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Cyclic RGD Peptides Containing Azabicycloalkane Reverse‐Turn Mimics
Author(s) -
Belvisi Laura,
Caporale Andrea,
Colombo Matteo,
Manzoni Leonardo,
Potenza Donatella,
Scolastico Carlo,
Castorina Massimo,
Cati Matilde,
Giannini Giuseppe,
Pisano Claudio
Publication year - 2002
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.200290017
Subject(s) - chemistry , integrin , lactam , stereochemistry , cyclic peptide , turn (biochemistry) , peptide , combinatorial chemistry , biochemistry , receptor
The Fmoc‐protected lactams 3 and 4 were used to prepare cyclo(Arg‐Gly‐Asp‐lactam) 1 and cyclo(Arg‐Gly‐Asp‐Phe‐lactam) 2 , which contain the Arg‐Gly‐Asp (RGD) recognition motif. Their solid‐phase synthesis, conformational analysis, and binding to purified α V β 3 and α V β 5 integrins are reported. Compound 1 was found to act as an active and selective inhibitor of the α V β 5 integrin.