A NOVEL RGD CONTAINING DODECAPEPTIDOMIMETIC WHICH EXHIBITS SELECTIVE BINDING TO THE ALPHA(V)BETA(3) RECEPTOR

Authors
TRAN TA MATTERN RH ZHU Q GOODMAN M
Citation
Ta. Tran et al., A NOVEL RGD CONTAINING DODECAPEPTIDOMIMETIC WHICH EXHIBITS SELECTIVE BINDING TO THE ALPHA(V)BETA(3) RECEPTOR, Bioorganic & medicinal chemistry letters, 7(8), 1997, pp. 997-1002
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
8
Year of publication
1997
Pages
997 - 1002
Database
ISI
SICI code
0960-894X(1997)7:8<997:ANRCDW>2.0.ZU;2-S
Abstract
We report the synthesis, bioactivity and conformational analysis by H- 1 NMR and computer simulations of a RGD containing dodecapeptidomimeti c incorporating the beta-turn mimetic BTD. This peptidomimetic exhibit s potent binding to the alpha(v) beta(3) receptor. The binding activit y to the alpha(v) beta(5) receptor is approximately tenfold weaker. Un like most active RGD containing peptides reported to date this molecul e does not show any binding to the fibronectin (alpha(v) beta(1)) or t he IIb/IIIa receptors. (C) 1997 Elsevier Science Ltd.