Synthesis and biological evaluation of new conformationally biased integrin ligands based on a tetrahydroazoninone scaffold.
The synthesis of new conformationally biased cyclic pentapeptides, incorporating the RGD sequence, and built around a tetrahydroazoninone scaffold, is reported. They exhibit interesting activity towards integrin alphaVbeta3 and a remarkable selectivity in comparison with integrin alphaVbeta5.
Banfi
Luca
L
Department of Chemistry and Industrial Chemistry, via Dodecaneso 31, 16146 Genova, Italy. banfi@chimica.unige.it
Basso
Andrea
A
Damonte
Gianluca
G
De Pellegrini
Federico
F
Galatini
Andrea
A
Guanti
Giuseppe
G
Monfardini
Ilaria
I
Riva
Renata
R
Scapolla
Carlo
C
D001391:Azo Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000378:metabolism; D016023:Integrins / Q000378:metabolism*; D008024:Ligands; D008968:Molecular Conformation; D009842:Oligopeptides; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology*; D019030:Receptors, Vitronectin / Q000378:metabolism; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D001391:Azo Compounds; D039302:Integrin alphaVbeta3; D016023:Integrins; D008024:Ligands; D009842:Oligopeptides; D010456:Peptides, Cyclic; D019030:Receptors, Vitronectin; C064660:integrin alphaVbeta5; C047981:arginyl-glycyl-aspartic acid