Identification of novel matrix metalloproteinase inhibitors by screening of phenol fragments library

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Abstract

In the last 20 years, a great variety of synthetic, low molecular weight MMP inhibitors (MMPIs) have been synthesized and tested, although none has reached clinical utility. Exploration of novel ZBGs and development of non-hydroxamate MMPI has become a focus in current research. It's well-known that polyphenols can produce beneficial effects on human health by their antioxidant properties as well as they have the ability to block gelatinase activity. In this work we tested a series of selected phenols as MMP inhibitors. The most interesting hit (B6) shows sub-micromolar activity against MMP-2 (IC(50) 0.59 +/- 0.05 microM, LE = 1.07) and a fairly good selectivity spectrum.

Autore Pugliese

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  • LAGHEZZA A.;LOIODICE F.;TORTORELLA P.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2011

ISSN

0365-6233

ISBN

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Numero di citazioni Wos

12

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

12

Ultimo Aggiornamento Citazioni

Non Disponibile

Settori ERC

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Codici ASJC

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