A potent dipeptide inhibitor of dipeptidyl peptidase IV

被引：14

作者：

Yamada, M ^{[1
]}

Okagaki, C ^{[1
]}

Higashijima, T ^{[1
]}

Tanaka, S ^{[1
]}

Ohnuki, T ^{[1
]}

Sugita, T ^{[1
]}

机构：

[1] Tanabe Seiyaku Co Ltd, Lead Generat Res Lab, Yodogawa Ku, Osaka 5328505, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 12期

关键词：

antiinflammatories; enzyme inhibitor; immunological activity; peptides and polypeptides;

D O I：

10.1016/S0960-894X(98)00259-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel potent inhibitors of dipeptidyl peptidase IV (DPP-IV) has been developed. A brief structure-activity relationship of the inhibitors was investigated. The dipeptide TSL-225, tryptophyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, was identified with the critical structure for the inhibitory activity. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1537 / 1540

页数：4

共 26 条

[1]

ASAI Y, 1997, ANTIBIOTICS, V50, P653

[2] 4-cyanothiazolidides as very potent, stable inhibitors of dipeptidyl peptidase IV [J].

Ashworth, DM ;

Atrash, B ;

Baker, GR ;

Baxter, AJ ;

Jenkins, PD ;

Jones, DM ;

Szelke, M .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (22) :2745-2748

[3] Pyrrolidides: Synthesis and structure-activity relationship as inhibitors of dipeptidyl peptidase IV [J].

Augustyns, KJL ;

Lambeir, AM ;

Borloo, M ;

DeMeester, I ;

Vedernikova, I ;

Vanhoof, G ;

Hendriks, D ;

Scharpe, S ;

Haemers, A .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1997, 32 (04) :301-309

[4] DIPEPTIDE PHOSPHONATES AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-IV [J].

BODUSZEK, B ;

OLEKSYSZYN, J ;

KAM, CM ;

SELZLER, J ;

SMITH, RE ;

POWERS, JC .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (23) :3969-3976

[5]

Demuth H U, 1988, J Enzyme Inhib, V2, P129, DOI 10.3109/14756368809040718

[6] CD26 - A SURFACE PROTEASE INVOLVED IN T-CELL ACTIVATION [J].

FLEISCHER, B .

IMMUNOLOGY TODAY, 1994, 15 (04) :180-184

[7] INHIBITION OF DIPEPTIDYL AMINOPEPTIDASE-IV (DP-IV) BY XAA-BOROPRO DIPEPTIDES AND USE OF THESE INHIBITORS TO EXAMINE THE ROLE OF DP-IV IN T-CELL FUNCTION [J].

FLENTKE, GR ;

MUNOZ, E ;

HUBER, BT ;

PLAUT, AG ;

KETTNER, CA ;

BACHOVCHIN, WW .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1991, 88 (04) :1556-1559

[8] DIPEPTIDYLPEPTIDASE-IV AND TRYPSIN-LIKE ENZYMATIC DEGRADATION OF HUMAN GROWTH-HORMONE RELEASING HORMONE IN PLASMA [J].

FROHMAN, LA ;

DOWNS, TR ;

HEIMER, EP ;

FELIX, AM .

JOURNAL OF CLINICAL INVESTIGATION, 1989, 83 (05) :1533-1540

[9] RAPID ENZYMATIC DEGRADATION OF GROWTH-HORMONE RELEASING HORMONE BY PLASMA INVITRO AND INVIVO TO A BIOLOGICALLY INACTIVE PRODUCT CLEAVED AT THE NH2 TERMINUS [J].

FROHMAN, LA ;

DOWNS, TR ;

WILLIAMS, TC ;

HEIMER, EP ;

PAN, YCE ;

FELIX, AM .

JOURNAL OF CLINICAL INVESTIGATION, 1986, 78 (04) :906-913

[10] APPLICATIONS OF COMBINATORIAL TECHNOLOGIES TO DRUG DISCOVERY .1. BACKGROUND AND PEPTIDE COMBINATORIAL LIBRARIES [J].

GALLOP, MA ;

BARRETT, RW ;

DOWER, WJ ;

FODOR, SPA ;

GORDON, EM .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (09) :1233-1251

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