Literature DB >> 19054672

Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.

Zhuyan Guo1, Peter Orth, Shing-Chun Wong, Brian J Lavey, Neng-Yang Shih, Xiaoda Niu, Daniel J Lundell, Vincent Madison, Joseph A Kozlowski.   

Abstract

We have discovered nanomolar inhibitors of TNF-alpha convertase (TACE) comprised of a novel spirocyclic scaffold and either a carboxylate or hydroxamate zinc binding moiety. X-ray crystal structures and computer models of selected compounds binding to TACE explain the observed SAR. We report the first TACE X-ray crystal structure for an inhibitor with a carboxylate zinc ligand.

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Year:  2008        PMID： 19054672     DOI： 10.1016/j.bmcl.2008.11.034

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


  4 in total

Review 1.  Targeting Metalloenzymes for Therapeutic Intervention.

Authors:  Allie Y Chen; Rebecca N Adamek; Benjamin L Dick; Cy V Credille; Christine N Morrison; Seth M Cohen
Journal:  Chem Rev       Date:  2018-09-07       Impact factor: 60.622

2.  Simultaneous detection of multiple proteases using a non-array nanopore platform.

Authors:  Xiaohan Chen; Youwen Zhang; Xiyun Guan
Journal:  Nanoscale       Date:  2021-08-03       Impact factor: 8.307

3.  In Silico and Experimental ADAM17 Kinetic Modeling as Basis for Future Screening System for Modulators.

Authors:  Marian Bienstein; Dmitriy Minond; Ulrich Schwaneberg; Mehdi D Davari; Daniela Yildiz
Journal:  Int J Mol Sci       Date:  2022-01-25       Impact factor: 5.923

4.  Vitamin D3 Prevents the Deleterious Effects of Testicular Torsion on Testis by Targeting miRNA-145 and ADAM17: In Silico and In Vivo Study.

Authors:  Doaa I Mohamed; Doaa A Abou-Bakr; Samar F Ezzat; Hanaa F Abd El-Kareem; Hebatallah H Abo Nahas; Hosam A Saad; Amir E Mehana; Essa M Saied
Journal:  Pharmaceuticals (Basel)       Date:  2021-11-25
  4 in total

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