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Identification of 6-hydroxy-5-phenyl sulfonylpyrimidin-4(1H)-one APJ receptor agonists.
Tora G, Jiang J, Bostwick JS, Gargalovic PS, Onorato JM, Luk CE, Generaux C, Xu C, Galella MA, Wang T, He Y, Wexler RR, Finlay HJ. Tora G, et al. Among authors: gargalovic ps. Bioorg Med Chem Lett. 2021 Oct 15;50:128325. doi: 10.1016/j.bmcl.2021.128325. Epub 2021 Aug 14. Bioorg Med Chem Lett. 2021. PMID: 34403724
In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure.
Gargalovic P, Wong P, Onorato J, Finlay H, Wang T, Yan M, Crain E, St-Onge S, Héroux M, Bouvier M, Xu C, Chen XQ, Generaux C, Lawrence M, Wexler R, Gordon D. Gargalovic P, et al. Circ Heart Fail. 2021 Mar;14(3):e007351. doi: 10.1161/CIRCHEARTFAILURE.120.007351. Epub 2021 Mar 5. Circ Heart Fail. 2021. PMID: 33663236 Free PMC article.
Design and preparation of N-linked hydroxypyridine-based APJ agonists.
Richter JM, Alex Bates J, Gargalovic P, Onorato JM, Generaux C, Wang T, Gordon DA, Wexler RR, Finlay HJ. Richter JM, et al. Bioorg Med Chem Lett. 2022 Oct 1;73:128882. doi: 10.1016/j.bmcl.2022.128882. Epub 2022 Jul 8. Bioorg Med Chem Lett. 2022. PMID: 35817293
Discovery and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ.
Myers MC, Bilder DM, Cavallaro CL, Chao HJ, Su S, Burford NT, Nayeem A, Wang T, Yan M, Langish RA, Dabros M, Li YX, Rose AV, Behnia K, Onorato JM, Gargalovic PS, Wexler RR, Lawrence RM. Myers MC, et al. Among authors: gargalovic ps. Bioorg Med Chem Lett. 2020 Apr 1;30(7):126955. doi: 10.1016/j.bmcl.2020.126955. Epub 2020 Jan 22. Bioorg Med Chem Lett. 2020. PMID: 32035698
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.
Johnson JA, Kim SH, Jiang J, Phillips M, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Luk CE, Generaux C, He Y, Chen XQ, Xu C, Galella MA, Wang T, Gordon DA, Wexler RR, Finlay HJ. Johnson JA, et al. Among authors: gargalovic ps. J Med Chem. 2021 Mar 25;64(6):3086-3099. doi: 10.1021/acs.jmedchem.0c01878. Epub 2021 Mar 9. J Med Chem. 2021. PMID: 33689340
Identification of 6-Hydroxypyrimidin-4(1H)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists.
Pi Z, Johnson JA, Meng W, Phillips M, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Generaux CN, Wang T, He Y, Gordon DA, Wexler RR, Finlay HJ. Pi Z, et al. Among authors: gargalovic ps. ACS Med Chem Lett. 2021 Oct 22;12(11):1766-1772. doi: 10.1021/acsmedchemlett.1c00385. eCollection 2021 Nov 11. ACS Med Chem Lett. 2021. PMID: 34795866 Free PMC article.
Biphenyl Acid Derivatives as APJ Receptor Agonists.
Su S, Clarke A, Han Y, Chao HJ, Bostwick J, Schumacher W, Wang T, Yan M, Hsu MY, Simmons E, Luk C, Xu C, Dabros M, Galella M, Onorato J, Gordon D, Wexler R, Gargalovic PS, Lawrence RM. Su S, et al. Among authors: gargalovic ps. J Med Chem. 2019 Nov 27;62(22):10456-10465. doi: 10.1021/acs.jmedchem.9b01513. Epub 2019 Nov 14. J Med Chem. 2019. PMID: 31724863
Linking (Pyr)1apelin-13 pharmacokinetics to efficacy: Stabilization and measurement of a high clearance peptide in rodents.
Onorato JM, Xu C, Chen XQ, Rose AV, Generaux C, Lentz K, Shipkova P, Arthur S, Hennan JK, Haskell R, Myers MC, Lawrence RM, Finlay HJ, Basso M, Bostwick J, Fernando G, Garcia R, Hellings S, Hsu MY, Zhang R, Zhao L, Gargalovic P. Onorato JM, et al. Anal Biochem. 2019 Mar 1;568:41-50. doi: 10.1016/j.ab.2018.12.022. Epub 2018 Dec 31. Anal Biochem. 2019. PMID: 30605634
38 results