Molecular Delivery of Cytotoxic Agents via Integrin Activation

Cancers

Daria Giacomini¹  Martina Cirillo¹ 

[1] Department of Chemistry “Giacomo Ciamician”, Alma Mater Studiorum University of Bologna, Via Selmi 2, 40126 Bologna, Italy;

关键词: integrins;    active targeting;    molecular delivery;    receptor targeting;    cancer;    selective citotoxycity;   

DOI  :  10.3390/cancers13020299

来源: DOAJ

【 摘 要 】

Integrins are cell adhesion receptors overexpressed in tumor cells. A direct inhibition of integrins was investigated, but the best inhibitors performed poorly in clinical trials. A gained attention towards these receptors arouse because they could be target for a selective transport of cytotoxic agents. Several active-targeting systems have been developed to use integrins as a selective cell entrance for some antitumor agents. The aim of this review paper is to report on the most recent results on covalent conjugates between integrin ligands and antitumor drugs. Cytotoxic drugs thus conjugated through specific linker to integrin ligands, mainly RGD peptides, demonstrated that the covalent conjugates were more selective against tumor cells and hopefully with fewer side effects than the free drugs.

【 授权许可】

Unknown