Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays
DJ Urban, NJ Martinez, MI Davis, KR Brimacombe… - Scientific reports, 2017 - nature.com
Abstract Isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2) are key metabolic enzymes that
are mutated in a variety of cancers to confer a gain-of-function activity resulting in the
accumulation of an oncometabolite, D-2-hydroxyglutarate (2-HG). Accumulation of 2-HG can
result in epigenetic dysregulation and a block in cellular differentiation, suggesting these
mutations play a role in neoplasia. Based on its potential as a cancer target, a number of
small molecule inhibitors have been developed to specifically inhibit mutant forms of IDH …
are mutated in a variety of cancers to confer a gain-of-function activity resulting in the
accumulation of an oncometabolite, D-2-hydroxyglutarate (2-HG). Accumulation of 2-HG can
result in epigenetic dysregulation and a block in cellular differentiation, suggesting these
mutations play a role in neoplasia. Based on its potential as a cancer target, a number of
small molecule inhibitors have been developed to specifically inhibit mutant forms of IDH …
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