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      A chemical genomics approach to drug reprofiling in oncology: Antipsychotic drug risperidone as a potential adenocarcinoma treatment.

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          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.

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          Author and article information

          Journal
          Cancer Lett
          Cancer letters
          Elsevier BV
          1872-7980
          0304-3835
          May 01 2017
          : 393
          Affiliations
          [1 ] ValiRx plc, 3rd Floor, 16 Upper Woburn Place, London, WC1H 0BS, UK.
          [2 ] Department of Chemistry, University of Warwick, Coventry, CV4 7AL, UK.
          [3 ] Warwick Medical School, University of Warwick, Coventry, CV4 7AL, UK.
          [4 ] School of Chemistry, University of Leeds, Leeds, LS2 9JT, UK.
          [5 ] School of Chemistry, University of Leeds, Leeds, LS2 9JT, UK. Electronic address: p.c.taylor@leeds.ac.uk.
          Article
          S0304-3835(17)30084-8
          10.1016/j.canlet.2017.01.042
          28188816
          ae581fc1-998e-4d62-9c12-7eca29d38fb7
          Crown Copyright © 2017. Published by Elsevier B.V. All rights reserved.
          History

          17-β-Hydroxysteroid dehydrogenase 10,Adenocarcinoma,Chemical genomics,Drosophila melanogaster,Drug reprofiling

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