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Page 1
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: james i. J Med Chem. 2005 Nov 3;48(22):6870-8. doi: 10.1021/jm0502079. J Med Chem. 2005. PMID: 16250645
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.
Yamashita DS, Marquis RW, Xie R, Nidamarthy SD, Oh HJ, Jeong JU, Erhard KF, Ward KW, Roethke TJ, Smith BR, Cheng HY, Geng X, Lin F, Offen PH, Wang B, Nevins N, Head MS, Haltiwanger RC, Narducci Sarjeant AA, Liable-Sands LM, Zhao B, Smith WW, Janson CA, Gao E, Tomaszek T, McQueney M, James IE, Gress CJ, Zembryki DL, Lark MW, Veber DF. Yamashita DS, et al. J Med Chem. 2006 Mar 9;49(5):1597-612. doi: 10.1021/jm050915u. J Med Chem. 2006. PMID: 16509577
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: james ie. J Med Chem. 2001 Apr 26;44(9):1380-95. doi: 10.1021/jm000481x. J Med Chem. 2001. PMID: 11311061
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: james ie. Bone. 2007 Jan;40(1):122-31. doi: 10.1016/j.bone.2006.07.015. Epub 2006 Sep 7. Bone. 2007. PMID: 16962401
Design of potent and selective human cathepsin K inhibitors that span the active site.
Thompson SK, Halbert SM, Bossard MJ, Tomaszek TA, Levy MA, Zhao B, Smith WW, Abdel-Meguid SS, Janson CA, D'Alessio KJ, McQueney MS, Amegadzie BY, Hanning CR, DesJarlais RL, Briand J, Sarkar SK, Huddleston MJ, Ijames CF, Carr SA, Garnes KT, Shu A, Heys JR, Bradbeer J, Zembryki D, Lee-Rykaczewski L, James IE, Lark MW, Drake FH, Gowen M, Gleason JG, Veber DF. Thompson SK, et al. Among authors: james ie. Proc Natl Acad Sci U S A. 1997 Dec 23;94(26):14249-54. doi: 10.1073/pnas.94.26.14249. Proc Natl Acad Sci U S A. 1997. PMID: 9405598 Free PMC article.
Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.
Miller WH, Manley PJ, Cousins RD, Erhard KF, Heerding DA, Kwon C, Ross ST, Samanen JM, Takata DT, Uzinskas IN, Yuan CC, Haltiwanger RC, Gress CJ, Lark MW, Hwang SM, James IE, Rieman DJ, Willette RN, Yue TL, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF. Miller WH, et al. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1483-6. doi: 10.1016/s0960-894x(03)00102-1. Bioorg Med Chem Lett. 2003. PMID: 12668017
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: james ie. 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.
645 results