-methyltransferase. 6. Affinity labeling with N-haloacetyl-3,5-dimethoxy-4-hydroxyphenylalkylamines. Journal of Medicinal Chemistry. 18: 152-8. PMID 1120981 DOI: 10.1021/Jm00236A008  0.318
1975 Borchardt RT, Thakker DR. Affinity labeling of catechol O-methyltransferase by N-haloacetyl derivatives of 3,5-dimethoxy-4-hydroxyphenylethylamine and 3,4-dimethoxy-5-hydroxyphenylethylamine. Kinetics of inactivation. Biochemistry. 14: 4543-51. PMID 240407 DOI: 10.1021/Bi00691A033  0.329
1974 Borchardt RT, Huber JA, Wu YS. Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 2. Modification of the base portion of S-adenosylhomocysteine Journal of Medicinal Chemistry. 17: 868-873. PMID 4845380 DOI: 10.1021/Jm00254A017  0.349
1973 Borchardt RT, Thakker D. Affinity labeling of catechol-O-methyltransferase with N-iodoacetyl-3,5-dimethoxy-4-hydroxyphenylethylamine. Biochemical and Biophysical Research Communications. 54: 1233-9. PMID 4753192 DOI: 10.1016/0006-291X(73)90824-3  0.31
1972 Smissman EE, Borchardt RT, Schowen KB. Conformational aspects of systems related to acetylcholine. 4. The syntheses of the dl-2-dimethylamino-trans-decalin methiodides. Journal of Medicinal Chemistry. 15: 545-8. PMID 5035280 DOI: 10.1021/Jm00275A027  0.529
1972 SMISSMAN EE, BORCHARDT RT, SCHOWEN KB. ChemInform Abstract: KONFORMATIVE ASPEKTE BEI MIT ACETYLCHOLIN VERWANDTEN SYST. 4. MITT. DIE SYNTH. DER D,L-2-DIMETHYLAMINO-TRANS-DECALIN-METHOJODIDE Chemischer Informationsdienst. 3: no-no. DOI: 10.1002/Chin.197236242  0.522
1971 Smissman EE, Borchardt RT. A conformational study of catecholamine receptor sites. 5. Syntheses of dl-3-amino-2-(3,4-dihydroxyphenyl)-trans-2-decalol hydrochlorides. Journal of Medicinal Chemistry. 14: 377-82. PMID 5117682 DOI: 10.1021/Jm00287A001  0.553
1971 Smissman EE, Borchardt RT. Conformational study oof catecholamine receptor sites. 7. Syntheses of erythro- and threo-3-amino-2-(3,4-dihydroxyphenyl)-2-butanol hydrochlorides and erythro- and threo-2-amino-3-(3,4-dihydroxyphenyl)butane hydrochlorides. Journal of Medicinal Chemistry. 14: 702-7. PMID 5114066 DOI: 10.1021/Jm00290A008  0.565
1971 Smissman E, Borchardt R. Additions and Corrections - A Conformational Study of Catecholamine Receptor Sites. 5. Syntheses of dl-3-Amino-2-(3,4-dihydroxyphenyl)-trans-2-decalol Hydrochlorides. Journal of Medicinal Chemistry. 14: 1251-1251. DOI: 10.1021/jm00294a609  0.508
1971 SMISSMAN EE, BORCHARDT RT. ChemInform Abstract: KONFORM.-STUDIE UEBER DIE CATECHOLAMIN-REZEPTORSTELLEN 7. MITT. SYNTH. VON ERYTHRO- UND THREO-3-AMINO-2-(3,4-DIHYDROXYPHENYL)-BUTANOL-(2)-HYDROCHLORIDEN UND ERYTHRO- UND THREO-2-AMINO-3-(3,4-DIHYDROXYPHENYL)-BUTANHYDROCHLORIDEN Chemischer Informationsdienst. Organische Chemie. 2: no-no. DOI: 10.1002/chin.197150257  0.515
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