Dhiren R. Thakker - Publications

Affiliations: 
University of North Carolina, Chapel Hill, Chapel Hill, NC 
Area:
Pharmacy, Molecular Biology, Biochemistry

128 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
2019 Cai H, Everett R, Thakker DR. Efficacious Dose of Metformin for Breast Cancer Therapy is Determined by Cation Transporter Expression in Tumors. British Journal of Pharmacology. PMID 31032880 DOI: 10.1111/bph.14694  0.52
2016 Proctor WR, Ming X, Bourdet D, Han TK, Everett RS, Thakker DR. Why Does the Intestine Lack Basolateral Efflux Transporters for Cationic Compounds? A Provocative Hypothesis. Journal of Pharmaceutical Sciences. 105: 484-96. PMID 26869413 DOI: 10.1016/j.xphs.2015.11.040  1
2016 Chen Y, Zane NR, Thakker DR, Wang MZ. Quantification of Flavin-containing Monooxygenases 1, 3 and 5 in Human Liver Microsomes by UPLC-MRM-based Targeted Quantitative Proteomics and Its Application to the Study of Ontogeny. Drug Metabolism and Disposition: the Biological Fate of Chemicals. PMID 26839369 DOI: 10.1124/dmd.115.067538  1
2015 Cai H, Zhang Y, Han TK, Everett RS, Thakker DR. Cation-selective transporters are critical to the ampk-mediated antiproliferative effects of metformin in human breast cancer cells. International Journal of Cancer. Journal International Du Cancer. PMID 26669511 DOI: 10.1002/ijc.29965  1
2015 Schowen KB, Schowen RL, Borchardt SE, Borchardt PM, Artursson P, Audus KL, Augustijns P, Nicolazzo JA, Raub TJ, Schöneich C, Siahaan TJ, Takakura Y, Thakker DR, Wolfe MS. A Tribute to Ronald T. Borchardt-Teacher, Mentor, Scientist, Colleague, Leader, Friend, and Family Man. Journal of Pharmaceutical Sciences. PMID 26453244 DOI: 10.1002/jps.24687  1
2015 Zane NR, Thakker DR. Response to: "Prediction of Voriconazole Non-Linear Pharmacokinetics Using a Paediatric Physiologically Based Pharmacokinetic Modelling Approach". Clinical Pharmacokinetics. 54: 569-72. PMID 25735635 DOI: 10.1007/s40262-015-0254-6  1
2015 Han TK, Proctor WR, Costales CL, Cai H, Everett RS, Thakker DR. Four cation-selective transporters contribute to apical uptake and accumulation of metformin in Caco-2 cell monolayers. The Journal of Pharmacology and Experimental Therapeutics. 352: 519-28. PMID 25563903 DOI: 10.1124/jpet.114.220350  1
2014 Zane NR, Thakker DR. A physiologically based pharmacokinetic model for voriconazole disposition predicts intestinal first-pass metabolism in children. Clinical Pharmacokinetics. 53: 1171-82. PMID 25245942 DOI: 10.1007/s40262-014-0181-y  1
2014 Steeb DR, Joyner PU, Thakker DR. Exploring the role of the pharmacist in global health. Journal of the American Pharmacists Association : Japha. 54: 552-5. PMID 25216886 DOI: 10.1331/JAPhA.2014.13251  1
2014 Alluri RV, Ward P, Kunta JR, Ferslew BC, Thakker DR, Dallas S. In vitro characterization of intestinal and hepatic transporters: MRP2 Methods in Pharmacology and Toxicology. 369-404. DOI: 10.1007/978-1-62703-742-6-22  1
2013 Dufek MB, Bridges AS, Thakker DR. Intestinal first-pass metabolism by cytochrome p450 and not p-glycoprotein is the major barrier to amprenavir absorption. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 41: 1695-702. PMID 23821186 DOI: 10.1124/dmd.113.052191  1
2013 Han TK, Everett RS, Proctor WR, Ng CM, Costales CL, Brouwer KL, Thakker DR. Organic cation transporter 1 (OCT1/mOct1) is localized in the apical membrane of Caco-2 cell monolayers and enterocytes. Molecular Pharmacology. 84: 182-9. PMID 23680637 DOI: 10.1124/mol.112.084517  1
2013 Swift B, Nebot N, Lee JK, Han T, Proctor WR, Thakker DR, Lang D, Radtke M, Gnoth MJ, Brouwer KL. Sorafenib hepatobiliary disposition: mechanisms of hepatic uptake and disposition of generated metabolites. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 41: 1179-86. PMID 23482500 DOI: 10.1124/dmd.112.048181  1
2013 Dufek MB, Knight BM, Bridges AS, Thakker DR. P-glycoprotein increases portal bioavailability of loperamide in mouse by reducing first-pass intestinal metabolism. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 41: 642-50. PMID 23288866 DOI: 10.1124/dmd.112.049965  1
