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Page 1
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: whaley jm. 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
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: whaley jm. 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 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. 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
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: whaley jm. 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
Unique pharmacology of a novel allosteric agonist/sensitizer insulin receptor monoclonal antibody.
Hinke SA, Cieniewicz AM, Kirchner T, D'Aquino K, Nanjunda R, Aligo J, Perkinson R, Cooper P, Boayke K, Chiu ML, Jarantow S, Lacy ER, Liang Y, Johnson DL, Whaley JM, Lingham RB, Kihm AJ. Hinke SA, et al. Among authors: whaley jm. Mol Metab. 2018 Apr;10:87-99. doi: 10.1016/j.molmet.2018.01.014. Epub 2018 Feb 3. Mol Metab. 2018. PMID: 29453154 Free PMC article.
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: whaley jm. 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 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: whaley jm. 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
Carcinogenicity risk assessment supports the chronic safety of dapagliflozin, an inhibitor of sodium-glucose co-transporter 2, in the treatment of type 2 diabetes mellitus.
Reilly TP, Graziano MJ, Janovitz EB, Dorr TE, Fairchild C, Lee F, Chen J, Wong T, Whaley JM, Tirmenstein M. Reilly TP, et al. Among authors: whaley jm. Diabetes Ther. 2014 Jun;5(1):73-96. doi: 10.1007/s13300-014-0053-3. Epub 2014 Jan 29. Diabetes Ther. 2014. PMID: 24474422 Free PMC article.
34 results