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

Diane   B.   Hauze; Kenneth   L.   Kees; Charles   W.   Mann; Horace      Fletcher III; Richard      Murrills; Jeanne      Matteo; Frederick      Bex; Bheem      Bhat; Valerie      Coleburn

doi:10.2174/1570180053765110

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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Letters in Drug Design & Discovery

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

Volume: 2 Issue: 3

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

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

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.

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Hauze B. Diane, Kees L. Kenneth, Mann W. Charles, Fletcher III Horace, Murrills Richard, Matteo Jeanne, Bex Frederick, Bhat Bheem and Coleburn Valerie, Preliminary In vitro Results Indicating Tartronic Acids as Aspartic Acid Mimetics in Vitronectin Receptor Antagonists: Evidence for Increased Hydroxyapatite Affinity, Letters in Drug Design & Discovery 2005; 2 (3) . https://dx.doi.org/10.2174/1570180053765110