2013 Generaux CN, Ainslie GR, Bridges AS, Ismail MA, Boykin DW, Tidwell RR, Thakker DR, Paine MF. Compartmental and enzyme kinetic modeling to elucidate the biotransformation pathway of a centrally acting antitrypanosomal prodrug. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 41: 518-28. PMID 23223498 DOI: 10.1124/dmd.112.048231  1
2011 Ming X, Knight BM, Thakker DR. Vectorial transport of fexofenadine across Caco-2 cells: involvement of apical uptake and basolateral efflux transporters. Molecular Pharmaceutics. 8: 1677-86. PMID 21780830 DOI: 10.1021/mp200026v  1
2011 Yanni SB, Smith PB, Benjamin DK, Augustijns PF, Thakker DR, Annaert PP. Higher clearance of micafungin in neonates compared with adults: role of age-dependent micafungin serum binding. Biopharmaceutics & Drug Disposition. 32: 222-32. PMID 21449041 DOI: 10.1002/bdd.752  1
2011 Klein RR, Bourdon DM, Costales CL, Wagner CD, White WL, Williams JD, Hicks SN, Sondek J, Thakker DR. Direct activation of human phospholipase C by its well known inhibitor u73122. The Journal of Biological Chemistry. 286: 12407-16. PMID 21266572 DOI: 10.1074/jbc.M110.191783  1
2010 Yanni SB, Augustijns PF, Benjamin DK, Brouwer KL, Thakker DR, Annaert PP. In vitro investigation of the hepatobiliary disposition mechanisms of the antifungal agent micafungin in humans and rats. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 38: 1848-56. PMID 20606004 DOI: 10.1124/dmd.110.033811  1
2010 Yanni SB, Annaert PP, Augustijns P, Ibrahim JG, Benjamin DK, Thakker DR. In vitro hepatic metabolism explains higher clearance of voriconazole in children versus adults: role of CYP2C19 and flavin-containing monooxygenase 3. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 38: 25-31. PMID 19841059 DOI: 10.1124/dmd.109.029769  1
2010 Ming X, Thakker DR. Role of basolateral efflux transporter MRP4 in the intestinal absorption of the antiviral drug adefovir dipivoxil. Biochemical Pharmacology. 79: 455-62. PMID 19735648 DOI: 10.1016/j.bcp.2009.08.029  1
2010 Proctor WR, Ming X, Thakker DR. In vitro techniques to study drug-drug interactions involving transport: Caco-2 model for study of P-glycoprotein and other transporters Enzyme- and Transporter-Based Drug-Drug Interactions: Progress and Future Challenges. 257-282. DOI: 10.1007/978-1-4419-0840-7_10  1
2009 Ming X, Ju W, Wu H, Tidwell RR, Hall JE, Thakker DR. Transport of dicationic drugs pentamidine and furamidine by human organic cation transporters. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 37: 424-30. PMID 18971316 DOI: 10.1124/dmd.108.024083  1
2008 Proctor WR, Bourdet DL, Thakker DR. Mechanisms underlying saturable intestinal absorption of metformin. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 36: 1650-8. PMID 18458049 DOI: 10.1124/dmd.107.020180  1
2008 Yanni SB, Annaert PP, Augustijns P, Bridges A, Gao Y, Benjamin DK, Thakker DR. Role of flavin-containing monooxygenase in oxidative metabolism of voriconazole by human liver microsomes. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 36: 1119-25. PMID 18362161 DOI: 10.1124/dmd.107.019646  1
2008 Tippin TK, Thakker DR. Biorelevant refinement of the Caco-2 cell culture model to assess efficacy of paracellular permeability enhancers. Journal of Pharmaceutical Sciences. 97: 1977-92. PMID 17724658 DOI: 10.1002/jps.21118  1
2006 Knight B, Troutman M, Thakker DR. Deconvoluting the effects of P-glycoprotein on intestinal CYP3A: a major challenge. Current Opinion in Pharmacology. 6: 528-32. PMID 16899406 DOI: 10.1016/j.coph.2006.04.009  1
2006 Bourdet DL, Pollack GM, Thakker DR. Intestinal absorptive transport of the hydrophilic cation ranitidine: a kinetic modeling approach to elucidate the role of uptake and efflux transporters and paracellular vs. transcellular transport in Caco-2 cells. Pharmaceutical Research. 23: 1178-87. PMID 16741656 DOI: 10.1007/s11095-006-0204-y  1
2006 Bourdet DL, Thakker DR. Saturable absorptive transport of the hydrophilic organic cation ranitidine in Caco-2 cells: role of pH-dependent organic cation uptake system and P-glycoprotein. Pharmaceutical Research. 23: 1165-77. PMID 16741655 DOI: 10.1007/s11095-006-0251-4  1
2005 Bourdet DL, Pritchard JB, Thakker DR. Differential substrate and inhibitory activities of ranitidine and famotidine toward human organic cation transporter 1 (hOCT1; SLC22A1), hOCT2 (SLC22A2), and hOCT3 (SLC22A3). The Journal of Pharmacology and Experimental Therapeutics. 315: 1288-97. PMID 16141367 DOI: 10.1124/jpet.105.091223  1
