Title of article
Arylamide derivatives as allosteric inhibitors of the integrin α2β1/type I collagen interaction
Author/Authors
Hang-Yin Ling، نويسنده , , Lars-Ole Gerlach، نويسنده , , Meredith W. Miller، نويسنده , , David T. Moore، نويسنده , , Dahui Liu، نويسنده , , Gaston Vilaire، نويسنده , , Joel S. Bennett، نويسنده , , William F. DeGrado، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
3
From page
3380
To page
3382
Abstract
We herein report a group of allosteric inhibitors of integrin α2β1 based on an arylamide scaffold. Compound 4 showed an IC50 of 4.80 μM in disrupting integrin I-domain/collagen binding in an ELISA. These arylamide compounds are able to block collagen binding to integrin α2β1 on the platelet surface. Further we find that compound 4 recognizes a hydrophobic cleft on the side of the α2 I-domain, suggesting an alternative targeting site for drug development.
Keywords
Allosteric inhibitor , Protein–protein interaction , platelet adhesion , integrin
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796994
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