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Asymmetric triplex metallohelices with high and selective activity against cancer cells

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Faulkner, Alan D., Kaner, Rebecca A., Abdallah, Qasem M. A., Clarkson, Guy J., Fox, David J., Gurnani, Pratik, Howson, Suzanne E., Phillips, Roger M. , Roper, David I., Simpson, Daniel H. and Scott, Peter (2014) Asymmetric triplex metallohelices with high and selective activity against cancer cells. Nature Chemistry, Volume 6 (Number 9). pp. 797-803. doi:10.1038/nchem.2024

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Official URL: http://dx.doi.org/10.1038/nchem.2024

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Abstract

Small cationic amphiphilic α-helical peptides are emerging as agents for the treatment of cancer and infection, but they are costly and display unfavourable pharmacokinetics. Helical coordination complexes may offer a three-dimensional scaffold for the synthesis of mimetic architectures. However, the high symmetry and modest functionality of current systems offer little scope to tailor the structure to interact with specific biomolecular targets, or to create libraries for phenotypic screens. Here, we report the highly stereoselective asymmetric self-assembly of very stable, functionalized metallohelices. Their anti-parallel head-to-head-to-tail ‘triplex’ strand arrangement creates an amphipathic functional topology akin to that of the active sub-units of, for example, host-defence peptides and ​p53. The metallohelices display high, structure-dependent toxicity to the human colon carcinoma cell-line HCT116 ​p53++, causing dramatic changes in the cell cycle without DNA damage. They have lower toxicity to human breast adenocarcinoma cells (MDA-MB-468) and, most remarkably, they show no significant toxicity to the bacteria methicillin-resistant Staphylococcus aureus and Escherichia coli.

At a glance

Item Type: Journal Article
Subjects: R Medicine > RC Internal medicine > RC0254 Neoplasms. Tumors. Oncology (including Cancer)
Divisions: Faculty of Science > Chemistry
Faculty of Science > Life Sciences (2010- )
Library of Congress Subject Headings (LCSH): Antineoplastic agents, Simple proteins
Journal or Publication Title: Nature Chemistry
Publisher: Nature Publishing Group
ISSN: 1755-4330
Official Date: 3 August 2014
Dates:
DateEvent
3 August 2014Published
30 June 2014Accepted
7 April 2014Submitted
Date of first compliant deposit: 28 December 2015
Volume: Volume 6
Number: Number 9
Page Range: pp. 797-803
DOI: 10.1038/nchem.2024
Status: Peer Reviewed
Publication Status: Published
Access rights to Published version: Restricted or Subscription Access
Funder: Engineering and Physical Sciences Research Council (EPSRC), University of Warwick

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