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Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs).

Abstract：

:N-arylsulfonyl-based MMPs inhibitors (MMPIs) are among the most prominent inhibitors possessing nanomolar affinity. However, their poor bioavailability remains critical for the drug development of this family of molecules. The structural analysis of the complex of NNGH (the most representative member of the family) with MMP-12 provided us with the basis to effectively design simple NNGH analogues with enhanced solubility in water. Following this approach, the sec-butyl residue, not directly involved in the binding with MMP, has been replaced with hydrophilic residues thus yielding new potent inhibitors soluble in water.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Attolino E,Calderone V,Dragoni E,Fragai M,Richichi B,Luchinat C,Nativi C

doi

10.1016/j.ejmech.2010.09.057

subject

Has Abstract

pub_date

2010-12-01 00:00:00

pages

5919-25

issue

12

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(10)00724-5

journal_volume

45

pub_type

杂志文章

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