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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: cao g. 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 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: cao g. 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
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: cao gg. 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 BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Nara SJ, Jogi S, Cheruku S, Kandhasamy S, Jaipuri F, Kathi PK, Reddy S, Sarodaya S, Cook EM, Wang T, Sitkoff D, Rossi KA, Ruzanov M, Kiefer SE, Khan JA, Gao M, Reddy S, Sivaprasad Lvj S, Sane R, Mosure K, Zhuo X, Cao GG, Ziegler M, Azzara A, Krupinski J, Soars MG, Ellsworth BA, Wacker DA. Nara SJ, et al. Among authors: cao gg. J Med Chem. 2022 Jul 14;65(13):8948-8960. doi: 10.1021/acs.jmedchem.2c00165. Epub 2022 Jun 15. J Med Chem. 2022. PMID: 35704802
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Carpenter J, Wu G, Wang Y, Cook EM, Wang T, Sitkoff D, Rossi KA, Mosure K, Zhuo X, Cao GG, Ziegler M, Azzara AV, Krupinski J, Soars MG, Ellsworth BA, Wacker DA. Carpenter J, et al. Among authors: cao gg. ACS Med Chem Lett. 2021 Aug 5;12(9):1413-1420. doi: 10.1021/acsmedchemlett.1c00198. eCollection 2021 Sep 9. ACS Med Chem Lett. 2021. PMID: 34531950 Free PMC article.
Targeting tumor suppressor p53 for organ fibrosis therapy.
Bao YN, Yang Q, Shen XL, Yu WK, Zhou L, Zhu QR, Shan QY, Wang ZC, Cao G. Bao YN, et al. Among authors: cao g. Cell Death Dis. 2024 May 14;15(5):336. doi: 10.1038/s41419-024-06702-w. Cell Death Dis. 2024. PMID: 38744865 Free article. Review.
4,496 results