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 αvβ3 and αvβ5 integrins are reported. Compound 1 was found to act as an active and selective inhibitor of the αvβ5 integrin.
Cyclic RGD peptides containing azabicycloalkane reverse-turn mimics / L. Belvisi, A. Caporale, M. Colombo, L. Manzoni, D. Potenza, C. Scolastico, M. Castorina, M. Cati, G. Giannini, C. Pisano. - In: HELVETICA CHIMICA ACTA. - ISSN 0018-019X. - 85:12(2002), pp. 4353-4368. [10.1002/hlca.200290017]
Cyclic RGD peptides containing azabicycloalkane reverse-turn mimics
L. BelvisiPrimo
;L. Manzoni;D. Potenza;C. Scolastico;
2002
Abstract
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 αvβ3 and αvβ5 integrins are reported. Compound 1 was found to act as an active and selective inhibitor of the αvβ5 integrin.
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