Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study

Vassiliou, Stamatia, Mucha, Artur, Cuniasse, Philippe, Georgiadis, Dimitris, Lucet-Levannier, Karine, Beau, Fabrice, Kannan, Rama, Murphy, Gillian, Knauper, Vera ORCID: https://orcid.org/0000-0002-3965-9924, Rio, Marie-Christine, Basset, Paul, Yiotakis, Athanasios and Dive, Vincent 1999. Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study. Journal of Medicinal Chemistry 42 (14) , pp. 2610-2620. 10.1021/jm9900164

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Abstract

Several phosphinic pseudo-tripeptides of general formula R-XaaΨ(PO2-CH2)Xaa‘-Yaa‘-NH2 were synthesized and evaluated for their in vitro activities to inhibit stromelysin-3, gelatinases A and B, membrane type-1 matrix metalloproteinase, collagenases 1 and 2, and matrilysin. With the exception of collagenase-1 and matrilysin, phosphinic pseudo-tripeptides behave as highly potent inhibitors of matrix metalloproteinases, provided they contain in P1‘ position an unusual long aryl−alkyl substituent. Study of structure−activity relationships regarding the influence of the R and Xaa‘ substituents in this series may contribute to the design of inhibitors able to block only a few members of the matrix metalloproteinase family.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Dentistry
Publisher:	American Chemical Society
ISSN:	0022-2623
Last Modified:	11 Sep 2023 08:42
URI:	https://orca.cardiff.ac.uk/id/eprint/161648

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