Reference : Novel RGD-like molecules based on the tyrosine template design, synthesis, and biolog...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
Physical, chemical, mathematical & earth Sciences : Chemistry
Life sciences : Biochemistry, biophysics & molecular biology
http://hdl.handle.net/2268/28936
Novel RGD-like molecules based on the tyrosine template design, synthesis, and biological evaluation on isolated integrins alpha(V)beta/alpha(IIb)beta(3) and in cellular adhesion tests
English
Biltresse, S. [> > > >]
Attolini, M. [> > > >]
Dive, Georges [Université de Liège - ULiège > > Centre d'ingénierie des protéines >]
Cordi, A. [> > > >]
Tucker, G. C. [> > > >]
Marchand-Brynaert, J. [> > > >]
15-Oct-2004
Bioorganic and Medicinal Chemistry
Pergamon-Elsevier Science Ltd
12
20
5379-5393
Yes (verified by ORBi)
International
0968-0896
Oxford
[en] RGD peptidomimetic ; tyrosine template ; integrin alpha(V)beta(3) ; integrin alpha(IIb)beta(3) ; cell adhesion
[en] RGD (Arg-Gly-Asp) peptidomimetics have been designed for covalent anchorage on biomaterials. The tyrosine template was thus equipped with (i) a basic side chain of various flexibility, (ii) an acidic side chain, which incorporated the XPS fluorine tag, and (iii) a spacer-arm terminated by a primary amine for surface grafting. The most active compounds showed IC50 values in the nanomolar range versus isolated human integrins alpha(v)beta(3) and alpha(IIb)beta(3). Preincubation of CaCo2 cells with soluble peptidomimetics (2 and 19a) prevented cellular adhesion on culture plates coated with vitronectin. On the other hand, peptidomimetics (19a and 19b) immobilized on a poly(ethylene)terephthalate membrane (PET) promoted CaCo2 cells adhesion. A modeling study at the ab initio level in MINI-1' basis allowed to compare the various synthetic ligands of integrins and to propose novel pharmacophore structures. (C) 2004 Elsevier Ltd. All rights reserved.
Researchers ; Professionals
http://hdl.handle.net/2268/28936
10.1016/j.bmc.2004.07.055

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