2004 Bourdet DL, Lee K, Thakker DR. Photoaffinity labeling of the anionic sites in Caco-2 cells mediating saturable transport of hydrophilic cations ranitidine and famotidine. Journal of Medicinal Chemistry. 47: 2935-8. PMID 15139772 DOI: 10.1021/jm030433n  1
2004 Zhou L, Thakker DR, Voyksner RD, Anbazhagan M, Boykin DW, Hall JE, Tidwell RR. Metabolites of an orally active antimicrobial prodrug, 2,5-bis(4-amidinophenyl)furan-bis-O-methylamidoxime, identified by liquid chromatography/tandem mass spectrometry. Journal of Mass Spectrometry : Jms. 39: 351-60. PMID 15103648 DOI: 10.1002/jms.591  1
2004 Ansede JH, Thakker DR. High-throughput screening for stability and inhibitory activity of compounds toward cytochrome P450-mediated metabolism. Journal of Pharmaceutical Sciences. 93: 239-55. PMID 14705182 DOI: 10.1002/jps.10545  1
2003 Troutman MD, Thakker DR. Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharmaceutical Research. 20: 1210-24. PMID 12948019 DOI: 10.1023/A:1025001131513  1
2003 Troutman MD, Thakker DR. Efflux ratio cannot assess P-glycoprotein-mediated attenuation of absorptive transport: asymmetric effect of P-glycoprotein on absorptive and secretory transport across Caco-2 cell monolayers. Pharmaceutical Research. 20: 1200-9. PMID 12948018 DOI: 10.1023/A:1025049014674  1
2003 Troutman MD, Thakker DR. Rhodamine 123 requires carrier-mediated influx for its activity as a P-glycoprotein substrate in Caco-2 cells. Pharmaceutical Research. 20: 1192-9. PMID 12948017 DOI: 10.1023/A:1025096930604  1
2003 Ward PD, Ouyang H, Thakker DR. Role of phospholipase C-beta in the modulation of epithelial tight junction permeability. The Journal of Pharmacology and Experimental Therapeutics. 304: 689-98. PMID 12538823 DOI: 10.1124/jpet.102.043638  1
2002 Zhou L, Lee K, Thakker DR, Boykin DW, Tidwell RR, Hall JE. Enhanced permeability of the antimicrobial agent 2,5-bis(4-amidinophenyl)furan across Caco-2 cell monolayers via its methylamidoidme prodrug. Pharmaceutical Research. 19: 1689-95. PMID 12458675 DOI: 10.1023/A:1020957430400  1
2002 Lee K, Ng C, Brouwer KL, Thakker DR. Secretory transport of ranitidine and famotidine across Caco-2 cell monolayers. The Journal of Pharmacology and Experimental Therapeutics. 303: 574-80. PMID 12388638 DOI: 10.1124/jpet.102.038521  1
2002 Ward PD, Klein RR, Troutman MD, Desai S, Thakker DR. Phospholipase C-gamma modulates epithelial tight junction permeability through hyperphosphorylation of tight junction proteins. The Journal of Biological Chemistry. 277: 35760-5. PMID 12101180 DOI: 10.1074/jbc.M203134200  1
2002 Ouyang H, Morris-Natschke SL, Ishaq KS, Ward P, Liu D, Leonard S, Thakker DR. Structure-activity relationship for enhancement of paracellular permeability across Caco-2 cell monolayers by 3-alkylamido-2-alkoxypropylphosphocholines. Journal of Medicinal Chemistry. 45: 2857-66. PMID 12061888 DOI: 10.1021/jm020001x  1
2002 Zhou L, Voyksner RD, Thakker DR, Stephens CE, Anbazhagan M, Boykin DW, Hall JE, Tidwell RR. Characterizing the fragmentation of 2,5-bis (4-amidinophenyl)furan-bis-O-methylamidoxime and selected metabolites using ion trap mass spectrometry. Rapid Communications in Mass Spectrometry : Rcm. 16: 1078-85. PMID 11992511 DOI: 10.1002/rcm.676  1
2002 Chen C, Thakker DR. The fallacy of using adrenochrome reaction for measurement of reactive oxygen species formed during cytochrome p450-mediated metabolism of xenobiotics. The Journal of Pharmacology and Experimental Therapeutics. 300: 417-20. PMID 11805199 DOI: 10.1124/jpet.300.2.417  1
2002 Zhou L, Thakker DR, Voyksner RD, Anbazhagan M, Boykin DW, Hall JE, Tidwell RR. Metabolites of an orally active antimicrobial prodrug, 2,5-bis(4- amidinophenyl)furan-bis-O-methylamidoxime, identified by liquid chromatography-tandem mass spectrometry Proceedings 50th Asms Conference On Mass Spectrometry and Allied Topics. 467-468.  1
2002 Zhou L, Voyksner RD, Thakker DR, Stephens CE, Anbazhagan M, Boykin DW, Tidwell RR, Hall JE. A novel fragmentation pathway involving formation of radical product ions from an antimicrobial prodrug DB289 and selected metabolites using ion trap mass spectrometry Proceedings 50th Asms Conference On Mass Spectrometry and Allied Topics. 479-480.  1
