Howard Bregman - Publications

Affiliations: 
2003-2007 University of Pennsylvania, Philadelphia, PA, United States 

19/42 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
2017 Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio AA, Bregman H, Chu-Moyer MY, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa RF, Gunaydin H, Guzman-Perez A, Huang H, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities. Journal of Medicinal Chemistry. PMID 28287723 DOI: 10.1021/Acs.Jmedchem.6B01851  0.307
2013 Huang H, Guzman-Perez A, Acquaviva L, Berry V, Bregman H, Dovey J, Gunaydin H, Huang X, Huang L, Saffran D, Serafino R, Schneider S, Wilson C, DiMauro EF. Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors. Acs Medicinal Chemistry Letters. 4: 1218-23. PMID 24900633 DOI: 10.1021/Ml4003315  0.342
2013 Hua Z, Bregman H, Buchanan JL, Chakka N, Guzman-Perez A, Gunaydin H, Huang X, Gu Y, Berry V, Liu J, Teffera Y, Huang L, Egge B, Emkey R, Mullady EL, et al. Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors. Journal of Medicinal Chemistry. 56: 10003-15. PMID 24294969 DOI: 10.1021/Jm401317Z  0.37
2013 Bregman H, Chakka N, Guzman-Perez A, Gunaydin H, Gu Y, Huang X, Berry V, Liu J, Teffera Y, Huang L, Egge B, Mullady EL, Schneider S, Andrews PS, Mishra A, et al. Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. Journal of Medicinal Chemistry. 56: 4320-42. PMID 23701517 DOI: 10.1021/Jm4000038  0.397
2013 Bregman H, Gunaydin H, Gu Y, Schneider S, Wilson C, DiMauro EF, Huang X. Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket. Journal of Medicinal Chemistry. 56: 1341-5. PMID 23316926 DOI: 10.1021/Jm301607V  0.397
2012 Huang H, Acquaviva L, Berry V, Bregman H, Chakka N, O'Connor A, DiMauro EF, Dovey J, Epstein O, Grubinska B, Goldstein J, Gunaydin H, Hua Z, Huang X, Huang L, et al. Structure-Based Design of Potent and Selective CK1γ Inhibitors. Acs Medicinal Chemistry Letters. 3: 1059-64. PMID 24900428 DOI: 10.1021/Ml300278F  0.364
2012 Hua Z, Huang X, Bregman H, Chakka N, DiMauro EF, Doherty EM, Goldstein J, Gunaydin H, Huang H, Mercede S, Newcomb J, Patel VF, Turci SM, Yan J, Wilson C, et al. 2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1γ) inhibitors. Bioorganic & Medicinal Chemistry Letters. 22: 5392-5. PMID 22877629 DOI: 10.1016/J.Bmcl.2012.07.046  0.462
2009 Pagano N, Wong EY, Breiding T, Liu H, Wilbuer A, Bregman H, Shen Q, Diamond SL, Meggers E. From imide to lactam metallo-pyridocarbazoles: distinct scaffolds for the design of selective protein kinase inhibitors. The Journal of Organic Chemistry. 74: 8997-9009. PMID 19886617 DOI: 10.1021/Jo901641K  0.796
2009 Bullock AN, Russo S, Amos A, Pagano N, Bregman H, Debreczeni JE, Lee WH, von Delft F, Meggers E, Knapp S. Crystal structure of the PIM2 kinase in complex with an organoruthenium inhibitor. Plos One. 4: e7112. PMID 19841674 DOI: 10.1371/Journal.Pone.0007112  0.752
2009 Xie P, Streu C, Qin J, Bregman H, Pagano N, Meggers E, Marmorstein R. The crystal structure of BRAF in complex with an organoruthenium inhibitor reveals a mechanism for inhibition of an active form of BRAF kinase. Biochemistry. 48: 5187-98. PMID 19371126 DOI: 10.1021/Bi802067U  0.789
2007 Pagano N, Maksimoska J, Bregman H, Williams DS, Webster RD, Xue F, Meggers E. Ruthenium half-sandwich complexes as protein kinase inhibitors: derivatization of the pyridocarbazole pharmacophore ligand. Organic & Biomolecular Chemistry. 5: 1218-27. PMID 17406720 DOI: 10.1039/B700433H  0.746
2007 Smalley KS, Contractor R, Haass NK, Kulp AN, Atilla-Gokcumen GE, Williams DS, Bregman H, Flaherty KT, Soengas MS, Meggers E, Herlyn M. An organometallic protein kinase inhibitor pharmacologically activates p53 and induces apoptosis in human melanoma cells. Cancer Research. 67: 209-17. PMID 17210701 DOI: 10.1158/0008-5472.Can-06-1538  0.709
2006 Bregman H, Meggers E. Ruthenium half-sandwich complexes as protein kinase inhibitors: an N-succinimidyl ester for rapid derivatizations of the cyclopentadienyl moiety. Organic Letters. 8: 5465-8. PMID 17107048 DOI: 10.1021/Ol0620646  0.745
