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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: antrilli tm. 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
Evaluation of PAI-039 [{1-benzyl-5-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}(oxo)acetic acid], a novel plasminogen activator inhibitor-1 inhibitor, in a canine model of coronary artery thrombosis.
Hennan JK, Elokdah H, Leal M, Ji A, Friedrichs GS, Morgan GA, Swillo RE, Antrilli TM, Hreha A, Crandall DL. Hennan JK, et al. Among authors: antrilli tm. J Pharmacol Exp Ther. 2005 Aug;314(2):710-6. doi: 10.1124/jpet.105.084129. Epub 2005 Apr 28. J Pharmacol Exp Ther. 2005. PMID: 15860572
WAY-140312 reduces plasma PAI-1 while maintaining normal platelet aggregation.
Crandall DL, Hennan JK, Elokdah H, Krishnamurthy G, Antrilli TM, Bauer JS, Morgan GA, Swillo RE. Crandall DL, et al. Among authors: antrilli tm. Biochem Biophys Res Commun. 2003 Nov 28;311(4):904-8. doi: 10.1016/j.bbrc.2003.10.088. Biochem Biophys Res Commun. 2003. PMID: 14623266