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Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST, Qi Y, Rocke BN, Smith A, Warmus JS, Zhang Y, Bowles D, Widlicka DW, Eng H, Ryder T, Sharma R, Wolford A, Okerberg C, Walters K, Maurer TS, Zhang Y, Bonin PD, Spath SN, Xing G, Hepworth D, Ahn K, Kalgutkar AS. Ruggeri RB, et al. Among authors: carpino pa. J Med Chem. 2015 Nov 12;58(21):8513-28. doi: 10.1021/acs.jmedchem.5b00963. Epub 2015 Oct 28. J Med Chem. 2015. PMID: 26509551
Deconstruction of activity-dependent covalent modification of heme in human neutrophil myeloperoxidase by multistage mass spectrometry (MS(4)).
Geoghegan KF, Varghese AH, Feng X, Bessire AJ, Conboy JJ, Ruggeri RB, Ahn K, Spath SN, Filippov SV, Conrad SJ, Carpino PA, Guimarães CR, Vajdos FF. Geoghegan KF, et al. Among authors: carpino pa. Biochemistry. 2012 Mar 13;51(10):2065-77. doi: 10.1021/bi201872j. Epub 2012 Mar 1. Biochemistry. 2012. PMID: 22352991
Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3.
Huard K, Londregan AT, Tesz G, Bahnck KB, Magee TV, Hepworth D, Polivkova J, Coffey SB, Pabst BA, Gosset JR, Nigam A, Kou K, Sun H, Lee K, Herr M, Boehm M, Carpino PA, Goodwin B, Perreault C, Li Q, Jorgensen CC, Tkalcevic GT, Subashi TA, Ahn K. Huard K, et al. Among authors: carpino pa. J Med Chem. 2015 Sep 24;58(18):7164-72. doi: 10.1021/acs.jmedchem.5b01008. Epub 2015 Sep 8. J Med Chem. 2015. PMID: 26258602
Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2).
Futatsugi K, Kung DW, Orr ST, Cabral S, Hepworth D, Aspnes G, Bader S, Bian J, Boehm M, Carpino PA, Coffey SB, Dowling MS, Herr M, Jiao W, Lavergne SY, Li Q, Clark RW, Erion DM, Kou K, Lee K, Pabst BA, Perez SM, Purkal J, Jorgensen CC, Goosen TC, Gosset JR, Niosi M, Pettersen JC, Pfefferkorn JA, Ahn K, Goodwin B. Futatsugi K, et al. Among authors: carpino pa. J Med Chem. 2015 Sep 24;58(18):7173-85. doi: 10.1021/acs.jmedchem.5b01006. J Med Chem. 2015. PMID: 26349027
Development of a selective activity-based probe for glycosylated LIPA.
Schwaid AG, Ruangsiriluk W, Reyes AR, Cabral S, Rajamohan F, Tu M, Ward J, Carpino PA. Schwaid AG, et al. Among authors: carpino pa. Bioorg Med Chem Lett. 2016 Apr 15;26(8):1993-6. doi: 10.1016/j.bmcl.2016.02.089. Epub 2016 Mar 2. Bioorg Med Chem Lett. 2016. PMID: 26965858
A Small-Molecule Anti-secretagogue of PCSK9 Targets the 80S Ribosome to Inhibit PCSK9 Protein Translation.
Petersen DN, Hawkins J, Ruangsiriluk W, Stevens KA, Maguire BA, O'Connell TN, Rocke BN, Boehm M, Ruggeri RB, Rolph T, Hepworth D, Loria PM, Carpino PA. Petersen DN, et al. Among authors: carpino pa. Cell Chem Biol. 2016 Nov 17;23(11):1362-1371. doi: 10.1016/j.chembiol.2016.08.016. Epub 2016 Oct 13. Cell Chem Biol. 2016. PMID: 27746128 Free article.
Structural basis for AMPK activation: natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms.
Calabrese MF, Rajamohan F, Harris MS, Caspers NL, Magyar R, Withka JM, Wang H, Borzilleri KA, Sahasrabudhe PV, Hoth LR, Geoghegan KF, Han S, Brown J, Subashi TA, Reyes AR, Frisbie RK, Ward J, Miller RA, Landro JA, Londregan AT, Carpino PA, Cabral S, Smith AC, Conn EL, Cameron KO, Qiu X, Kurumbail RG. Calabrese MF, et al. Among authors: carpino pa. Structure. 2014 Aug 5;22(8):1161-1172. doi: 10.1016/j.str.2014.06.009. Epub 2014 Jul 24. Structure. 2014. PMID: 25066137 Free article.
37 results