期刊
CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 16, 期 3, 页码 314-329出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026615666150701114343
关键词
Anticancer Prodrugs; Drug Targeting; Integrins; Peptidomimetics; RGD; Small Molecule-Drug Conjugates
资金
- Milan University
- Ministero dell'Universita e della Ricerca (PRIN project: Synthesis and biomedical applications of tumour-targeting peptidomimetics) [2010NRREPL]
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, alpha(v)beta(3) 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 integrin- targeted 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, alpha(v)beta(3) 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.
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