INHIBITION OF STROMELYSIN-1 (MMP-3) BY PEPTIDYL PHOSPHINIC ACIDS

被引：32

作者：

GOULET, JL ^{[1
]}

KINNEARY, JF ^{[1
]}

DURETTE, PL ^{[1
]}

STEIN, RL ^{[1
]}

HARRISON, RK ^{[1
]}

IZQUIERDOMARTIN, M ^{[1
]}

KUO, DW ^{[1
]}

LIN, TY ^{[1
]}

HAGMANN, WK ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD,DEPT ENZYMOL,RAHWAY,NJ 07065

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(01)80334-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of phosphinic acid-containing peptide inhibitors of human stromelysin-1 (MMP-3) were prepared. The P1 through P3 subsites were varied in a systematic manner on analogs possessing an invariant P1'-P3' segment. The in vitro activity of these compounds as inhibitors of stromelysin and collagenase is discussed.

引用

页码：1221 / 1224

页数：4

共 15 条

[1] 1-AMINOALKYLPHOSPHONOUS ACIDS .1. ISOSTERES OF THE PROTEIN AMINO-ACIDS [J].

BAYLIS, EK ;

CAMPBELL, CD ;

DINGWALL, JG .

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1984, (12) :2845-2853

[2]

BROADHURST MJ, 1987, Patent No. 276436

[3] INHIBITION OF MATRIX METALLOPROTEINASES BY N-CARBOXYALKYL PEPTIDES [J].

CHAPMAN, KT ;

KOPKA, IE ;

DURETTE, PL ;

ESSER, CK ;

LANZA, TJ ;

IZQUIERDOMARTIN, M ;

NIEDZWIECKI, L ;

CHANG, B ;

HARRISON, RK ;

KUO, DW ;

LIN, TY ;

STEIN, RL ;

HAGMANN, WK .

JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (26) :4293-4301

[4] A CONVENIENT SYNTHESIS OF AMINOMETHYLPHOSPHONOUS ACID [J].

GROBELNY, D .

SYNTHETIC COMMUNICATIONS, 1989, 19 (7-8) :1177-1180

[5] THE ROLE OF STROMELYSIN IN THE CARTILAGE DESTRUCTION THAT ACCOMPANIES INFLAMMATORY ARTHRITIS [J].

HASTY, KA ;

REIFE, RA ;

KANG, AH ;

STUART, JM .

ARTHRITIS AND RHEUMATISM, 1990, 33 (03) :388-397

[6] ANGIOTENSIN-CONVERTING ENZYME-INHIBITORS - MERCAPTAN, CARBOXYALKYL DIPEPTIDE, AND PHOSPHINIC ACID INHIBITORS INCORPORATING 4-SUBSTITUTED PROLINES [J].

KRAPCHO, J ;

TURK, C ;

CUSHMAN, DW ;

POWELL, JR ;

DEFORREST, JM ;

SPITZMILLER, ER ;

KARANEWSKY, DS ;

DUGGAN, M ;

ROVNYAK, G ;

SCHWARTZ, J ;

NATARAJAN, S ;

GODFREY, JD ;

RYONO, DE ;

NEUBECK, R ;

ATWAL, KS ;

PETRILLO, EW .

JOURNAL OF MEDICINAL CHEMISTRY, 1988, 31 (06) :1148-1160

[7] SUBSTRATE-SPECIFICITY OF THE HUMAN MATRIX METALLOPROTEINASE STROMELYSIN AND THE DEVELOPMENT OF CONTINUOUS FLUOROMETRIC ASSAYS [J].

NIEDZWIECKI, L ;

TEAHAN, J ;

HARRISON, RK ;

STEIN, RL .

BIOCHEMISTRY, 1992, 31 (50) :12618-12623

[8]

OKADA Y, 1987, J RHEUMATOL, V14, P41

[9]

OKADA Y, 1992, LAB INVEST, V66, P680

[10]

OKADA Y, 1986, J BIOL CHEM, V261, P14245

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