Data from Targeted Delivery of Paclitaxel to EphA2-Expressing Cancer Cells
Year: 2023
Type: other
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 reduced tumor vasculature in a syngeneic orthotopic allograft mouse model of renal cancer compared with vehicle or paclitaxel treatments. Conclusion: This study reveals that targeting EphA2 with dYNH drug conjugates could represent an effective way to deliver anticancer agents to a variety of tumor types. Clin Cancer Res; 19(1); 128–37. ©2012 AACR.
Authors: Si Wang, Roberta Noberini, John L. Stebbins, Swadesh Das, Ziming Zhang, Bainan Wu, Sayantan Mitra, Sandrine Billet, Ana Fernandez, Neil A. Bhowmick, Shinichi Kitada, Elena B. Pasquale, Paul B. Fisher, Maurizio Pellecchia
Language: English
Subfield: Biomaterials
Field: Materials Science
Domain: Physical Sciences
Open Access status: gold
OpenAlex ID: W4361950381