2001 Annaert PP, Turncliff RZ, Booth CL, Thakker DR, Brouwer KL. P-glycoprotein-mediated in vitro biliary excretion in sandwich-cultured rat hepatocytes. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 29: 1277-83. PMID 11560870  1
2000 Ward PD, Tippin TK, Thakker DR. Enhancing paracellular permeability by modulating epithelial tight junctions. Pharmaceutical Science & Technology Today. 3: 346-358. PMID 11050459 DOI: 10.1016/S1461-5347(00)00302-3  1
1999 Liu DZ, Morris-Natschke SL, Kucera LS, Ishaq KS, Thakker DR. Structure-activity relationships for enhancement of paracellular permeability by 2-alkoxy-3-alkylamidopropylphosphocholines across Caco-2 cell monolayers. Journal of Pharmaceutical Sciences. 88: 1169-74. PMID 10564066 DOI: 10.1021/js9900957  1
1999 Liu DZ, LeCluyse EL, Thakker DR. Dodecylphosphocholine-mediated enhancement of paracellular permeability and cytotoxicity in Caco-2 cell monolayers. Journal of Pharmaceutical Sciences. 88: 1161-8. PMID 10564065 DOI: 10.1021/js990094e  1
1999 Lee K, Thakker DR. Saturable transport of H2-antagonists ranitidine and famotidine across Caco-2 cell monolayers. Journal of Pharmaceutical Sciences. 88: 680-7. PMID 10393565 DOI: 10.1021/js980474k  1
1998 Gan LS, Yanni S, Thakker DR. Modulation of the tight junctions of the Caco-2 cell monolayers by H2-antagonists. Pharmaceutical Research. 15: 53-7. PMID 9487546 DOI: 10.1023/A:1011944602662  1
1997 Kang SH, Sinhababu AK, Cory JG, Mitchell BS, Thakker DR, Cho MJ. Cellular delivery of nucleoside diphosphates: a prodrug approach. Pharmaceutical Research. 14: 706-12. PMID 9210185 DOI: 10.1023/A:1012133902314  1
1997 Gan LSL, Thakker DR. Applications of the Caco-2 model in the design and development of orally active drugs: Elucidation of biochemical and physical barriers posed by the intestinal epithelium Advanced Drug Delivery Reviews. 23: 77-98. DOI: 10.1016/S0169-409X(96)00427-9  1
1996 Gan LS, Moseley MA, Khosla B, Augustijns PF, Bradshaw TP, Hendren RW, Thakker DR. CYP3A-like cytochrome P450-mediated metabolism and polarized efflux of cyclosporin A in Caco-2 cells. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 24: 344-9. PMID 8820426  1
1996 Sinhababu AK, Thakker DR. Prodrugs of anticancer agents Advanced Drug Delivery Reviews. 19: 241-273. DOI: 10.1016/0169-409X(95)00109-K  1
1995 Sinhababu AK, Boehlert CC, Gan LS, Yanni SB, Thakker DR. High-performance liquid chromatographic purification, optimization of the assay, and properties of ribonucleoside diphosphate reductase from rabbit bone marrow. Archives of Biochemistry and Biophysics. 317: 285-91. PMID 7872796 DOI: 10.1006/abbi.1995.1164  1
1994 Iyer RP, Boal JH, Phillips LR, Thakker DR, Egan W. Synthesis, hydrolytic behavior, and anti-HIV activity of selected acyloxyalkyl esters of trisodium phosphonoformate (foscarnet sodium). Journal of Pharmaceutical Sciences. 83: 1269-73. PMID 7530302  1
1993 Augustijns PF, Bradshaw TP, Gan LS, Hendren RW, Thakker DR. Evidence for a polarized efflux system in CACO-2 cells capable of modulating cyclosporin A transport. Biochemical and Biophysical Research Communications. 197: 360-5. PMID 7903526 DOI: 10.1006/bbrc.1993.2487  1
1991 Thakker DR, Boehlert C, Levin W, Ryan DE, Thomas PE, Yagi H, Jerina DM. Novel stereoselectivity of rat liver cytochrome(s) P450 toward enantiomers of the trans-1,2-dihydrodiol of triphenylene. Archives of Biochemistry and Biophysics. 288: 54-63. PMID 1898024 DOI: 10.1016/0003-9861(91)90164-E  1
1991 Prasad GK, Thakker DR. Oxidative conversion of 6-fluorobenzo(c)phenanthrene to its K-region oxide by liver microsomes from 3-methylcholanthrene treated rats: reversal of stereoselectivity of cytochrome P-450c due to the influence of fluoro group. Biochemical and Biophysical Research Communications. 181: 1516-23. PMID 1764102 DOI: 10.1016/0006-291X(91)92111-V  1
1991 Patrick MA, Sethi SK, Unger SE, Mirsadeghi S, Ribeiro AA, Thakker DR. A novel reaction between acetone and the benzo[c]phenanthrene K-region o-quinone containing a Peri-fluoro substituent Journal of Organic Chemistry. 56: 888-891.  1
