Structural highlights
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
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.
Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs).,Schafer S, Saunders L, Eliseeva E, Velena A, Jung M, Schwienhorst A, Strasser A, Dickmanns A, Ficner R, Schlimme S, Sippl W, Verdin E, Jung M Bioorg Med Chem. 2008 Feb 15;16(4):2011-33. Epub 2007 Nov 4. PMID:18054239[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Schafer S, Saunders L, Eliseeva E, Velena A, Jung M, Schwienhorst A, Strasser A, Dickmanns A, Ficner R, Schlimme S, Sippl W, Verdin E, Jung M. Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs). Bioorg Med Chem. 2008 Feb 15;16(4):2011-33. Epub 2007 Nov 4. PMID:18054239 doi:10.1016/j.bmc.2007.10.092
