Premium
Cover Picture: A Chimeric SERM–Histone Deacetylase Inhibitor Approach to Breast Cancer Therapy (ChemMedChem 3/2014)
Author(s) -
Patel Hitisha K.,
Siklos Marton I.,
Abdelkarim Hazem,
Mendonca Emma L.,
Vaidya Aditya,
Petukhov Pavel A.,
Thatcher Gregory R. J.
Publication year - 2014
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201490005
Subject(s) - histone deacetylase , breast cancer , selective estrogen receptor modulator , antiestrogen , raloxifene , histone deacetylase inhibitor , chemistry , estrogen receptor , cancer research , tamoxifen , pharmacology , medicine , cancer , histone , biochemistry , gene
The front cover picture shows 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 p. 602 ff.