## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a βFull Textβ option. The original article is trackable v
Rational Design and Development of Radiation-Sensitizing Histone Deacetylase Inhibitors
β Scribed by Mira Jung; Alan Kozikowski; Anatoly Dritschilo
- Publisher
- John Wiley and Sons
- Year
- 2005
- Tongue
- English
- Weight
- 102 KB
- Volume
- 2
- Category
- Article
- ISSN
- 1612-1872
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β¦ Synopsis
Histone deacetylases (HDACs) offer potentially attractive molecular targets for sensitizing cancers to treatment with radiation therapy. By affecting patterns of gene expression, differentiation, apoptosis, and enhanced responses to therapeutic agents may be induced in cancer cells. Here, we review the drug characteristics underlying design and screening of HDAC inhibitors with a focus on radiation-sensitizing properties. Radiation-sensitizing capacities have been observed in three model systems, squamous carcinoma of head and neck origin (SQ-20B), prostate adenocarcinoma (PC-3), and breast adenocarcinoma (MCF 7). Celltype specificities in radiation-sensitizing properties have been observed. Mechanisms underlying specificity are under investigation.
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## Abstract Various structurally modified analogues of FR235222 (**1**), a natural tetrapeptide inhibitor of mammalian histone deacetylases, were prepared in a convergent approach. The design of the compounds was aimed to investigate the effect of structural modifications of the tetrapeptide core i