Novel modified tripeptide inhibitors of α4β7 mediated lymphoid cell adhesion to MAdCAM-1

Abstract MAdCAM-1 specifically binds the lymphocyte integrin α 4 β 7 and 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/ α 4 β 7 interactions. N-Terminus acylation of the LDT motif and modification of the C-terminus carboxamide with amines led to low micromolar MAdCAM-1 inhibitors.