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Azepanone-based inhibitors of human and rat cathepsin K.
Marquis RW, Ru Y, LoCastro SM, Zeng J, Yamashita DS, Oh HJ, Erhard KF, Davis LD, Tomaszek TA, Tew D, Salyers K, Proksch J, Ward K, Smith B, Levy M, Cummings MD, Haltiwanger RC, Trescher G, Wang B, Hemling ME, Quinn CJ, Cheng HY, Lin F, Smith WW, Janson CA, Zhao B, McQueney MS, D'Alessio K, Lee CP, Marzulli A, Dodds RA, Blake S, Hwang SM, James IE, Gress CJ, Bradley BR, Lark MW, Gowen M, Veber DF. Marquis RW, et al. Among authors: blake s. J Med Chem. 2001 Apr 26;44(9):1380-95. doi: 10.1021/jm000481x. J Med Chem. 2001. PMID: 11311061
Azepanone-based inhibitors of human cathepsin L.
Marquis RW, James I, Zeng J, Trout RE, Thompson S, Rahman A, Yamashita DS, Xie R, Ru Y, Gress CJ, Blake S, Lark MA, Hwang SM, Tomaszek T, Offen P, Head MS, Cummings MD, Veber DF. Marquis RW, et al. Among authors: blake s. J Med Chem. 2005 Nov 3;48(22):6870-8. doi: 10.1021/jm0502079. J Med Chem. 2005. PMID: 16250645
Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate.
Stroup GB, Lark MW, Veber DF, Bhattacharyya A, Blake S, Dare LC, Erhard KF, Hoffman SJ, James IE, Marquis RW, Ru Y, Vasko-Moser JA, Smith BR, Tomaszek T, Gowen M. Stroup GB, et al. Among authors: blake s. J Bone Miner Res. 2001 Oct;16(10):1739-46. doi: 10.1359/jbmr.2001.16.10.1739. J Bone Miner Res. 2001. PMID: 11585335 Free article.
A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys.
Kumar S, Dare L, Vasko-Moser JA, James IE, Blake SM, Rickard DJ, Hwang SM, Tomaszek T, Yamashita DS, Marquis RW, Oh H, Jeong JU, Veber DF, Gowen M, Lark MW, Stroup G. Kumar S, et al. Among authors: blake sm. Bone. 2007 Jan;40(1):122-31. doi: 10.1016/j.bone.2006.07.015. Epub 2006 Sep 7. Bone. 2007. PMID: 16962401
Disease-modifying activity of SB 273005, an orally active, nonpeptide alphavbeta3 (vitronectin receptor) antagonist, in rat adjuvant-induced arthritis.
Badger AM, Blake S, Kapadia R, Sarkar S, Levin J, Swift BA, Hoffman SJ, Stroup GB, Miller WH, Gowen M, Lark MW. Badger AM, et al. Among authors: blake s. Arthritis Rheum. 2001 Jan;44(1):128-37. doi: 10.1002/1529-0131(200101)44:1<128::AID-ANR17>3.0.CO;2-M. Arthritis Rheum. 2001. PMID: 11212150 Free article.
Disease-modifying activity of SB 242235, a selective inhibitor of p38 mitogen-activated protein kinase, in rat adjuvant-induced arthritis.
Badger AM, Griswold DE, Kapadia R, Blake S, Swift BA, Hoffman SJ, Stroup GB, Webb E, Rieman DJ, Gowen M, Boehm JC, Adams JL, Lee JC. Badger AM, et al. Among authors: blake s. Arthritis Rheum. 2000 Jan;43(1):175-83. doi: 10.1002/1529-0131(200001)43:1<175::AID-ANR22>3.0.CO;2-S. Arthritis Rheum. 2000. PMID: 10643714 Free article.
563 results