2006 Atilla-Gokcumen GE, Williams DS, Bregman H, Pagano N, Meggers E. Organometallic compounds with biological activity: a very selective and highly potent cellular inhibitor for glycogen synthase kinase 3. Chembiochem : a European Journal of Chemical Biology. 7: 1443-50. PMID 16858717 DOI: 10.1002/Cbic.200600117  0.751
2006 Bregman H, Carroll PJ, Meggers E. Rapid access to unexplored chemical space by ligand scanning around a ruthenium center: discovery of potent and selective protein kinase inhibitors. Journal of the American Chemical Society. 128: 877-84. PMID 16417378 DOI: 10.1021/Ja055523R  0.741
2006 Debreczeni JE, Bullock AN, Atilla GE, Williams DS, Bregman H, Knapp S, Meggers E. Ruthenium half-sandwich complexes bound to protein kinase Pim-1. Angewandte Chemie (International Ed. in English). 45: 1580-5. PMID 16381041 DOI: 10.1002/Anie.200503468  0.806
2006 Debreczeni JÉ, Bullock AN, Atilla GE, Williams DS, Bregman H, Knapp S, Meggers E. Ruthenium Half-Sandwich Complexes Bound to Protein Kinase Pim-1 Angewandte Chemie. 118: 1610-1615. DOI: 10.1002/ange.200503468  0.806
2005 Williams DS, Atilla GE, Bregman H, Arzoumanian A, Klein PS, Meggers E. Switching on a signaling pathway with an organoruthenium complex. Angewandte Chemie (International Ed. in English). 44: 1984-7. PMID 15742314 DOI: 10.1002/Anie.200462501  0.781
2004 Bregman H, Williams DS, Atilla GE, Carroll PJ, Meggers E. An organometallic inhibitor for glycogen synthase kinase 3. Journal of the American Chemical Society. 126: 13594-5. PMID 15493898 DOI: 10.1021/Ja046049C  0.81
Low-probability matches (unlikely to be authored by this person)
2016 DiMauro EF, Altmann S, Berry LM, Bregman H, Chakka N, Chu-Moyer M, Feric Bojic E, Foti RS, Fremeau RT, Gao H, Gunaydin H, Guzman-Perez A, Hall BE, Huang H, Jarosh M, et al. Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors. Journal of Medicinal Chemistry. PMID 27441383 DOI: 10.1021/Acs.Jmedchem.6B00425  0.299
2016 Liu L, Lee MR, Kim JL, Whittington DA, Bregman H, Hua Z, Lewis RT, Martin MW, Nishimura N, Potashman M, Yang K, Yi S, Vaida KR, Epstein LF, Babij C, et al. Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. Bioorganic & Medicinal Chemistry. PMID 27085672 DOI: 10.1016/j.bmc.2016.03.055  0.293
2016 Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. Acs Medicinal Chemistry Letters. 7: 1062-1067. PMID 27994738 DOI: 10.1021/Acsmedchemlett.6B00243  0.229
2012 Bregman H, Nguyen HN, Feric E, Ligutti J, Liu D, McDermott JS, Wilenkin B, Zou A, Huang L, Li X, McDonough SI, Dimauro EF. The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR. Bioorganic & Medicinal Chemistry Letters. 22: 2033-42. PMID 22306122 DOI: 10.1016/J.Bmcl.2012.01.023  0.229
2017 Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, et al. Correction to "Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement". Acs Medicinal Chemistry Letters. 8: 378. PMID 28337335 DOI: 10.1021/Acsmedchemlett.7B00075  0.225
2016 Liu L, Lee MR, Kim JL, Whittington DA, Bregman H, Hua Z, Lewis RT, Martin MW, Nishimura N, Potashman M, Yang K, Yi S, Vaida KR, Epstein LF, Babij C, et al. Corrigendum to "Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling" [Bioorg. Med. Chem. 24 (2016) 2215-2234]. Bioorganic & Medicinal Chemistry. PMID 27234892 DOI: 10.1016/j.bmc.2016.05.014  0.22
2017 La DS, Peterson EA, Bode C, Boezio AA, Bregman H, Chu-Moyer MY, Coats J, DiMauro EF, Dineen TA, Du B, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Fremeau R, et al. The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement. Bioorganic & Medicinal Chemistry Letters. PMID 28629594 DOI: 10.1016/J.Bmcl.2017.05.070  0.171
2011 Bregman H, Berry L, Buchanan JL, Chen A, Du B, Feric E, Hierl M, Huang L, Immke D, Janosky B, Johnson D, Li X, Ligutti J, Liu D, Malmberg A, et al. Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. Journal of Medicinal Chemistry. 54: 4427-45. PMID 21634377 DOI: 10.1021/Jm200018K  0.17
2018 Bambouskova M, Gorvel L, Lampropoulou V, Sergushichev A, Loginicheva E, Johnson K, Korenfeld D, Mathyer ME, Kim H, Huang LH, Duncan D, Bregman H, Keskin A, Santeford A, Apte RS, et al. Electrophilic properties of itaconate and derivatives regulate the IκBζ-ATF3 inflammatory axis. Nature. PMID 29670287 DOI: 10.1038/S41586-018-0052-Z  0.166
