Title of article
Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs) Original Research Article
Author/Authors
Stefan Sch?fer، نويسنده , , Laura Saunders، نويسنده , , Elena Eliseeva، نويسنده , , Alfredo Velena، نويسنده , , Mira Jung، نويسنده , , Andreas Schwienhorst، نويسنده , , Anja Strasser، نويسنده , , Achim Dickmanns، نويسنده , , Wolfgang Garten and Ralf Ficner، نويسنده , , Sonja Schlimme، نويسنده , , Wolfgang Sippl، نويسنده , , Eric Verdin، نويسنده , , Manfred Jung، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
23
From page
2011
To page
2033
Abstract
We synthesized biarylalanine-containing hydroxamic acids and tested them on immunoprecipitated HDAC1 and HDAC6 and show a subtype selectivity for HDAC6 that was confirmed in cells by Western blot (tubulin vs histones). We obtained an X-ray structure with a HDAC6-selective inhibitor with the bacterial deacetylase HDAH. Docking studies were carried out using HDAC1 and HDAC6 protein models. Antiproliferative activity was shown on cancer cells for selected compounds.
Keywords
Class I and II HDAC inhibitor , Gold docking , Histone deacetylase (HDAC) , subtype selectivity , Hydroxamic acid
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2008
Journal title
Bioorganic and Medicinal Chemistry
Record number
1304049
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