425403-78-7Relevant articles and documents
Specific and dual antagonists of α4β1 and α4β7 integrins
Lin, Linus S.,Lanza Jr., Thomas,McCauley, Ermenegilda,Riper, Gail Van,Kidambi, Usha,Cao, Jin,Egger, Linda A.,Mumford, Richard A.,Schmidt, John A.,MacCoss, Malcolm,Hagmann, William K.
, p. 133 - 136 (2007/10/03)
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.