title: NGR-based strategies for targeting delivery of chemotherapeutics to tumor vasculature.
abstract: In the last decades, NGR-containing peptides have been proved useful for ligand-directed targeted delivery of various chemotherapeutic drugs to tumor vasculature. Aminopeptidase N (APN; CD13) has been demonstrated to be a key binding site for NGR peptides on tumor vasculature. For drug targeting, chemical means have been applied to couple NGR-peptides to small molecule drugs, such as cytokines, antiangiogenic compounds, viral particles, contrast agents, DNA complexes and other biologic response modifiers. Some products have shown impressive results in preclinical animal models, such as NGR-TNF which was currently tested in Phase III trials. In this article we will review the process of NGR-to-isoDGR transition and provide suggestions for the design of the diverse NGR peptide-chemotherapeutics conjugates.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, ShanDong University, Jinan, ShanDong, P.R. China.
authors.forename: Mingming
authors.initials: M
authors.lastname: Zou
authors.forename: Lei
authors.initials: L
authors.lastname: Zhang
authors.forename: Yuanchao
authors.initials: Y
authors.lastname: Xie
authors.forename: Wenfang
authors.initials: W
authors.lastname: Xu
mesh_terms: D020533:Angiogenesis Inhibitors / Q000008:administration & dosage*; D000818:Animals; D002986:Clinical Trials as Topic; D016503:Drug Delivery Systems / Q000379:methods; D004353:Drug Evaluation, Preclinical; D006801:Humans; D009369:Neoplasms / Q000098:blood supply* / Q000188:drug therapy*; D009389:Neovascularization, Pathologic / Q000188:drug therapy / Q000473:pathology; D009842:Oligopeptides / Q000008:administration & dosage*
chemical_list: D020533:Angiogenesis Inhibitors; C526428:NGR peptide; D009842:Oligopeptides