Author/Authors :
Linus S. Lin، نويسنده , , Thomas Lanza Jr.، نويسنده , , Ermenegilda McCauley، نويسنده , , Gail Van Riper، نويسنده , , Usha Kidambi، نويسنده , , Jin Cao، نويسنده , , Linda A. Egger، نويسنده , , Richard A. Mumford، نويسنده , , John A. Schmidt، نويسنده , , Malcolm MacCoss، نويسنده , , William K. Hagmann، نويسنده ,
Abstract :
N-(3,5-Dichlorophenylsulfonyl)-(R)-thioprolyl biarylalanine 10a has been identified as a potent and specific antagonist of the α4β1 integrin. Altering the configuration of thioproline from R to S led to a series of dual antagonists of α4β1 and α4β7, and the N-acetyl analogue 8b was found to be the most potent dual antagonist. A binding site model for α4β1 and α4β7 is proposed to explain the structure–activity relationship.
