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Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).
Zhou HJ, Aujay MA, Bennett MK, Dajee M, Demo SD, Fang Y, Ho MN, Jiang J, Kirk CJ, Laidig GJ, Lewis ER, Lu Y, Muchamuel T, Parlati F, Ring E, Shenk KD, Shields J, Shwonek PJ, Stanton T, Sun CM, Sylvain C, Woo TM, Yang J. Zhou HJ, et al. Among authors: muchamuel t. J Med Chem. 2009 May 14;52(9):3028-38. doi: 10.1021/jm801329v. J Med Chem. 2009. PMID: 19348473
Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit.
Johnson HWB, Anderl JL, Bradley EK, Bui J, Jones J, Arastu-Kapur S, Kelly LM, Lowe E, Moebius DC, Muchamuel T, Kirk C, Wang Z, McMinn D. Johnson HWB, et al. Among authors: muchamuel t. ACS Med Chem Lett. 2017 Mar 9;8(4):413-417. doi: 10.1021/acsmedchemlett.6b00496. eCollection 2017 Apr 13. ACS Med Chem Lett. 2017. PMID: 28435528 Free PMC article.
Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide).
Johnson HWB, Lowe E, Anderl JL, Fan A, Muchamuel T, Bowers S, Moebius DC, Kirk C, McMinn DL. Johnson HWB, et al. Among authors: muchamuel t. J Med Chem. 2018 Dec 27;61(24):11127-11143. doi: 10.1021/acs.jmedchem.8b01201. Epub 2018 Dec 11. J Med Chem. 2018. PMID: 30380863
23 results