αvβ3 integrin-targeted peptide/peptidomimetic-drug conjugates: in-depth analysis of the linker technology
Articolo
Data di Pubblicazione:
2016
Citazione:
αvβ3 integrin-targeted peptide/peptidomimetic-drug conjugates: in-depth analysis of the linker technology / A. Dal Corso, L. Pignataro, L. Belvisi, C. Gennari. - In: CURRENT TOPICS IN MEDICINAL CHEMISTRY. - ISSN 1568-0266. - 16:3(2016), pp. 314-329. [10.2174/1568026615666150701114343]
Abstract:
Covalent conjugation of anticancer drugs to targeting carriers (e.g., antibodies or small molecules) capable of selectively binding to tumor-specific antigens, is emerging as a successful strategy to overcome the drawbacks of traditional chemotherapy. Due to its overexpression on blood vessels of human tumors, αvβ3 integrin is one of the most studied receptors of tumor-targeted therapeutics: several peptides and peptidomimetics, bearing the RGD (Arg-Gly-Asp) recognition sequence, have been developed as integrin ligands and linked to different anticancer drugs. The resulting integrintargeted small molecule-drug conjugates (SMDCs) are able to release the cytotoxic agents upon cleavage of a linker under specific conditions (i.e., hydrolysis, enzymatic action or reduction). Despite the significant efforts made in this field, αvβ3 integrin-targeted SMDCs are still far from the clinic. In this review, we survey this approach with a special focus on the different linkers employed and the reported biological activities in vitro and in vivo.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
anticancer prodrugs; drug targeting; integrins; peptidomimetics; RGD; small molecule-drug conjugates
Elenco autori:
A. Dal Corso, L. Pignataro, L. Belvisi, C. Gennari
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