Targeted delivery of paclitaxel to EphA2-expressing cancer cells.

ABSTRACT:

Purpose

YSA is an EphA2-targeting peptide that effectively delivers anticancer agents to prostate cancer tumors. Here, we report on how we increased the drug-like properties of this delivery system.

Experimental design

By introducing non-natural amino acids, we have designed two new EphA2 targeting peptides: YNH, where norleucine and homoserine replace the two methionine residues of YSA, and dYNH, where a D-tyrosine replaces the L-tyrosine at the first position of the YNH peptide. We describe the details of the synthesis of YNH and dYNH paclitaxel conjugates (YNH-PTX and dYNH-PTX) and their characterization in cells and in vivo.

Results

dYNH-PTX showed improved stability in mouse serum and significantly reduced tumor size in a prostate cancer xenograft model and also

SUBMITTER: Wang S 

PROVIDER: S-EPMC3537892 | biostudies-literature | 2013 Jan

REPOSITORIES: biostudies-literature