NOVEL MODIFIED TRIPEPTIDE INHIBITORS OF ALPHA(4)BETA(7) MEDIATED LYMPHOID-CELL ADHESION TO MADCAM-1

Authors
SHROFF HN SCHWENDER CF BAXTER AD BROOKFIELD F PAYNE LJ COCHRAN NA GALLANT DL BRISKIN MJ
Citation
Hn. Shroff et al., NOVEL MODIFIED TRIPEPTIDE INHIBITORS OF ALPHA(4)BETA(7) MEDIATED LYMPHOID-CELL ADHESION TO MADCAM-1, Bioorganic & medicinal chemistry letters, 8(13), 1998, pp. 1601-1606
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
13
Year of publication
1998
Pages
1601 - 1606
Database
ISI
SICI code
0960-894X(1998)8:13<1601:NMTIOA>2.0.ZU;2-6
Abstract
MAdCAM-1 specifically binds the lymphocyte integrin alpha(4)beta(7) an d participates in the homing of leukocytes to intestinal mucosal sites . The LDT sequence located on the CD loop of MAdCAM-1 is an important binding site for MAdCAM-1/alpha(4)beta(7) interactions. N-Terminus acy lation of the LDT motif and modification of the C-terminus carboxamide with amines led to low micromolar MAdCAM-1 inhibitors. (C) 1998 Elsev ier Science Ltd. All rights reserved.