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Page 1
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: lark mw. J Med Chem. 2001 Apr 26;44(9):1380-95. doi: 10.1021/jm000481x. J Med Chem. 2001. PMID: 11311061
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. Among authors: lark mw. J Med Chem. 2006 Mar 9;49(5):1597-612. doi: 10.1021/jm050915u. J Med Chem. 2006. PMID: 16509577
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: lark mw. 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.
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: lark mw. 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.
Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.
Miller WH, Alberts DP, Bhatnagar PK, Bondinell WE, Callahan JF, Calvo RR, Cousins RD, Erhard KF, Heerding DA, Keenan RM, Kwon C, Manley PJ, Newlander KA, Ross ST, Samanen JM, Uzinskas IN, Venslavsky JW, Yuan CC, Haltiwanger RC, Gowen M, Hwang SM, James IE, Lark MW, Rieman DJ, Stroup GB, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF. Miller WH, et al. Among authors: lark mw. J Med Chem. 2000 Jan 13;43(1):22-6. doi: 10.1021/jm990446u. J Med Chem. 2000. PMID: 10633035 No abstract available.
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. Among authors: lark mw. 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 nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality.
Lee D, Long SA, Adams JL, Chan G, Vaidya KS, Francis TA, Kikly K, Winkler JD, Sung CM, Debouck C, Richardson S, Levy MA, DeWolf WE Jr, Keller PM, Tomaszek T, Head MS, Ryan MD, Haltiwanger RC, Liang PH, Janson CA, McDevitt PJ, Johanson K, Concha NO, Chan W, Abdel-Meguid SS, Badger AM, Lark MW, Nadeau DP, Suva LJ, Gowen M, Nuttall ME. Lee D, et al. Among authors: lark mw. J Biol Chem. 2000 May 26;275(21):16007-14. doi: 10.1074/jbc.275.21.16007. J Biol Chem. 2000. PMID: 10821855 Free article.
110 results