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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Bianchini G,Aschi M,Cavicchio G,Crucianelli M,Preziuso S,Gallina C,Nastari A,Gavuzzo E,Mazza F

doi

10.1016/j.bmc.2005.04.079

subject

Has Abstract

pub_date

2005-08-01 00:00:00

pages

4740-9

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00390-1

journal_volume

13

pub_type

杂志文章

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