Literature DB >> 18835710

Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.

Robert D Mazzola1, Zhaoning Zhu, Lisa Sinning, Brian McKittrick, Brian Lavey, James Spitler, Joseph Kozlowski, Shih Neng-Yang, Guowei Zhou, Zhuyan Guo, Peter Orth, Vincent Madison, Jing Sun, Daniel Lundell, Xiaoda Niu.   

Abstract

A series of cyclopropyl hydroxamic acids were prepared. Many of the compounds displayed picomolar affinity for the TACE enzyme while maintaining good to excellent selectivity profiles versus MMP-1, -2, -3, -7, -14, and ADAM-10. X-ray analysis of an inhibitor in the TACE active site indicated that the molecules bound to the enzyme in the S1'-S3' pocket.

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Year:  2008        PMID： 18835710     DOI： 10.1016/j.bmcl.2008.09.045

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


  9 in total

1.  Structure of human ADAM-8 catalytic domain complexed with batimastat.

Authors:  Troii Hall; Huey Sheng Shieh; Jacqueline E Day; Nicole Caspers; Jill E Chrencik; Jennifer M Williams; Lyle E Pegg; Adele M Pauley; Andrea F Moon; Joseph M Krahn; David H Fischer; James R Kiefer; Alfredo G Tomasselli; Marc D Zack
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2012-05-22

2.  A transforming Src mutant increases the bioavailability of EGFR ligands via stimulation of the cell-surface metalloproteinase ADAM17.

Authors:  T Maretzky; W Zhou; X-Y Huang; C P Blobel
Journal:  Oncogene       Date:  2010-09-27       Impact factor: 9.867

3.  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

4.  ADAM17 cleaves CD16b (FcγRIIIb) in human neutrophils.

Authors:  Yue Wang; Jianming Wu; Robert Newton; Nooshin S Bahaie; Chunmei Long; Bruce Walcheck
Journal:  Biochim Biophys Acta       Date:  2012-12-08

5.  ADAMs 10 and 17 represent differentially regulated components of a general shedding machinery for membrane proteins such as transforming growth factor alpha, L-selectin, and tumor necrosis factor alpha.

Authors:  Sylvain M Le Gall; Pierre Bobé; Karina Reiss; Keisuke Horiuchi; Xiao-Da Niu; Daniel Lundell; David R Gibb; Daniel Conrad; Paul Saftig; Carl P Blobel
Journal:  Mol Biol Cell       Date:  2009-01-21       Impact factor: 4.138

6.  Molecular Descriptors in Modelling the Tumour Necrosis Factor-α Converting Enzyme Inhibition Activity of Novel Tartrate-Based Analogues.

Authors:  P Singh
Journal:  Indian J Pharm Sci       Date:  2013-01       Impact factor: 0.975

7.  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

8.  Molecular basis for the mechanism of action of an anti-TACE antibody.

Authors:  Li Peng; Kimberly Cook; Linda Xu; Li Cheng; Melissa Damschroder; Changshou Gao; Herren Wu; William F Dall'Acqua
Journal:  MAbs       Date:  2016-09-09       Impact factor: 5.857

9.  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
  9 in total

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