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7415629 
Journal Article 
Carbamate prodrug concept for hydroxamate HDAC inhibitors 
Schlimme, S; Hauser, AT; Carafa, V; Heinke, R; Kannan, S; Stolfa, DA; Cellamare, S; Carotti, A; Altucci, LL; Jung, M; Sippl, W; , 
2011 
0 
ChemMedChem
ISSN: 1860-7179
EISSN: 1860-7187 
WILEY-BLACKWELL 
MALDEN 
6 
7 
1193-1198 
English 
21416613 
WOS:000292212100005 
Virtual screening efforts have identified several novel HDAC6 inhibitors with cellular isoform selectivity. In particular, a carbamate-protected hydroxamic acid exhibited improved effects with respect to protein hyperacetylation compared with the parent hydroxamate, possibly because of improved cell permeability. The carbamate structure therefore represents a potential prodrug concept for hydroxamic acid-containing HDAC inhibitors. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. 
Carbamates; Epigenetics; Histone deacetylases; Virtual screening; carbamic acid; histone deacetylase 6; histone deacetylase inhibitor; hydroxamic acid; prodrug; tubulin; animal cell; animal tissue; article; binding affinity; cell cycle arrest; cell cycle G1 phase; crystal structure; DNA binding motif; drug screening; drug selectivity; enzyme inhibition; histone acetylation; human; IC 50; in vitro study; inhibition kinetics; molecular docking; molecular model; nonhuman; priority journal; rat; structure activity relation; virtual reality; Western blotting; Carbamates; Computer Simulation; Histone Deacetylase Inhibitors; Histone Deacetylases; Hydroxamic Acids; Prodrugs; Recombinant Proteins; Structure-Activity Relationship 
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