Literature DB >> 14684342

Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.

John G Catalano1, David N Deaton, Eric S Furfine, Annie M Hassell, Robert B McFadyen, Aaron B Miller, Larry R Miller, Lisa M Shewchuk, Derril H Willard, Lois L Wright.   

Abstract

The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM.

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Year:  2004        PMID: 14684342     DOI: 10.1016/j.bmcl.2003.09.088

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

1.  Calpain 10 homology modeling with CYGAK and increased lipophilicity leads to greater potency and efficacy in cells.

Authors:  Matthew A Smith; Campbell McInnes; Ryan M Whitaker; Christopher C Lindsey; Richard F Comer; Craig C Beeson; Rick G Schnellmann
Journal:  ACS Chem Biol       Date:  2012-05-31       Impact factor: 5.100

2.  The crystal structure of human dipeptidyl peptidase I (cathepsin C) in complex with the inhibitor Gly-Phe-CHN2.

Authors:  Anne Mølgaard; Jose Arnau; Conni Lauritzen; Sine Larsen; Gitte Petersen; John Pedersen
Journal:  Biochem J       Date:  2007-02-01       Impact factor: 3.857

3.  Limitations of SLLVY-AMC in calpain and proteasome measurements.

Authors:  Christopher J Giguere; Rick G Schnellmann
Journal:  Biochem Biophys Res Commun       Date:  2008-05-05       Impact factor: 3.575

Review 4.  Cathepsin K inhibitors for osteoporosis and potential off-target effects.

Authors:  Dieter Brömme; Fabien Lecaille
Journal:  Expert Opin Investig Drugs       Date:  2009-05       Impact factor: 6.206

5.  Total synthesis of (-)-aplaminal.

Authors:  Amos B Smith; Zhuqing Liu
Journal:  Org Lett       Date:  2008-08-28       Impact factor: 6.005

6.  Molecular dynamics simulations of the catalytic pathway of a cysteine protease: a combined QM/MM study of human cathepsin K.

Authors:  Shuhua Ma; Lakshmi S Devi-Kesavan; Jiali Gao
Journal:  J Am Chem Soc       Date:  2007-10-13       Impact factor: 15.419

7.  A modeling study of aldehyde inhibitors of human cathepsin K using partial least squares method.

Authors:  M Shahlaei; A Fassihi; L Saghaie; E Arkan; A Pourhossein
Journal:  Res Pharm Sci       Date:  2011-07
  7 in total

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