title: Arylamide derivatives as allosteric inhibitors of the integrin alpha2beta1/type I collagen interaction.
abstract: We herein report a group of allosteric inhibitors of integrin alpha(2)beta(1) based on an arylamide scaffold. Compound 4 showed an IC(50) of 4.80 microM in disrupting integrin I-domain/collagen binding in an ELISA. These arylamide compounds are able to block collagen binding to integrin alpha(2)beta(1) on the platelet surface. Further we find that compound 4 recognizes a hydrophobic cleft on the side of the alpha(2) I-domain, suggesting an alternative targeting site for drug development.
authors: Department of Biochemistry and Biophysics, University of Pennsylvania School of Medicine, Philadelphia, 19104, USA.
authors: Hang
authors: H
authors: Yin
authors: Lars Ole
authors: LO
authors: Gerlach
authors: Meredith W
authors: MW
authors: Miller
authors: David T
authors: DT
authors: Moore
authors: Dahui
authors: D
authors: Liu
authors: Gaston
authors: G
authors: Vilaire
authors: Joel S
authors: JS
authors: Bennett
authors: William F
authors: WF
authors: DeGrado