Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


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, Valerie Coleburn.


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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Article Details

Year: 2005
Page: [201 - 204]
Pages: 4
DOI: 10.2174/1570180053765110
Price: $58