1989 Iyer RP, Phillips LR, Biddle JA, Thakker DR, Egan W, Aoki S, Mitsuya H. Synthesis of acyloxyalkyl acylphosphonates as potential prodrugs of the antiviral, trisodium phosphonoformate (foscarnet sodium) Tetrahedron Letters. 30: 7141-7144. DOI: 10.1016/S0040-4039(01)93918-8  1
1989 Mirsadeghi S, Prasad GKB, Whittaker N, Thakker DR. Synthesis of the K-region monofluoro- and difluorobenzo[c]phenanthrenes Journal of Organic Chemistry. 54: 3091-3096.  1
1988 Prasad GK, Mirsadeghi S, Boehlert C, Byrd RA, Thakker DR. Oxidative metabolism of the carcinogen 6-fluorobenzo[c]phenanthrene. Effect of a K-region fluoro substituent on the regioselectivity of cytochromes P-450 in liver microsomes from control and induced rats. The Journal of Biological Chemistry. 263: 3676-83. PMID 3346217  1
1988 Thakker DR, Boehlert C, Mirsadeghi S, Levin W, Ryan DE, Thomas PE, Yagi H, Pannell LK, Sayer JM, Jerina DM. Differential stereoselectivity on metabolism of triphenylene by cytochromes P-450 in liver microsomes from 3-methylcholanthrene- and phenobarbital-treated rats. The Journal of Biological Chemistry. 263: 98-105. PMID 3335511  1
1987 Chang RL, Wood AW, Conney AH, Yagi H, Sayer JM, Thakker DR, Jerina DM, Levin W. Role of diaxial versus diequatorial hydroxyl groups in the tumorigenic activity of a benzo[a]pyrene bay-region diol epoxide. Proceedings of the National Academy of Sciences of the United States of America. 84: 8633-6. PMID 3479808  1
1987 van Bladeren PJ, Balani SK, Sayer JM, Thakker DR, Boyd DR, Ryan DE, Thomas PE, Levin W, Jerina DM. Stereoselective formation of benzo(c)phenanthrene (+)-(3S,4R) and (+)-(5S,6R)-oxides by cytochrome P450c in a highly purified and reconstituted system. Biochemical and Biophysical Research Communications. 145: 160-7. PMID 3109408 DOI: 10.1016/0006-291X(87)91301-5  1
1987 Yagi H, Sayer JM, Thakker DR, Levin W, Jerina DM. Effects of a 6-fluoro substituent on the solvolytic properties of the diastereomeric 7,8-diol 9,10-epoxides of the carcinogen benzo[a]pyrene Journal of the American Chemical Society. 109: 838-846.  1
1986 Thakker DR, Levin W, Yagi H, Yeh HJ, Ryan DE, Thomas PE, Conney AH, Jerina DM. Stereoselective metabolism of the (+)-(S,S)- and (-)-(R,R)-enantiomers of trans-3,4-dihydroxy-3,4-dihydrobenzo[c]-phenanthrene by rat and mouse liver microsomes and by a purified and reconstituted cytochrome P-450 system. The Journal of Biological Chemistry. 261: 5404-13. PMID 3957930  1
1986 Thakker DR, Boehlert C, Kirk KL, Antkowiak R, Creveling CR. Regioselectivity of catechol O-methyltransferase. The effect of pH on the site of O-methylation of fluorinated norepinephrines. The Journal of Biological Chemistry. 261: 178-84. PMID 3753600  1
1985 Thakker DR, Shirai N, Levin W. Metabolism of dibenz[c,h]acridine by rat liver microsomes and by cytochrome P450c with and without epoxide hydrolase Proceedings of the American Association For Cancer Research. No. 449.  1
1985 Thakker DR, Boehlert C, Levin W. Metabolism of triphenylene by liver microsomes from control, phenobarbital(PB)-treated and 3-methylcholanthrene(MC)-treated rats Proceedings of the American Association For Cancer Research. No. 448.  1
1984 Levin W, Chang RL, Wood AW, Yagi H, Thakker DR, Jerina DM, Conney AH. High stereoselectivity among the optical isomers of the diastereomeric bay-region diol-epoxides of benz(a)anthracene in the expression of tumorigenic activity in murine tumor models. Cancer Research. 44: 929-33. PMID 6692415  1
1984 Thakker DR, Yagi H, Sayer JM, Kapur U, Levin W, Chang RL, Wood AW, Conney AH, Jerina DM. Effects of a 6-fluoro substituent on the metabolism of benzo(a)pyrene 7,8-dihydrodiol to bay-region diol epoxides by rat liver enzymes. The Journal of Biological Chemistry. 259: 11249-56. PMID 6432795  1
1983 Ittah Y, Thakker DR, Levin W, Croisy-Delcey M, Ryan DE, Thomas PE, Conney AH, Jerina DM. Metabolism of benzo[c]phenanthrene by rat liver microsomes and by a purified monooxygenase system reconstituted with different isozymes of cytochrome P-450. Chemico-Biological Interactions. 45: 15-28. PMID 6872097 DOI: 10.1016/0009-2797(83)90039-X  1
1983 Vyas KP, van Bladeren PJ, Thakker DR, Yagi H, Sayer JM, Levin W, Jerina DM. Regioselectivity and stereoselectivity in the metabolism of trans-1,2-dihydroxy-1,2-dihydrobenz[a]anthracene by rat liver microsomes. Molecular Pharmacology. 24: 115-23. PMID 6865920  1
