Tomaszek T - Search Results

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: tomaszek t. J Med Chem. 2005 Nov 3;48(22):6870-8. doi: 10.1021/jm0502079. J Med Chem. 2005. PMID: 16250645

2

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: tomaszek t. J Med Chem. 2006 Mar 9;49(5):1597-612. doi: 10.1021/jm050915u. J Med Chem. 2006. PMID: 16509577

3

Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.

Kerns JK, Nie H, Bondinell W, Widdowson KL, Yamashita DS, Rahman A, Podolin PL, Carpenter DC, Jin Q, Riflade B, Dong X, Nevins N, Keller PM, Mitchell L, Tomaszek T. Kerns JK, et al. Among authors: tomaszek t. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4409-15. doi: 10.1016/j.bmcl.2011.06.045. Epub 2011 Jun 17. Bioorg Med Chem Lett. 2011. PMID: 21733692

4

An azepanone-based inhibitor of human cathepsin K with improved oral bioavailability in the rat and the monkey.

Marquis RW, Ward KW, Roethke T, Smith BR, Ru Y, Yamashita DS, Tomaszek TA, Gorycki PD, Cheng HY, James IE, Stroup GB, Lark MW, Gowen M, Veber DF. Marquis RW, et al. Among authors: tomaszek ta. Mol Pharm. 2004 Jan 12;1(1):97-100. doi: 10.1021/mp034017a. Mol Pharm. 2004. PMID: 15832505 No abstract available.

5

Cyclic ketone inhibitors of the cysteine protease cathepsin K.

Marquis RW, Ru Y, Zeng J, Trout RE, LoCastro SM, Gribble AD, Witherington J, Fenwick AE, Garnier B, Tomaszek T, Tew D, Hemling ME, Quinn CJ, Smith WW, Zhao B, McQueney MS, Janson CA, D'Alessio K, Veber DF. Marquis RW, et al. Among authors: tomaszek t. J Med Chem. 2001 Mar 1;44(5):725-36. doi: 10.1021/jm000320t. J Med Chem. 2001. PMID: 11262083

6

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: tomaszek t. Bone. 2007 Jan;40(1):122-31. doi: 10.1016/j.bone.2006.07.015. Epub 2006 Sep 7. Bone. 2007. PMID: 16962401

7

Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.

Marquis RW, Yamashita DS, Ru Y, LoCastro SM, Oh HJ, Erhard KF, DesJarlais RL, Head MS, Smith WW, Zhao B, Janson CA, Abdel-Meguid SS, Tomaszek TA, Levy MA, Veber DF. Marquis RW, et al. Among authors: tomaszek ta. J Med Chem. 1998 Sep 10;41(19):3563-7. doi: 10.1021/jm980295f. J Med Chem. 1998. PMID: 9733481 No abstract available.

8

Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic.

Thompson SK, Smith WW, Zhao B, Halbert SM, Tomaszek TA, Tew DG, Levy MA, Janson CA, DAlessio KJ, McQueney MS, Kurdyla J, Jones CS, DesJarlais RL, Abdel-Meguid SS, Veber DF. Thompson SK, et al. Among authors: tomaszek ta. J Med Chem. 1998 Oct 8;41(21):3923-7. doi: 10.1021/jm980474x. J Med Chem. 1998. PMID: 9767629

9

Use of papain as a model for the structure-based design of cathepsin K inhibitors: crystal structures of two papain-inhibitor complexes demonstrate binding to S'-subsites.

LaLonde JM, Zhao B, Smith WW, Janson CA, DesJarlais RL, Tomaszek TA, Carr TJ, Thompson SK, Oh HJ, Yamashita DS, Veber DF, Abdel-Meguid SS. LaLonde JM, et al. Among authors: tomaszek ta. J Med Chem. 1998 Nov 5;41(23):4567-76. doi: 10.1021/jm980249f. J Med Chem. 1998. PMID: 9804696

10

Potent dipeptidylketone inhibitors of the cysteine protease cathepsin K.

Marquis RW, Ru Y, Yamashita DS, Oh HJ, Yen J, Thompson SK, Carr TJ, Levy MA, Tomaszek TA, Ijames CF, Smith WW, Zhao B, Janson CA, Abdel-Meguid SS, D'Alessio KJ, McQueney MS, Veber DF. Marquis RW, et al. Among authors: tomaszek ta. Bioorg Med Chem. 1999 Apr;7(4):581-8. doi: 10.1016/s0968-0896(99)00011-5. Bioorg Med Chem. 1999. PMID: 10353637

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