47376-56-7Relevant academic research and scientific papers
Inhibitors selective for HDAC6 in enzymes and cells
Gupta, Praveer K.,Reid, Robert C.,Liu, Ligong,Lucke, Andrew J.,Broomfield, Steve A.,Andrews, Melanie R.,Sweet, Matthew J.,Fairlie, David P.
supporting information; experimental part, p. 7067 - 7070 (2011/01/03)
Histone deacetylase inhibitors with anticancer or anti-inflammatory activity bind to Class I or Class I and II HDAC enzymes. Here we compare selectivity of inhibitors of a Class II HDAC enzyme (HDAC6) and find one that retains high selectivity in macrophages.
Antimalarial histone deacetylase inhibitors containing cinnamate or NSAID components
Wheatley, Nicole C.,Andrews, Katherine T.,Tran, Truc L.,Lucke, Andrew J.,Reid, Robert C.,Fairlie, David P.
supporting information; experimental part, p. 7080 - 7084 (2010/12/25)
Malaria is the most lethal parasite-mediated tropical infectious disease, killing 1-2 million people each year. An emerging drug target is the enzyme Plasmodium falciparum histone deacetylase 1 (PfHDAC1). We report 26 compounds designed to bind the zinc and exterior surface around the entrance to the active site of PfHDAC1, 16 displaying potent in vitro antimalarial activity (IC 50 10-fold more cytotoxic towards P. falciparum than a normal human cell type (NFF). Twenty-two inhibitors feature cinnamic acid derivatives or non-steroidal anti-inflammatory drugs (NSAIDs) as HDAC-binding components. A homology model of PfHDAC1 enzyme gives new insights to interactions likely made by some of these inhibitors. Results support PfHDAC1 as a promising new antimalarial drug target.
