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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Yin H,Gerlach LO,Miller MW,Moore DT,Liu D,Vilaire G,Bennett JS,DeGrado WF

doi

10.1016/j.bmcl.2006.04.037

subject

Has Abstract

pub_date

2006-07-01 00:00:00

pages

3380-2

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)00432-X

journal_volume

16

pub_type

杂志文章

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