Literature DB >> 15935680

Design, modelling, synthesis and biological evaluation of peptidomimetic phosphinates as inhibitors of matrix metalloproteinases MMP-2 and MMP-8.

Gianluca Bianchini1, Massimiliano Aschi, Giancarlo Cavicchio, Marcello Crucianelli, Serena Preziuso, Carlo Gallina, Adele Nastari, Enrico Gavuzzo, Fernando Mazza.   

Abstract

Three novel peptidomimetic phosphinate inhibitors have been synthesized and evaluated as inhibitors of matrix metalloproteinases MMP-2 and MMP-8. Their IC50 values are in the micromolar range, and one of them showed to be the most effective inhibitor of MMP-2. The differences in binding affinities for MMP-2 and MMP-8 of the three phosphinates have been rationalized by means of modelling studies and molecular dynamics simulations.

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Year:  2005        PMID: 15935680     DOI: 10.1016/j.bmc.2005.04.079

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  7 in total

1.  Triple-helical transition state analogues: a new class of selective matrix metalloproteinase inhibitors.

Authors:  Janelle Lauer-Fields; Keith Brew; John K Whitehead; Shunzi Li; Robert P Hammer; Gregg B Fields
Journal:  J Am Chem Soc       Date:  2007-08-02       Impact factor: 15.419

2.  Combined structure- and ligand-based pharmacophore modeling and molecular dynamics simulation studies to identify selective inhibitors of MMP-8.

Authors:  Sukesh Kalva; D Vinod; Lilly M Saleena
Journal:  J Mol Model       Date:  2014-04-23       Impact factor: 1.810

3.  Borane Complexes of the H(3)PO(2) P(III) Tautomer: Useful Phosphinate Equivalents.

Authors:  Yamina Belabassi; Monika I Antczak; Jennifer Tellez; Jean-Luc Montchamp
Journal:  Tetrahedron       Date:  2008-09-22       Impact factor: 2.457

4.  Synthesis, cytotoxicity, DNA binding and apoptosis of rhein-phosphonate derivatives as antitumor agents.

Authors:  Man-Yi Ye; Gui-Yang Yao; Jing-Chen Wei; Ying-Ming Pan; Zhi-Xin Liao; Heng-Shan Wang
Journal:  Int J Mol Sci       Date:  2013-04-29       Impact factor: 5.923

5.  Selectively fluorinated cyclohexane building blocks: Derivatives of carbonylated all-cis-3-phenyl-1,2,4,5-tetrafluorocyclohexane.

Authors:  Mohammed Salah Ayoup; David B Cordes; Alexandra M Z Slawin; David O'Hagan
Journal:  Beilstein J Org Chem       Date:  2015-12-21       Impact factor: 2.883

Review 6.  The Rebirth of Matrix Metalloproteinase Inhibitors: Moving Beyond the Dogma.

Authors:  Gregg B Fields
Journal:  Cells       Date:  2019-08-27       Impact factor: 6.600

7.  Discovery of Sulfated Small Molecule Inhibitors of Matrix Metalloproteinase-8.

Authors:  Shravan Morla; Umesh R Desai
Journal:  Biomolecules       Date:  2020-08-09
  7 in total

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