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Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease.
Cioffi CL, Racz B, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Zhu L, Kitchen DB, Barnes KD, Dobri N, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K. Cioffi CL, et al. Among authors: cywin cl. J Med Chem. 2015 Aug 13;58(15):5863-88. doi: 10.1021/acs.jmedchem.5b00423. Epub 2015 Aug 4. J Med Chem. 2015. PMID: 26181715 Free PMC article.
Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease.
Cioffi CL, Dobri N, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Golden KC, Zhu L, Kitchen DB, Barnes KD, Racz B, Qin Q, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K. Cioffi CL, et al. Among authors: cywin cl. J Med Chem. 2014 Sep 25;57(18):7731-57. doi: 10.1021/jm5010013. Epub 2014 Sep 11. J Med Chem. 2014. PMID: 25210858 Free PMC article.
Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode.
Qian K, Wang L, Cywin CL, Farmer BT 2nd, Hickey E, Homon C, Jakes S, Kashem MA, Lee G, Leonard S, Li J, Magboo R, Mao W, Pack E, Peng C, Prokopowicz A 3rd, Welzel M, Wolak J, Morwick T. Qian K, et al. Among authors: cywin cl. J Med Chem. 2009 Apr 9;52(7):1814-27. doi: 10.1021/jm801242y. J Med Chem. 2009. PMID: 19256503
5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk).
Winters MP, Robinson DJ, Khine HH, Pullen SS, Woska JR Jr, Raymond EL, Sellati R, Cywin CL, Snow RJ, Kashem MA, Wolak JP, King J, Kaplita PV, Liu LH, Farrell TM, DesJarlais R, Roth GP, Takahashi H, Moriarty KJ. Winters MP, et al. Among authors: cywin cl. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5541-4. doi: 10.1016/j.bmcl.2008.09.016. Epub 2008 Sep 7. Bioorg Med Chem Lett. 2008. PMID: 18823779
Discovery of potent and selective PKC-theta inhibitors.
Cywin CL, Dahmann G, Prokopowicz AS 3rd, Young ER, Magolda RL, Cardozo MG, Cogan DA, Disalvo D, Ginn JD, Kashem MA, Wolak JP, Homon CA, Farrell TM, Grbic H, Hu H, Kaplita PV, Liu LH, Spero DM, Jeanfavre DD, O'Shea KM, White DM, Woska JR Jr, Brown ML. Cywin CL, et al. Bioorg Med Chem Lett. 2007 Jan 1;17(1):225-30. doi: 10.1016/j.bmcl.2006.09.056. Epub 2006 Oct 19. Bioorg Med Chem Lett. 2007. PMID: 17055721
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