| First Author | Waitkus MS | Year | 2018 |
| Journal | Cancer Cell | Volume | 34 |
| Issue | 2 | Pages | 186-195 |
| PubMed ID | 29805076 | Mgi Jnum | J:264235 |
| Mgi Id | MGI:6195997 | Doi | 10.1016/j.ccell.2018.04.011 |
| Citation | Waitkus MS, et al. (2018) Biological Role and Therapeutic Potential of IDH Mutations in Cancer. Cancer Cell 34(2):186-195 |
| abstractText | Hotspot mutations in isocitrate dehydrogenase 1 (IDH1) and isocitrate dehydrogenase 2 (IDH2) occur in a variety of myeloid malignancies and solid tumors. Mutant IDH proteins acquire a neomorphic enzyme activity to produce the putative oncometabolite D-2-hydroxyglutarate, which is thought to block cellular differentiation by competitively inhibiting alpha-ketoglutarate-dependent dioxygenases involved in histone and DNA demethylation. Small-molecule inhibitors of mutant IDH1 and IDH2 have been developed and are progressing through pre-clinical and clinical development. In this review, we provide an overview of mutant IDH-targeted therapy and discuss a number of important recent pre-clinical studies using models of IDH-mutant solid tumors. |