1983 Levin W, Wood AW, Chang RL, Newman MS, Thakker DR, Conney AH, Jerina DM. The effect of steric strain in the bay-region of polycyclic aromatic hydrocarbons: tumorigenicity of alkyl-substituted benz[a]anthracenes. Cancer Letters. 20: 139-46. PMID 6421476 DOI: 10.1016/0304-3835(83)90042-3  1
1983 Buhler DR, Unlü F, Thakker DR, Slaga TJ, Conney AH, Wood AW, Chang RL, Levin W, Jerina DM. Effect of a 6-fluoro substituent on the metabolism and biological activity of benzo(a)pyrene. Cancer Research. 43: 1541-9. PMID 6299523  1
1983 Yagi H, Thakker DR, Ittah Y, Croisy-Delcey M, Jerina DM. Synthesis and assignment of absolute configuration to the trans 3,4-dihydrodiols and 3,4-diol-1,2-epoxides of benzo[c]phenanthrene Tetrahedron Letters. 24: 1349-1352. DOI: 10.1016/S0040-4039(00)81653-6  1
1982 Vyas KP, Levin W, Yagi H, Thakker DR, Ryan DE, Thomas PE, Conney AH, Jerina DM. Stereoselective metabolism of the (+)- and (-)-enantiomers of trans-1,2-dihydroxy-1,2-dihydrochrysene to bay-region 1,2-diol-3,4-epoxide diastereomers by rat liver enzymes. Molecular Pharmacology. 22: 182-9. PMID 7121449  1
1982 Thakker DR, Levin W, Yagi H, Tada M, Ryan DE, Thomas PE, Conney AH, Jerina DM. Stereoselective metabolism of the (+)- and (-)-enantiomers of trans-3,4-dihydroxy-3,4-dihydrobenz[a]anthracene by rat liver microsomes and by a purified and reconstituted cytochrome P-450 system. The Journal of Biological Chemistry. 257: 5103-10. PMID 7068678  1
1982 Vyas KP, Thakker DR, Levin W, Yagi H, Conney AH, Jerina DM. Stereoselective metabolism of the optical isomers of trans-1,2-dihydroxy-1,2-dihydrophenanthrene to bay-region diol epoxides by rat liver microsomes. Chemico-Biological Interactions. 38: 203-13. PMID 7055851 DOI: 10.1016/0009-2797(82)90040-0  1
1982 van Bladeren PJ, Armstrong RN, Cobb D, Thakker DR, Ryan DE, Thomas PE, Sharma ND, Boyd DR, Levin W, Jerina DM. Stereoselective formation of benz[a]anthracene (+)-(5S,6R)-oxide and (+)-(8R,9S)-oxide by a highly purified and reconstituted system containing cytochrome P-450c. Biochemical and Biophysical Research Communications. 106: 602-9. PMID 6809007 DOI: 10.1016/0006-291X(82)91153-6  1
1982 Yagi H, Vyas KP, Tada M, Thakker DR, Jerina DM. Synthesis of the enantiomeric bay-region diol epoxides of benz[a]anthracene and chrysene Journal of Organic Chemistry. 47: 1110-1117.  1
1981 Thakker DR, Levin W, Yagi H, Conney AH, Jerina DM. Regio- and stereoselectivity of hepatic cytochrome P-450 toward polycyclic aromatic hydrocarbon substrates. Advances in Experimental Medicine and Biology. 136: 525-39. PMID 7344478  1
1981 Nordqvist M, Thakker DR, Vyas KP, Yagi H, Levin W, Ryan DE, Thomas PE, Conney AH, Jerina DM. Metabolism of chrysene and phenanthrene to bay-region diol epoxides by rat liver enzymes. Molecular Pharmacology. 19: 168-78. PMID 7207460  1
1981 Thakker DR, Levin W, Buening M, Yagi H, Lehr RE, Wood AW, Conney AH, Jerina DM. Species-specific enhancement by 7,8-benzoflavone of hepatic microsomal metabolism of benzo[e]pyrene 9,10-dihydrodiol to bay-region diol epoxides. Cancer Research. 41: 1389-96. PMID 7194138  1
1981 Jerina DM, Sayer JM, Yagi H, Croisy-Delcey M, Ittah Y, Thakker DR, Wood AW, Chang RL, Levin W, Conney AH. Highly tumorigenic bay-region diol epoxides from the weak carcinogen benzo[c]phenanthrene. Advances in Experimental Medicine and Biology. 136: 501-23. PMID 7046379  1
1981 Kedzierski B, Thakker DR, Armstrong RN, Jerina DM. absolute configuration of the k-region 4,5-dihydrodiols and 4,5-oxide of benzo[a]pyrene Tetrahedron Letters. 22: 405-408. DOI: 10.1016/0040-4039(81)80111-6  1
1981 Thakker DR, Levin W, Yagi H. Stereoselective metabolism of (+)- and (-)-benzo(a)anthracene 3,4-dihydrodiols by rat liver microsomes and a reconstituted cytochrome P-450 system Proceedings of the American Association For Cancer Research. 387.  1
1980 Levin W, Buening MK, Wood AW, Chang RL, Kedzierski B, Thakker DR, Boyd DR, Gadaginamath GS, Armstrong RN, Yagi H, Karle JM, Slaga TJ, Jerina DM, Conney AH. An enantiomeric interaction in the metabolism and tumorigenicity of (+)- and (-)-benzo[a]pyrene 7,8-oxide. The Journal of Biological Chemistry. 255: 9067-74. PMID 7410412  1
