The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic

被引：22

作者：

Fotouhi, N ^{[1
]}

Joshi, P ^{[1
]}

Fry, D ^{[1
]}

Cook, C ^{[1
]}

Tilley, JW ^{[1
]}

Kaplan, G ^{[1
]}

Hanglow, A ^{[1
]}

Rowan, K ^{[1
]}

Schwinge, V ^{[1
]}

Wolitzky, B ^{[1
]}

机构：

[1] Hoffmann La Roche Inc, Roche Res Ctr, Nutley, NJ 07110 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(00)00174-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The Asp-Pro sequence of the cyclic peptide Ac-HN-Tyr-Cys*-Asp-Pro-Cys*-OH (1) could be replaced with the achiral dipeptide mimetic 1-(2-aminoethyl)cyclpentylcarboxylic acid with retention of potent inhibition of the VCAM-VLA-4 interaction. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1171 / 1173

页数：3

共 7 条

[1] CHEN L, 1999, Patent No. 10312
[2] ELICES M, 1999, CURR OPIN ANTIINFLAM, V1, P14
[3] ELICES MJ, 1998, CELL ADHESION MOL MA, P133
[4] Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents
Jackson, DY
Quan, C
Artis, DR
Rawson, T
Blackburn, B
Struble, M
Fitzgerald, G
Chan, K
Mullins, S
Burnier, JP
Fairbrother, WJ
Clark, K
Berisini, M
Chui, H
Renz, M
Jones, S
Fong, S
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (21) : 3359 - 3368
[5] Very late antigen 4 (VLA4) antagonists as anti-inflammatory agents
Lin, KC
Castro, AC
[J]. CURRENT OPINION IN CHEMICAL BIOLOGY, 1998, 2 (04) : 453 - 457
[6] Selective, tight-binding inhibitors of integrin α4β1 that inhibit allergic airway responses
Lin, KC
Ateeq, HS
Hsiung, SH
Chong, LT
Zimmerman, CN
Castro, A
Lee, WC
Hammond, CE
Kalkunte, S
Chen, LL
Pepinsky, RB
Leone, DR
Sprague, AG
Abraham, WM
Gill, A
Lobb, RR
Adams, SP
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (05) : 920 - 934
[7] LOBL TJ, 1992, Patent No. 00995

← 1 →