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 ,
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
