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Page 1
Discovery of cofactor-specific, bactericidal Mycobacterium tuberculosis InhA inhibitors using DNA-encoded library technology.
Soutter HH, Centrella P, Clark MA, Cuozzo JW, Dumelin CE, Guie MA, Habeshian S, Keefe AD, Kennedy KM, Sigel EA, Troast DM, Zhang Y, Ferguson AD, Davies G, Stead ER, Breed J, Madhavapeddi P, Read JA. Soutter HH, et al. Among authors: centrella p. Proc Natl Acad Sci U S A. 2016 Dec 6;113(49):E7880-E7889. doi: 10.1073/pnas.1610978113. Epub 2016 Nov 18. Proc Natl Acad Sci U S A. 2016. PMID: 27864515 Free PMC article.
Design, synthesis and selection of DNA-encoded small-molecule libraries.
Clark MA, Acharya RA, Arico-Muendel CC, Belyanskaya SL, Benjamin DR, Carlson NR, Centrella PA, Chiu CH, Creaser SP, Cuozzo JW, Davie CP, Ding Y, Franklin GJ, Franzen KD, Gefter ML, Hale SP, Hansen NJ, Israel DI, Jiang J, Kavarana MJ, Kelley MS, Kollmann CS, Li F, Lind K, Mataruse S, Medeiros PF, Messer JA, Myers P, O'Keefe H, Oliff MC, Rise CE, Satz AL, Skinner SR, Svendsen JL, Tang L, van Vloten K, Wagner RW, Yao G, Zhao B, Morgan BA. Clark MA, et al. Among authors: centrella pa. Nat Chem Biol. 2009 Sep;5(9):647-54. doi: 10.1038/nchembio.211. Epub 2009 Aug 2. Nat Chem Biol. 2009. PMID: 19648931
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).
Deng H, O'Keefe H, Davie CP, Lind KE, Acharya RA, Franklin GJ, Larkin J, Matico R, Neeb M, Thompson MM, Lohr T, Gross JW, Centrella PA, O'Donovan GK, Bedard KL, van Vloten K, Mataruse S, Skinner SR, Belyanskaya SL, Carpenter TY, Shearer TW, Clark MA, Cuozzo JW, Arico-Muendel CC, Morgan BA. Deng H, et al. Among authors: centrella pa. J Med Chem. 2012 Aug 23;55(16):7061-79. doi: 10.1021/jm300449x. Epub 2012 Aug 14. J Med Chem. 2012. PMID: 22891645
Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA.
Encinas L, O'Keefe H, Neu M, Remuiñán MJ, Patel AM, Guardia A, Davie CP, Pérez-Macías N, Yang H, Convery MA, Messer JA, Pérez-Herrán E, Centrella PA, Alvarez-Gómez D, Clark MA, Huss S, O'Donovan GK, Ortega-Muro F, McDowell W, Castañeda P, Arico-Muendel CC, Pajk S, Rullás J, Angulo-Barturen I, Alvarez-Ruíz E, Mendoza-Losana A, Ballell Pages L, Castro-Pichel J, Evindar G. Encinas L, et al. Among authors: centrella pa. J Med Chem. 2014 Feb 27;57(4):1276-88. doi: 10.1021/jm401326j. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24450589
Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Yang H, Medeiros PF, Raha K, Elkins P, Lind KE, Lehr R, Adams ND, Burgess JL, Schmidt SJ, Knight SD, Auger KR, Schaber MD, Franklin GJ, Ding Y, DeLorey JL, Centrella PA, Mataruse S, Skinner SR, Clark MA, Cuozzo JW, Evindar G. Yang H, et al. Among authors: centrella pa. ACS Med Chem Lett. 2015 Mar 20;6(5):531-6. doi: 10.1021/acsmedchemlett.5b00025. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005528 Free PMC article.
Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library.
Deng H, Zhou J, Sundersingh FS, Summerfield J, Somers D, Messer JA, Satz AL, Ancellin N, Arico-Muendel CC, Sargent Bedard KL, Beljean A, Belyanskaya SL, Bingham R, Smith SE, Boursier E, Carter P, Centrella PA, Clark MA, Chung CW, Davie CP, Delorey JL, Ding Y, Franklin GJ, Grady LC, Herry K, Hobbs C, Kollmann CS, Morgan BA, Pothier Kaushansky LJ, Zhou Q. Deng H, et al. Among authors: centrella pa. ACS Med Chem Lett. 2015 Jul 21;6(8):919-24. doi: 10.1021/acsmedchemlett.5b00179. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288694 Free PMC article.
Cell-Based Selection Expands the Utility of DNA-Encoded Small-Molecule Library Technology to Cell Surface Drug Targets: Identification of Novel Antagonists of the NK3 Tachykinin Receptor.
Wu Z, Graybill TL, Zeng X, Platchek M, Zhang J, Bodmer VQ, Wisnoski DD, Deng J, Coppo FT, Yao G, Tamburino A, Scavello G, Franklin GJ, Mataruse S, Bedard KL, Ding Y, Chai J, Summerfield J, Centrella PA, Messer JA, Pope AJ, Israel DI. Wu Z, et al. ACS Comb Sci. 2015 Dec 14;17(12):722-31. doi: 10.1021/acscombsci.5b00124. Epub 2015 Dec 3. ACS Comb Sci. 2015. PMID: 26562224
Design and Synthesis of Biaryl DNA-Encoded Libraries.
Ding Y, Franklin GJ, DeLorey JL, Centrella PA, Mataruse S, Clark MA, Skinner SR, Belyanskaya S. Ding Y, et al. ACS Comb Sci. 2016 Oct 10;18(10):625-629. doi: 10.1021/acscombsci.6b00078. Epub 2016 Sep 1. ACS Comb Sci. 2016. PMID: 27571034
34 results