Targeting the Eph System with Peptides and Peptide Conjugates

Molecular targeting with peptides or peptide-polymer conjugates: just a question of size?

The integrin ␣v␤3 is currently being evaluated as a molecular target for anti-angiogenic therapies. Several targeting strategies and probes are being studied to enable noninvasive imaging of ␣v␤3 expression in vivo. In the September issue of The Journal of Nuclear Medicine, Line et al. investigated peptide-polymer conjugates to exploit the " enhanced per-meability and retention " (EPR) effect a...

Targeting tumor angiogenesis: comparison of peptide and polymer-peptide conjugates.

UNLABELLED Endothelial cells in tumor angiogenesis are highly accessible, genetically stable and present unique molecular markers for targeted therapy. Neoplasia is also characterized by enhanced vascular permeability and disordered lymphatics so that both active and passive targeting strategies may play a role in localizing angiogenesis-targeted agents. To investigate the relative importance o...

NGR-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...

Preparation and evaluation of tumor-targeting peptide-oligonucleotide conjugates.

Enormous progress has been made in the development of antisense oligodeoxynucleotides (ODNs) as therapeutic agents inhibiting gene expression. Unfortunately, the therapeutical application of ODNs is still held back because of the low cellular uptake and the lack of specific transport into particular cells. In this paper, we report a drug-targeting system using somatostatin receptors (SSTRs) whi...

Bromoacetylated synthetic peptides. Starting materials for cyclic peptides, peptomers, and peptide conjugates.