(4-((2-Methylphenyl)aminocarbonyl)-aminophenyl)acetyl-Fibronectin CS-1 Fragment (1980-1983)

The VLA-4 inhibitor BIO-1211 based on the LDVP motif represents a selective, tight-binding inhibitor of integrin α₄β₁ achieved by appending an optimal organic group to the N-terminus of the peptide (Kd = 70 pM). Moreover, this inhibitor exhibited > 200-fold selectivity for the activated form of the integrin α₄β₁ receptor.