NGR Tumor-Homing Peptides: Structural Requirements for Effective APN (CD13) Targeting
نویسندگان
چکیده
منابع مشابه
1 A unified mechanism for aminopeptidase N - based tumor cell motility and tumor
Tumor cell surface aminopeptidase N (APN or CD13) has two puzzling functions unrelated to its enzymatic activity: mediating tumor cell motility and serving as a receptor for tumor-homing peptides (peptides that bring anti-cancer drugs to tumor cells). To investigate APN-based tumor-homing therapy, we determined the crystal structure of APN complexed with a tumor-homing peptide containing a repr...
متن کاملA unified mechanism for aminopeptidase N-based tumor cell motility and tumor-homing therapy.
Tumor cell surface aminopeptidase N (APN or CD13) has two puzzling functions unrelated to its enzymatic activity: mediating tumor cell motility and serving as a receptor for tumor-homing peptides (peptides that bring anti-cancer drugs to tumor cells). To investigate APN-based tumor-homing therapy, we determined the crystal structure of APN complexed with a tumor-homing peptide containing a repr...
متن کاملNGR-peptide−drug conjugates with dual targeting properties
Peptides containing the asparagine-glycine-arginine (NGR) motif are recognized by CD13/aminopeptidase N (APN) receptor isoforms that are selectively overexpressed in tumor neovasculature. Spontaneous decomposition of NGR peptides can result in isoAsp derivatives, which are recognized by RGD-binding integrins that are essential for tumor metastasis. Peptides binding to CD13 and RGD-binding integ...
متن کاملAminopeptidase N is a receptor for tumor-homing peptides and a target for inhibiting angiogenesis.
Phage that display a surface peptide with the NGR sequence motif home selectively to tumor vasculature in vivo. A drug coupled to an NGR peptide has more potent antitumor effects than the free drug [W. Arap et al., Science (Washington DC), 279: 377-380, 1998]. We show here that the receptor for the NGR peptides in tumor vasculature is aminopeptidase N (APN; also called CD13). NGR phage specific...
متن کاملCD13 Isoforms in Tumor Vessels, Epithelia, and Myeloid Cells Differential Binding of Drugs Containing the NGR Motif to
The NGR peptide motif is an aminopeptidase N (CD13) ligand that targets angiogenic blood vessels. NGR-containing peptides have proven useful for delivering cytotoxic drugs, proapoptotic peptides, and tumor necrosis factor(TNF) to tumor vasculature. Given that CD13 is not only expressed in the angiogenic endothelium but also in other cell types, the mechanism(s) for the tumor-homing properties o...
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ژورنال
عنوان ژورنال: Bioconjugate Chemistry
سال: 2016
ISSN: 1043-1802,1520-4812
DOI: 10.1021/acs.bioconjchem.6b00136