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Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors.
Bachovchin DA, Mohr JT, Speers AE, Wang C, Berlin JM, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Schürer SC, Nomura DK, Rosen H, Fu GC, Cravatt BF. Bachovchin DA, et al. Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6811-6. doi: 10.1073/pnas.1015248108. Epub 2011 Mar 11. Proc Natl Acad Sci U S A. 2011. PMID: 21398589 Free PMC article.
Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2).
Nagano JM, Hsu KL, Whitby LR, Niphakis MJ, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder P, Srinivasan P, Gonzalez TD, Rosen H, Bahnson BJ, Cravatt BF. Nagano JM, et al. Bioorg Med Chem Lett. 2013 Feb 1;23(3):839-43. doi: 10.1016/j.bmcl.2012.11.061. Epub 2012 Dec 2. Bioorg Med Chem Lett. 2013. PMID: 23260346 Free PMC article.
Identification of Potent and Selective Inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (PfM18AAP) of Human Malaria via High-Throughput Screening.
Spicer T, Fernandez-Vega V, Chase P, Scampavia L, To J, Dalton JP, Da Silva FL, Skinner-Adams TS, Gardiner DL, Trenholme KR, Brown CL, Ghosh P, Porubsky P, Wang JL, Whipple DA, Schoenen FJ, Hodder P. Spicer T, et al. J Biomol Screen. 2014 Aug;19(7):1107-15. doi: 10.1177/1087057114525852. Epub 2014 Mar 11. J Biomol Screen. 2014. PMID: 24619116 Free PMC article.
Target-based screen against a periplasmic serine protease that regulates intrabacterial pH homeostasis in Mycobacterium tuberculosis.
Zhao N, Darby CM, Small J, Bachovchin DA, Jiang X, Burns-Huang KE, Botella H, Ehrt S, Boger DL, Anderson ED, Cravatt BF, Speers AE, Fernandez-Vega V, Hodder PS, Eberhart C, Rosen H, Spicer TP, Nathan CF. Zhao N, et al. ACS Chem Biol. 2015 Feb 20;10(2):364-71. doi: 10.1021/cb500746z. Epub 2014 Dec 5. ACS Chem Biol. 2015. PMID: 25457457 Free PMC article.
Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival.
Chang JW, Zuhl AM, Speers AE, Niessen S, Brown SJ, Mulvihill MM, Fan YC, Spicer TP, Southern M, Scampavia L, Fernandez-Vega V, Dix MM, Cameron MD, Hodder PS, Rosen H, Nomura DK, Kwon O, Hsu KL, Cravatt BF. Chang JW, et al. ACS Chem Biol. 2015 Apr 17;10(4):925-32. doi: 10.1021/cb500893q. Epub 2015 Jan 20. ACS Chem Biol. 2015. PMID: 25602368 Free PMC article.
45 results