Small molecule inhibitors of mutant Isocitrate dehydrogenase 1 (IDH1) have been developed for the treatment of cancer. Normal IDH1 converts isocitrate into ketoglutarate. A mutated form of IDH1 is found in several cancers including glioma, cholangiocarcinoma, and acute myeloid leukemia. Expression of mutated IDH1 leadd to elevated levels of R-2-hydroxyglutarate (2HG). 2HG has been linked to the development of cancerous cells. Our investigators have developed small moleucle in hibitors of the mutant IDH1 enzyme. An advantage of targeting mutant IDH1 is that it is not present in non-cancerous cells, meaning that the use of these inhibitors should have little impact on healthy cells. We believe that these inhibitors provide a novel approach to cancer therapy.
- Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays. Sci Rep. 2017 Oct 6;7(1):12758.