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Platinum(iv) oxaliplatin-peptide conjugates targeting memHsp70+ phenotype in colorectal cancer cells.

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posted on 23.11.2019, 11:48 by Aoife M. McKeon, Janis Noonan, Marc Devocelle, Brona M. Murphy, Darren M. Griffith

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.

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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.

Publication Date

12/10/2017

Publisher

Royal Society of Chemistry

PubMed ID

28967013

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