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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Preliminary In vitro Results Indicating Tartronic Acids as Aspartic Acid Mimetics in Vitronectin Receptor Antagonists: Evidence for Increased Hydroxyapatite Affinity

Author(s): Diane B. Hauze, Kenneth L. Kees, Charles W. Mann, Horace Fletcher III, Richard Murrills, Jeanne Matteo, Frederick Bex, Bheem Bhat and Valerie Coleburn

Volume 2, Issue 3, 2005

Page: [201 - 204] Pages: 4

DOI: 10.2174/1570180053765110

Price: $65

Abstract

A series of tartronic acid analogs of a non-peptide RGD mimetic were prepared and evaluated both for antagonism of the vitronectin receptor and for affinity to hydroxyapatite, the main inorganic component of bone matrix. The hydroxy bis acid unit was found to be optimal for both receptor binding and hydroxyapatite affinity, while the N-terminus affected only receptor binding affinity.

Keywords: Arginine-Glycine-Aspartic Acid (rgd), vitronectin receptor, osteoporosis, tetracycline, aminotriazole, palladium-catalyzed coupling reactions, hydroxyapatite


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