Dilly, SJ, Clark, AJ, Marsh, A et al. (4 more authors) (2017) A Chemical Genomics Approach to Drug Reprofiling in Oncology: Antipsychotic Drug Risperidone as a Potential Adenocarcinoma Treatment. Cancer Letters, 393. pp. 16-21. ISSN 0304-3835
Abstract
Drug reprofiling is emerging as an effective paradigm for discovery of cancer treatments. Herein, an antipsychotic drug is immobilised using the Magic Tag® chemical genomics tool and screened against a T7 bacteriophage displayed library of polypeptides from Drosophila melanogaster, as a whole genome model, to uncover an interaction with a section of 17-β-HSD10, a proposed prostate cancer target. A computational study and enzyme inhibition assay with full length human 17-β-HSD10 identifies risperidone as a drug reprofiling candidate. When formulated with rumenic acid, risperidone slows proliferation of PC3 prostate cancer cells in vitro and retards PC3 prostate cancer tumour growth in vivo in xenografts in mice, presenting an opportunity to reprofile risperidone as a cancer treatment.
Metadata
Item Type: | Article |
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Authors/Creators: |
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Copyright, Publisher and Additional Information: | © 2017 Published by Elsevier Ireland Ltd. This is an author produced version of a paper published in Cancer Letters. Uploaded in accordance with the publisher's self-archiving policy. |
Keywords: | chemical genomics; drug reprofiling; Drosophila melanogaster; 17-β-hydroxysteroid dehydrogenase 10; adenocarcinoma |
Dates: |
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Institution: | The University of Leeds |
Academic Units: | The University of Leeds > Faculty of Engineering & Physical Sciences (Leeds) > School of Chemistry (Leeds) > Organic Chemistry (Leeds) |
Depositing User: | Symplectic Publications |
Date Deposited: | 03 Feb 2017 11:53 |
Last Modified: | 08 Feb 2018 01:38 |
Published Version: | https://doi.org/10.1016/j.canlet.2017.01.042 |
Status: | Published |
Publisher: | Elsevier |
Identification Number: | 10.1016/j.canlet.2017.01.042 |
Open Archives Initiative ID (OAI ID): | oai:eprints.whiterose.ac.uk:111561 |