INHIBITION OF MATRIX METALLOPROTEINASES BY N-CARBOXYALKYL DIPEPTIDES - ENHANCED POTENCY AND SELECTIVITY WITH SUBSTITUTED P-1' HOMOPHENYLALANINES

Authors
SAHOO SP CALDWELL CG CHAPMAN KT DURETTE PL ESSER CK KOPKA IE POLO SA SPEROW KM NIEDZWIECKI LM IZQUIERDOMARTIN M CHANG BC HARRISON RK STEIN RL MACCOSS M HAGMANN WK
Citation
Sp. Sahoo et al., INHIBITION OF MATRIX METALLOPROTEINASES BY N-CARBOXYALKYL DIPEPTIDES - ENHANCED POTENCY AND SELECTIVITY WITH SUBSTITUTED P-1' HOMOPHENYLALANINES, Bioorganic & medicinal chemistry letters, 5(20), 1995, pp. 2441-2446
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
20
Year of publication
1995
Pages
2441 - 2446
Database
ISI
SICI code
0960-894X(1995)5:20<2441:IOMMBN>2.0.ZU;2-C
Abstract
A series of N-carboxyalkyl dipeptides were synthesized to evaluate the ir inhibitory activities against human stromelysin-1(MMP-3), collagena se(MMP-1), and gelatinase A(MMP-2). Structures with a homophenylalanin e residue at P-1' substituted at the para position with small alkyl gr oups are potent inhibitors of (MMP-3) and (MMP-2) (K-i' s 2-40 nM), bu t weak inhibitors of (MMP-1).