Novel Pt(iv) tumour penetrating peptide (TPP) conjugates are reported. They are the first example of metallodrugs to target a membrane bound heat shock protein 70 positive (memHSP70+) phenotype in cancer cells. The conjugates exhibit superior cytotoxicity as compared to oxaliplatin alone in Pt resistant colorectal cancer cells with relatively high memHSP70+ expression. Substitution of TPP in Pt(iv) peptide conjugates with scrambled peptide (ScP) essentially abolishes the observed cytotoxicity.
Funding
Science Foundation Ireland (SFI) under Grant Number 12/IP/1305
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This article is also available at http://pubs.rsc.org/en/Content/ArticleLanding/2017/CC/C7CC04764A#!divAbstract
Published Citation
McKeon AM, Noonan J, Devocelle M, Murphy BM, Griffith DM. Platinum(iv) oxaliplatin-peptide conjugates targeting memHsp70+ phenotype in colorectal cancer cells. Chemical Communications. 2017;53(82):11318-11321.