Literature DB >> 17064892

Identification of potent and selective TACE inhibitors via the S1 pocket.

Jeffrey S Condon1, Diane Joseph-McCarthy, Jeremy I Levin, Henry-Georges Lombart, Frank E Lovering, Linhong Sun, Weiheng Wang, Weixin Xu, Yuhua Zhang.   

Abstract

By focusing on the P1 portion of the piperidine beta-sulfone ligands we identified a motif that induces selectivity and resulted in a series of TACE inhibitors that demonstrated excellent in vitro potency against isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and 14.

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Year:  2006        PMID: 17064892     DOI: 10.1016/j.bmcl.2006.10.004

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


  7 in total

1.  Anthranilate derivatives as TACE inhibitors: docking based CoMFA and CoMSIA analyses.

Authors:  Malkeet Singh Bahia; Shravan Kumar Gunda; Shwetha Reddy Gade; Saikh Mahmood; Ravikumar Muttineni; Om Silakari
Journal:  J Mol Model       Date:  2010-03-28       Impact factor: 1.810

2.  A novel inhibitor of ADAM17 sensitizes colorectal cancer cells to 5-Fluorouracil by reversing Notch and epithelial-mesenchymal transition in vitro and in vivo.

Authors:  Dan-Dan Li; Chang-Hao Zhao; Huai-Wei Ding; Qiong Wu; Tian-Shu Ren; Jian Wang; Cong-Qin Chen; Qing-Chun Zhao
Journal:  Cell Prolif       Date:  2018-08-02       Impact factor: 6.831

3.  Novel drug-target interactions via link prediction and network embedding.

Authors:  E Amiri Souri; R Laddach; S N Karagiannis; L G Papageorgiou; S Tsoka
Journal:  BMC Bioinformatics       Date:  2022-04-04       Impact factor: 3.169

4.  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

5.  Isoxazolium N-ylides and 1-oxa-5-azahexa-1,3,5-trienes on the way from isoxazoles to 2H-1,3-oxazines.

Authors:  Alexander F Khlebnikov; Mikhail S Novikov; Yelizaveta G Gorbunova; Ekaterina E Galenko; Kirill I Mikhailov; Viktoriia V Pakalnis; Margarita S Avdontceva
Journal:  Beilstein J Org Chem       Date:  2014-08-14       Impact factor: 2.883

Review 6.  The ADAM metalloproteinases.

Authors:  Dylan R Edwards; Madeleine M Handsley; Caroline J Pennington
Journal:  Mol Aspects Med       Date:  2008-08-15

7.  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
  7 in total

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