Thursday, April 4, 2013
This week in techniques
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Trifluoromethyloxadiazole (TFMO)-containing compounds to identify
class IIa histone
compounds could be used as research compounds to guide development of class
IIa HDAC inhibitors. Genetic associations have been identified between class
IIa HDACs and Huntington's disease (HD), glucose homeostasis, muscular
dystrophies, autoimmunity and ischemic stroke. A screen of about 2 million
compounds from GlaxoSmithKline
plc's diversity collection identified compounds with HDAC9
inhibitory activity, with 3 of the 4 most potent hits containing the TFMO
chemical group. In inhibition assays of HDACs 1-11, the top hit showed
preferential inhibition of class IIa HDACs and did not cause cell toxicity.
Next steps at Tempero
Pharmaceuticals Inc. and GSK include using the research
compounds to evaluate the therapeutic potential of class IIa HDACs in
autoimmune diseases (see Closer to class IIa HDAC inhibitors,
Published online April 4, 2013
Patent status undisclosed;
Tempero is interested in collaboration opportunities
Lobera, M. et al. Nat.
Chem. Biol.; published online March 24, 2013;
Contact: Michael A. Nolan, Tempero Pharmaceuticals Inc., Cambridge,
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