INHIBITION OF MATRIX METALLOPROTEINASES BY N-CARBOXYALKYL PEPTIDES CONTAINING EXTENDED ALKYL RESIDUES AT P-1

被引:15
作者
ESSER, CK [1 ]
KOPKA, IE [1 ]
DURETTE, PL [1 ]
HARRISON, RK [1 ]
NIEDZWIECKI, LM [1 ]
IZQUIERDOMARTIN, M [1 ]
STEIN, RL [1 ]
HAGMANN, WK [1 ]
机构
[1] MERCK & CO INC,RES LABS,DEPT ENZYMOL,RAHWAY,NJ 07065
关键词
D O I
10.1016/0960-894X(95)00079-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of N-carboxyalkyl peptides were prepared to test their inhibitory activity against human stromelysin (MMP-3), collagenase (MMP-1), and gelatinase A (MMP-2). Linear alkyl and omega-aminoalkyl residues were employed as replacements for a phenethyl group yielding inhibitors with in vitro activities comparable to their corresponding aromatic analogs.
引用
收藏
页码:539 / 542
页数:4
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