1980 Wood AW, Chang RL, Huang MT, Levin W, Lehr RE, Kumar S, Thakker DR, Yagi H, Jerina DM, Conney AH. Mutagenicity of benzo(e)pyrene and triphenylene tetrahydroepoxides and diol-epoxides in bacterial and mammalian cells. Cancer Research. 40: 1985-9. PMID 6989494  1
1979 Nordqvist M, Thakker DR, Levin W, Yagi H, Ryan DE, Thomas PE, Conney AH, Jerina DM. The highly tumorigenic 3,4-dihydrodiol is a principal metabolite formed from dibenzo[a,h]anthracene by liver enzymes. Molecular Pharmacology. 16: 643-55. PMID 514264  1
1979 Thakker DR, Levin W, Yagi H, Turujman S, Kapadia D, Conney AH, Jerina DM. Absolute stereochemistry of the trans-dihydrodiols formed from benzo[a]anthracene by liver microsomes. Chemico-Biological Interactions. 27: 145-61. PMID 498352 DOI: 10.1016/0009-2797(79)90122-4  1
1979 Levin W, Buening MK, Wood AW, Chang RL, Thakker DR, Jerina DM, Conney AH. Tumorigenic activity of 3-methylcholanthrene metabolites on mouse skin and in newborn mice. Cancer Research. 39: 3549-53. PMID 476681  1
1979 Thakker DR, Levin W, Yagi H, Ryan D, Thomas PE, Karle JM, Lehr RE, Jerina DM, Conney AH. Metabolism of benzo[a]anthracene to its tumorigenic 3,4-dihydrodiol. Molecular Pharmacology. 15: 138-53. PMID 423885  1
1979 Chang RL, Wood AW, Levin W, Mah HD, Thakker DR, Jerina DM, Conney AH. Differences in mutagenicity and cytotoxicity of (+)- and (-)-benzo[a]pyrene 4,5-oxide: a synergistic interaction of enantiomers. Proceedings of the National Academy of Sciences of the United States of America. 76: 4280-4. PMID 388437  1
1979 Wood AW, Levin W, Thakker DR, Yagi H, Chang RL, Ryan DE, Thomas PE, Dansette PM, Whittaker N, Turujman S, Lehr RE, Kumar S, Jerina DM, Conney AH. Biological activity of benzo[e]pyrene. An assessment based on mutagenic activities and metabolic profiles of the polycyclic hydrocarbon and its derivatives. The Journal of Biological Chemistry. 254: 4408-15. PMID 374411  1
1979 Thakker DR, Levin W, Turujman S. Absolute stereochemistry of the trans dihydrodiols formed from benzo[a]anthracene (BA) by rat liver microsomes Proceedings of the American Association For Cancer Research 1
1979 Yagi H, Thakker DR, Lehr RE, Jerina DM. Benzo-ring diol epoxides of benzo[e]pyrene and triphenylene Journal of Organic Chemistry. 44: 3439-3442.  1
1979 Whalen DL, Ross AM, Montemarano JA, Thakker DR, Yagi H, Jerina DM. General acid catalysis in the hydrolysis of benzo[a]pyrene 7,8-diol 9,10-epoxides [19] Journal of the American Chemical Society. 101: 5086-5088.  1
1978 Kapitulnik J, Wislocki PG, Levin W, Yagi H, Thakker DR, Akagi H, Koreeda M, Jerina DM, Conney AH. Marked differences in the carcinogenic activity of optically pure (+)- and (-)-trans-7,8-dihydroxy-7,8-dihydrobenzo(a)pyrene in newborn mice. Cancer Research. 38: 2661-5. PMID 679168  1
1978 Thakker DR, Yagi H, Jerina DM. Analysis of polycyclic aromatic hydrocarbons and their metabolites by high-pressure liquid chromatography. Methods in Enzymology. 52: 279-96. PMID 672632 DOI: 10.1016/S0076-6879(78)52030-2  1
1978 Thakker DR, Yagi H, Lehr RE, Levin W, Buening M, Lu AY, Chang RL, Wood AW, Conney AH, Jerina DM. Metabolism of trans-9,10-dihydroxy-9,10-dihydrobenzo[a]pyrene occurs primarily by arylhydroxylation rather than formation of a diol epoxide. Molecular Pharmacology. 14: 502-13. PMID 661815  1
1978 Levin W, Thakker DR, Wood AW, Chang RL, Lehr RE, Jerina DM, Conney AH. Evidence that benzo(a)anthracene 3,4-diol-1,2-epoxide is an ultimate carcinogen on mouse skin. Cancer Research. 38: 1705-10. PMID 647681  1
1978 Thakker DR, Levin W, Wood AW, Conney AH, Stoming TA, Jerina DM. Metabolic formation of 1,9,10-trihydroxy-9,10-dihydro-3-methylcholanthrene: a potential proximate carcinogen from 3-methylcholanthrene. Journal of the American Chemical Society. 100: 645-7. PMID 624805 DOI: 10.1021/ja00470a057  1
1978 Wood AW, Chang RL, Levin W, Thomas PE, Ryan D, Stoming TA, Thakker DR, Jerina DM, Conney AH. Metabolic activation of 3-methylcholanthrene and its metabolites to products mutagenic to bacterial and mammalian cells. Cancer Research. 38: 3398-404. PMID 356964  1
