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Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ.
Bubenik M, Mader P, Mochirian P, Vallée F, Clark J, Truchon JF, Perryman AL, Pau V, Kurinov I, Zahn KE, Leclaire ME, Papp R, Mathieu MC, Hamel M, Duffy NM, Godbout C, Casas-Selves M, Falgueyret JP, Baruah PS, Nicolas O, Stocco R, Poirier H, Martino G, Fortin AB, Roulston A, Chefson A, Dorich S, St-Onge M, Patel P, Pellerin C, Ciblat S, Pinter T, Barabé F, El Bakkouri M, Parikh P, Gervais C, Sfeir A, Mamane Y, Morris SJ, Black WC, Sicheri F, Gallant M. Bubenik M, et al. Among authors: black wc. J Med Chem. 2022 Oct 13;65(19):13198-13215. doi: 10.1021/acs.jmedchem.2c00998. Epub 2022 Sep 20. J Med Chem. 2022. PMID: 36126059 Free PMC article.
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Black WC, Bayly CI, Davis DE, Desmarais S, Falgueyret JP, Léger S, Li CS, Massé F, McKay DJ, Palmer JT, Percival MD, Robichaud J, Tsou N, Zamboni R. Black WC, et al. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4741-4. doi: 10.1016/j.bmcl.2005.07.071. Bioorg Med Chem Lett. 2005. PMID: 16154747
Identification of a potent and selective non-basic cathepsin K inhibitor.
Li CS, Deschenes D, Desmarais S, Falgueyret JP, Gauthier JY, Kimmel DB, Léger S, Massé F, McGrath ME, McKay DJ, Percival MD, Riendeau D, Rodan SB, Thérien M, Truong VL, Wesolowski G, Zamboni R, Black WC. Li CS, et al. Among authors: black wc. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9. doi: 10.1016/j.bmcl.2005.12.071. Epub 2006 Jan 18. Bioorg Med Chem Lett. 2006. PMID: 16413777
Primary amides as selective inhibitors of cathepsin K.
Léger S, Bayly CI, Black WC, Desmarais S, Falgueyret JP, Massé F, Percival MD, Truchon JF. Léger S, et al. Among authors: black wc. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4328-32. doi: 10.1016/j.bmcl.2007.05.024. Epub 2007 May 16. Bioorg Med Chem Lett. 2007. PMID: 17544269
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
Gauthier JY, Black WC, Courchesne I, Cromlish W, Desmarais S, Houle R, Lamontagne S, Li CS, Massé F, McKay DJ, Ouellet M, Robichaud J, Truchon JF, Truong VL, Wang Q, Percival MD. Gauthier JY, et al. Among authors: black wc. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33. doi: 10.1016/j.bmcl.2007.06.023. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17590332
Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.
Robichaud J, Black WC, Thérien M, Paquet J, Oballa RM, Bayly CI, McKay DJ, Wang Q, Isabel E, Léger S, Mellon C, Kimmel DB, Wesolowski G, Percival MD, Massé F, Desmarais S, Falgueyret JP, Crane SN. Robichaud J, et al. Among authors: black wc. J Med Chem. 2008 Oct 23;51(20):6410-20. doi: 10.1021/jm800610j. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811135
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.
Isabel E, Bateman KP, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Gauthier JY, Lamontagne S, Lau CK, Léger S, LeRiche T, Lévesque JF, Li CS, Massé F, McKay DJ, Mellon C, Nicoll-Griffith DA, Oballa RM, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC. Isabel E, et al. Among authors: black wc. Bioorg Med Chem Lett. 2010 Feb 1;20(3):887-92. doi: 10.1016/j.bmcl.2009.12.083. Epub 2009 Dec 28. Bioorg Med Chem Lett. 2010. PMID: 20061146
415 results