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Titolo:
Conformations and pharmacophores of cyclic RGD containing peptides which selectively bind integrin alpha(v)beta(3)
Autore:
Locardi, E; Mullen, DG; Mattern, RH; Goodman, M;
Indirizzi:
Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA Univ Calif San Diego La Jolla CA USA 92093 iochem, La Jolla, CA 92093 USA Integra Lifesci Corp, Corp Res Ctr, San Diego, CA 92121 USA Integra Lifesci Corp San Diego CA USA 92121 Ctr, San Diego, CA 92121 USA
Titolo Testata:
JOURNAL OF PEPTIDE SCIENCE
fascicolo: 11, volume: 5, anno: 1999,
pagine: 491 - 506
SICI:
1075-2617(199911)5:11<491:CAPOCR>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
NUCLEAR MAGNETIC-RESONANCE; CELL-ADHESION; MONOCLONAL-ANTIBODY; COUPLING-CONSTANT; GLYCOPROTEIN-IIB; HIGHLY POTENT; ALPHA-V-BETA-3; SPECTROSCOPY; ANTAGONISTS; RECEPTOR;
Keywords:
RGD; integrins alpha(v)beta(3) and alpha(IIb)beta(3); molecular dynamics; nuclear magnetic resonance; peptide conformations;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
42
Recensione:
Indirizzi per estratti:
Indirizzo: Goodman, M Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA Univ Calif San Diego La Jolla CA USA 92093 Jolla, CA 92093 USA
Citazione:
E. Locardi et al., "Conformations and pharmacophores of cyclic RGD containing peptides which selectively bind integrin alpha(v)beta(3)", J PEPT SCI, 5(11), 1999, pp. 491-506

Abstract

This paper reports a detailed conformational characterization in solution by H-1-MMR in H2O and DMSO-d(6) and molecular modeling simulations of cyclic peptides containing the RGDDV pharmacophore and the RGDY(Me)R pharmacophore. These two pentapeptide sequences when properly constrained in cyclic peptides are low to sub-nanomolar inhibitors of integrin alpha(v)beta(3). Thepeptides containing the RGDDY(Me)R sequence bind potently to integrin alpha(IIb)beta(3) as well. The conformations found in H2O and in DMSO-d(6) solutions are valuable for the design of peptidomimetics of these two pharmacophores. The structure-activity relationships of the RGDDV and RGDY(Me)R pharmacophores within cyclic peptides are discussed. Specifically, the orientation of surface-accessible chemical features on the ligand, such as hydrophobic, positive and negative ionizable groups, which are considered to be responsible for the desired biological activity, is focused on. Copyright (C) 1999 European Peptide Society and John Wiley & Sons, Ltd.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/07/20 alle ore 04:40:47