Cover Picture: A Chimeric SERM–Histone Deacetylase Inhibitor Approach to Breast Cancer Therapy (ChemMedChem 3/2014). Issue 3 (March 2014)

• Record Type: Journal Article
• Authors: Patel, Hitisha K.; Siklos, Marton I.; Abdelkarim, Hazem; Mendonca, Emma L.; Vaidya, Aditya; Petukhov, Pavel A.; Thatcher, Gregory R. J.
• Is Part Of: ChemMedChem. Volume 9:Issue 3(2014:Mar.)
• Page Start: 413
• Page End: 413
• Publication Date: 2014-03
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201490005
• Languages: English
• ISSNs: 1860-7179

Abstract

<abstract abstract-type="graphical" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold>The front cover picture shows</bold> a novel hybrid SERMostat that acts as both a class I histone deacetylase (HDAC) inhibitor and a selective estrogen receptor modulator (SERM). A combinatorial therapy using an HDAC inhibitor and antiestrogen drug is currently being tested in clinical trials for the treatment of ER() breast cancer, since HDAC inhibitors are proposed to increase transcription of ER (blue arrow). Based on this concept, SERMostats were designed with computational guidance and evaluated for their activity against ER() breast cancer cells. The SERMostats showed increased efficacy compared with the combinatorial treatment using the parent SERM and HDAC inhibitor. For further details, see the Full Paper by Gregory R. J. Thatcher et al. on <ext-link ext-link-type="doi" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink">p. 602 ff.</ext-link><boxed-text content-type="graphic" position="anchor" orientation="portrait"><graphic position="anchor" mimetype="image" xlink:href="ark:/27927/pgg4ss7jvj7" orientation="portrait" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /></boxed-text></p> </abstract>