Discovery and evaluation of potent, tyrosine-based α4β1 integrin antagonists

被引：24

作者：

Archibald, SC

Head, JC

Gozzard, N

Howat, DW

Parton, TAH

Porter, JR

Robinson, MK

Shock, A

Warrellow, GJ

Abraham, WM

机构：

[1] Celltech Chirosci, Slough SL1 4EN, Berks, England

[2] Mt Sinai Med Ctr, Miami Beach, FL 33140 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(00)00147-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using disulphide cysteine-based inhibitors as lead structures, this communication describes our strategy for identifying more stable, potent antagonists of the alpha 4 beta 1 integrin. These studies ultimately discovered potent, low molecular weight inhibitors based on D-thioproline-L-tyrosine. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：997 / 999

页数：3

共 7 条

[1] ALPHA(4)-INTEGRINS MEDIATE ANTIGEN-INDUCED LATE BRONCHIAL RESPONSES AND PROLONGED AIRWAY HYPERRESPONSIVENESS IN SHEEP [J].

ABRAHAM, WM ;

SIELCZAK, MW ;

AHMED, A ;

CORTES, A ;

LAUREDO, IT ;

KIM, J ;

PEPINSKY, B ;

BENJAMIN, CD ;

LEONE, DR ;

LOBB, RR ;

WELLER, PF .

JOURNAL OF CLINICAL INVESTIGATION, 1994, 93 (02) :776-787

[2]

ABRAHAM WM, 1994, AM J RESP CRIT CARE, V156, P776

[3] Discovery and evaluation of potent, cysteine-based α4βl integrin antagonists [J].

Archibald, SC ;

Head, JC ;

Linsley, JM ;

Porter, JR ;

Robinson, MK ;

Shock, A ;

Warrellow, GJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (09) :993-995

[4]

BOCHNER BS, 1998, CELL ADHESION MOL MA, P113

[5]

ELICES MJ, 1998, CELL ADHESION MOL MA, P133

[6]

LOBB M, 1999, EXPERT OPIN INV DRUG, V8, P935

[7] Peptide and peptidomimetic inhibitors of VLA-4 [J].

Zimmerman, CN .

EXPERT OPINION ON THERAPEUTIC PATENTS, 1999, 9 (02) :129-133

← 1 →