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Page 1
Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Turdi H, Chao H, Hangeland JJ, Ahmad S, Meng W, Brigance R, Zhao G, Wang W, Moore F, Ye XY, Mathur A, Hou X, Kempson J, Wu DR, Li YX, Azzara AV, Ma Z, Chu CH, Chen L, Cullen MJ, Rooney S, Harvey S, Kopcho L, Panemangelor R, Abell L, O'Malley K, Keim WJ, Dierks E, Chang S, Foster K, Apedo A, Harden D, Dabros M, Gao Q, Pelleymounter MA, Whaley JM, Robl JA, Cheng D, Lawrence RM, Devasthale P. Turdi H, et al. Among authors: foster k. J Med Chem. 2021 Oct 14;64(19):14773-14792. doi: 10.1021/acs.jmedchem.1c01356. Epub 2021 Oct 6. J Med Chem. 2021. PMID: 34613725
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.
Jurica EA, Wu X, Williams KN, Hernandez AS, Nirschl DS, Rampulla RA, Mathur A, Zhou M, Cao G, Xie C, Jacob B, Cai H, Wang T, Murphy BJ, Liu H, Xu C, Kunselman LK, Hicks MB, Sun Q, Schnur DM, Sitkoff DF, Dierks EA, Apedo A, Moore DB, Foster KA, Cvijic ME, Panemangalore R, Flynn NA, Maxwell BD, Hong Y, Tian Y, Wilkes JJ, Zinker BA, Whaley JM, Barrish JC, Robl JA, Ewing WR, Ellsworth BA. Jurica EA, et al. Among authors: foster ka. J Med Chem. 2017 Feb 23;60(4):1417-1431. doi: 10.1021/acs.jmedchem.6b01559. Epub 2017 Feb 9. J Med Chem. 2017. PMID: 28112924
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists.
Carpenter J, Wang Y, Wu G, Feng J, Ye XY, Morales CL, Broekema M, Rossi KA, Miller KJ, Murphy BJ, Wu G, Malmstrom SE, Azzara AV, Sher PM, Fevig JM, Alt A, Bertekap RL Jr, Cullen MJ, Harper TM, Foster K, Luk E, Xiang Q, Grubb MF, Robl JA, Wacker DA. Carpenter J, et al. Among authors: foster k. J Med Chem. 2017 Jul 27;60(14):6166-6190. doi: 10.1021/acs.jmedchem.7b00385. Epub 2017 Jul 7. J Med Chem. 2017. PMID: 28635286
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Shi J, Gu Z, Jurica EA, Wu X, Haque LE, Williams KN, Hernandez AS, Hong Z, Gao Q, Dabros M, Davulcu AH, Mathur A, Rampulla RA, Gupta AK, Jayaram R, Apedo A, Moore DB, Liu H, Kunselman LK, Brady EJ, Wilkes JJ, Zinker BA, Cai H, Shu YZ, Sun Q, Dierks EA, Foster KA, Xu C, Wang T, Panemangalore R, Cvijic ME, Xie C, Cao GG, Zhou M, Krupinski J, Whaley JM, Robl JA, Ewing WR, Ellsworth BA. Shi J, et al. Among authors: foster ka. J Med Chem. 2018 Feb 8;61(3):681-694. doi: 10.1021/acs.jmedchem.7b00982. Epub 2018 Jan 27. J Med Chem. 2018. PMID: 29316397
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
Cherney EC, Zhang L, Nara S, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, Darienzo C, Discenza L, Ranasinghe A, Grubb M, Ziemba T, Traeger SC, Li X, Johnston K, Kopcho L, Fereshteh M, Foster K, Stefanski K, Fargnoli J, Swanson J, Brown J, Delpy D, Seitz SP, Borzilleri R, Vite G, Balog A. Cherney EC, et al. Among authors: foster k. ACS Med Chem Lett. 2021 Jan 28;12(2):288-294. doi: 10.1021/acsmedchemlett.0c00668. eCollection 2021 Feb 11. ACS Med Chem Lett. 2021. PMID: 33603977 Free PMC article.
Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.
Cherney EC, Zhang L, Guo W, Huang A, Williams D, Seitz S, Shan W, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, D'Arienzo CJ, Discenza LN, Ranasinghe A, Grubb MF, Traeger SC, Li X, Johnston KA, Kopcho L, Fereshteh M, Foster KA, Stefanski K, Delpy D, Dhar G, Anandam A, Mahankali S, Padmanabhan S, Rajanna P, Murali V, Mariappan TT, Pattasseri S, Nimje RY, Hong Z, Kempson J, Rampulla R, Mathur A, Gupta A, Borzilleri R, Vite G, Balog A. Cherney EC, et al. Among authors: foster ka. ACS Med Chem Lett. 2021 Jun 16;12(7):1143-1150. doi: 10.1021/acsmedchemlett.1c00236. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267885 Free PMC article.
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.
Jurica EA, Wu X, Williams KN, Haque LE, Rampulla RA, Mathur A, Zhou M, Cao G, Cai H, Wang T, Liu H, Xu C, Kunselman LK, Antrilli TM, Hicks MB, Sun Q, Dierks EA, Apedo A, Moore DB, Foster KA, Cvijic ME, Panemangalore R, Khandelwal P, Wilkes JJ, Zinker BA, Robertson DG, Janovitz EB, Galella M, Li YX, Li J, Ramar T, Jalagam PR, Jayaram R, Whaley JM, Barrish JC, Robl JA, Ewing WR, Ellsworth BA. Jurica EA, et al. Among authors: foster ka. Bioorg Med Chem. 2023 May 1;85:117273. doi: 10.1016/j.bmc.2023.117273. Epub 2023 Apr 4. Bioorg Med Chem. 2023. PMID: 37030194
Discovery of novel pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.
Moore F, Wang W, Zhao G, Mignone J, Meng W, Chu CH, Ma Z, Azzara A, Cullen MJ, Pelleymounter MA, Appiah K, Cvijic ME, Dierks E, Chang S, Foster K, Kopcho L, O'Malley K, Li YX, Khandelwal P, Whaley JM, Mathur A, Hou X, Wu DR, Robl JA, Cheng D, Devasthale P. Moore F, et al. Among authors: foster k. Bioorg Med Chem Lett. 2023 Jul 15;91:129362. doi: 10.1016/j.bmcl.2023.129362. Epub 2023 Jun 8. Bioorg Med Chem Lett. 2023. PMID: 37295614
Discovery of 12 (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders.
Meng W, Brigance R, Mignone J, Negash L, Zhao G, Ahmad S, Wang W, Moore F, Ye XY, Sun JH, Mathur A, Li YX, Azzara A, Ma Z, Chu CH, Cullen MJ, Rooney S, Harvey S, Kopcho L, Abell L, O'Malley K, Keim W, Dierks EA, Chang S, Foster KA, Harden D, Dabros M, Goti V, De Oliveira C, Krishna G, Pelleymounter MA, Whaley J, Robl JA, Cheng D, Devasthale P. Meng W, et al. Among authors: foster ka. J Med Chem. 2023 Sep 28;66(18):13135-13147. doi: 10.1021/acs.jmedchem.3c01147. Epub 2023 Sep 19. J Med Chem. 2023. PMID: 37724542
1,463 results