Literature DB >> 15177446

Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.

Eric E Boros1, David N Deaton, Anne M Hassell, Robert B McFadyen, Aaron B Miller, Larry R Miller, Margot G Paulick, Lisa M Shewchuk, James B Thompson, 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 S2 and S3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P2 and P3 positions afforded analogs with cathepsin K IC50s between 600 nM and 130 pM.

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Year:  2004        PMID： 15177446     DOI： 10.1016/j.bmcl.2004.04.084

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


  4 in total

1.  New Peptidomimetic Boronates for Selective Inhibition of the Chymotrypsin-like Activity of the 26S Proteasome.

Authors:  Xiaozhou Zhang; Alaknanda Adwal; Andrew G Turner; David F Callen; Andrew D Abell
Journal:  ACS Med Chem Lett       Date:  2016-09-13       Impact factor: 4.345

2.  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

3.  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

Review 4.  Advances in the discovery of cathepsin K inhibitors on bone resorption.

Authors:  Jun Lu; Maolin Wang; Ziyue Wang; Zhongqi Fu; Aiping Lu; Ge Zhang
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051
  4 in total

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