2016 Huang X, Shaffer PL, Ayube S, Bregman H, Chen H, Lehto SG, Luther JA, Matson DJ, McDonough SI, Michelsen K, Plant MH, Schneider S, Simard JR, Teffera Y, Yi S, et al. Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators. Nature Structural & Molecular Biology. PMID 27991902 DOI: 10.1038/Nsmb.3329  0.154
2015 Matson DJ, Hamamoto DT, Bregman H, Cooke M, DiMauro EF, Huang L, Johnson D, Li X, McDermott J, Morgan C, Wilenkin B, Malmberg AB, McDonough SI, Simone DA. Inhibition of Inactive States of Tetrodotoxin-Sensitive Sodium Channels Reduces Spontaneous Firing of C-Fiber Nociceptors and Produces Analgesia in Formalin and Complete Freund's Adjuvant Models of Pain. Plos One. 10: e0138140. PMID 26379236 DOI: 10.1371/Journal.Pone.0138140  0.146
2016 Bregman H, Simard JR, Andrews KL, Ayube S, Chen H, Gunaydin H, Guzman-Perez A, Hu J, Huang L, Huang X, Krolikowski PH, Lehto SG, Lewis RT, Michelsen K, Pegman P, et al. The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors. Journal of Medicinal Chemistry. PMID 28001399 DOI: 10.1021/Acs.Jmedchem.6B01496  0.133
2017 Chakka N, Andrews KL, Berry LM, Bregman H, Gunaydin H, Huang L, Guzman-Perez A, Plant MH, Simard JR, Gingras J, DiMauro EF. Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators. European Journal of Medicinal Chemistry. 137: 63-75. PMID 28575722 DOI: 10.1016/J.Ejmech.2017.05.036  0.128
2004 Handy ST, Zhang Y, Bregman H. A modular synthesis of the lamellarins: total synthesis of lamellarin G trimethyl ether. The Journal of Organic Chemistry. 69: 2362-6. PMID 15049631 DOI: 10.1021/jo0352833  0.087
1985 Prochaska HJ, Bregman HS, De Long MJ, Talalay P. Specificity of induction of cancer protective enzymes by analogues of tert-butyl-4-hydroxyanisole (BHA) Biochemical Pharmacology. 34: 3909-3914. PMID 4062966 DOI: 10.1016/0006-2952(85)90443-5  0.045
2022 Plumb ID, Feldstein LR, Barkley E, Posner AB, Bregman HS, Hagen MB, Gerhart JL. Effectiveness of COVID-19 mRNA Vaccination in Preventing COVID-19-Associated Hospitalization Among Adults with Previous SARS-CoV-2 Infection - United States, June 2021-February 2022. Mmwr. Morbidity and Mortality Weekly Report. 71: 549-555. PMID 35421077 DOI: 10.15585/mmwr.mm7115e2  0.02
1980 Winchester JF, Rahman A, Tilstone WJ, Bregman H, Mortensen LM, Gelfand MC, Scheest PS, Schreiner GE. Will hemoperfusion be useful for cancer chemotherapeutic drug removal? Clinical Toxicology. 17: 557-569. PMID 7460507 DOI: 10.3109/15563658008990006  0.018
1981 Bregman H, Gelfand M. Iron Overload in Patients on Maintenance Hemodialysis The International Journal of Artificial Organs. 4: 56-57. DOI: 10.1177/039139888100400203  0.016
1992 Kniaz D, Eisenberg GM, Elrad H, Johnson CA, Valaitis J, Bregman H. Postpartum hemolytic uremic syndrome associated with antiphospholipid antibodies. A case report and review of the literature. American Journal of Nephrology. 12: 126-33. PMID 1492877 DOI: 10.1159/000168432  0.01
1988 Bregman HL, McCabe WL, Sutcliffe WG. Capturing Air Traffic Controller Expertise for Incorporation in Automated Air Traffic Control Systems Proceedings of the Human Factors Society Annual Meeting. 32: 1031-1035. DOI: 10.1177/154193128803201608  0.01
1986 Daugirdas J, Bregman H, Rahman MA, Ramanujam L, Nawab Z, Leehey D, Ing T. Ultrafiltration Control during Continuous Arteriovenous Hemodialysis Using Paired Volumetric Dialysate Pumps The International Journal of Artificial Organs. 9: 273-274. DOI: 10.1177/039139888600900414  0.01
1985 Ing T, Daugirdas J, Bregman H, Leehey D. Continuous Arteriovenous Hemodialysis The International Journal of Artificial Organs. 8: 117-118. DOI: 10.1177/039139888500800301  0.01
1983 Bregman H, Brown J, Rogers A, Bourke E. Osteopetrosis with combined proximal and distal renal tubular acidosis. American Journal of Kidney Diseases : the Official Journal of the National Kidney Foundation. 2: 357-62. PMID 7148827 DOI: 10.1016/S0272-6386(82)80095-4  0.01
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