1978 Buening MK, Wislocki PG, Levin W, Yagi H, Thakker DR, Akagi H, Koreeda M, Jerina DM, Conney AH. Tumorigenicity of the optical enantiomers of the diastereomeric benzo[a]pyrene 7,8-diol-9,10-epoxides in newborn mice: exceptional activity of (+)-7beta,8alpha-dihydroxy-9alpha,10alpha-epoxy-7,8,9,10-tetrahydrobenzo[a]pyrene. Proceedings of the National Academy of Sciences of the United States of America. 75: 5358-61. PMID 281685  1
1978 Jerina DM, Levin W, Thakker DR, Wood AW, Yagi H, Conney AH. Carcinogenicity of benzo[a]pyrene derivatives: The bay region theory Pure and Applied Chemistry. 50: 1033-1044. DOI: 10.1351/pac197850091033  1
1978 Thakker DR, Yagi H, Lehr RE. Metabolism and biological activity of benzo[a]pyrene 9,10-dihydrodiol Federation Proceedings. 37: No.2811.  1
1978 Thakker DR, Levin W, Wood AW. 9,10-Dihydrodiols of 1-hydroxy-3-methylcholanthrene: potential proximate carcinogens derived from 3-methylcholanthrene Proceedings of the American Association For Cancer Research 1
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  1
1977 Bresnick E, Stoming TA, Vaught JB, Thakker DR, Jerina DM. Nuclear metabolism of benzo(a)pyrene and of (+/-)-trans-7-8-dihydroxy-7-8,-dihydrobenzo(a)pyrene. Comparative chromatographic analysis of alkylated DNA. Archives of Biochemistry and Biophysics. 183: 31-7. PMID 907356 DOI: 10.1016/0003-9861(77)90415-5  1
1977 Thakker DR, Yagi H, Levin W, Lu AY, Conney AH, Jerina DM. Stereospecificity of microsomal and purified epoxide hydrase from rat liver. Hydration of arene oxides of polycyclic hydrocarbons. The Journal of Biological Chemistry. 252: 6328-34. PMID 893410  1
1977 Yagi H, Akagi H, Thakker DR, Mah HD, Koreeda M, Jerina DM. Absolute sterochemistry of the highly mutagenic 7,8-diol 9,10-epoxides derived from the potent carcinogen trans-7,8-dihydroxy-7,8-dihydrobenzol[a]pyrene. Journal of the American Chemical Society. 99: 2358-9. PMID 864141  1
1977 Thakker DR, Yagi H, Akagi H, Koreeda M, Lu AH, Levin W, Wood AW, Conney AH, Jerina DM. Metabolism of benzo[a]pyrene. VI. Stereoselective metabolism of benzo[a]pyrene and benzo[a]pyrene 7,8-dihydrodiol to diol epoxides. Chemico-Biological Interactions. 16: 281-300. PMID 862130 DOI: 10.1016/0009-2797(77)90108-9  1
1977 Yagi H, Thakker DR, Hernandez O, Koreeda M, Jerina DM. Synthesis and reactions of the highly mutagenic 7,8-diol 9,10-epoxides of the carcinogen benzo[a]pyrene. Journal of the American Chemical Society. 99: 1604-11. PMID 839009  1
1977 Wood AW, Levin W, Ryan D, Thomas PE, Yagi H, Mah HD, Thakker DR, Jerina DM, Conney AH. High mutageniticity of metabolically activated chrysene 1,2 dihydrodiol: evidence for bay region activation of chrysene. Biochemical and Biophysical Research Communications. 78: 847-54. PMID 334179 DOI: 10.1016/0006-291X(77)90500-9  1
1977 Wood AW, Chang RL, Levin W, Yagi H, Thakker DR, Jerina DM, Conney AH. Differences in mutagenicity of the optical enantiomers of the diastereomeric benzo[a]pyrene 7,8-diol-9,10-epoxides. Biochemical and Biophysical Research Communications. 77: 1389-96. PMID 332178 DOI: 10.1016/S0006-291X(77)80133-2  1
1977 Whalen DL, Montemarano JA, Thakker DR, Yagi H, Jerina DM. Changes of mechanisms and product distributions in the hydrolysis of benzo[a]pyrene-7,8-diol 9,10-epoxide metabolites induced by changes in pH. Journal of the American Chemical Society. 99: 5522-4. PMID 18500  1
1977 Bresnick E, Vaught JB, Thakker DR. Nuclear metabolism of benzo(a)pyrene (BP) and of (±)trans 7,8 dihydroxy 7,8 dihydro BP: chromatographic analysis of aralkylated DNA Proceedings of the American Association For Cancer Research 1
1976 Thakker DR, Yagi H, Lu AY, Levin W, Conney AH. Metabolism of benzo[a]pyrene: conversion of (+/-)-trans-7,8-dihydroxy-7,8-dihydrobenzo[a]pyrene to highly mutagenic 7,8-diol-9,10-epoxides. Proceedings of the National Academy of Sciences of the United States of America. 73: 3381-5. PMID 1068451  1
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  1
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  1
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  1
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  1
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  1
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  1
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