Biological Role and Therapeutic Potential of IDH Mutations in Cancer.
Publication
, Journal Article
Waitkus, MS; Diplas, BH; Yan, H
Published in: Cancer Cell
August 13, 2018
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 α-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.
Duke Scholars
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Published In
Cancer Cell
DOI
EISSN
1878-3686
Publication Date
August 13, 2018
Volume
34
Issue
2
Start / End Page
186 / 195
Location
United States
Related Subject Headings
- TOR Serine-Threonine Kinases
- Oncology & Carcinogenesis
- Neoplasms
- Mutation
- Mice
- Leukemia, Myeloid, Acute
- Isocitrate Dehydrogenase
- Humans
- Glioma
- Animals
Citation
APA
Chicago
ICMJE
MLA
NLM
Waitkus, M. S., Diplas, B. H., & Yan, H. (2018). Biological Role and Therapeutic Potential of IDH Mutations in Cancer. Cancer Cell, 34(2), 186–195. https://doi.org/10.1016/j.ccell.2018.04.011
Waitkus, Matthew S., Bill H. Diplas, and Hai Yan. “Biological Role and Therapeutic Potential of IDH Mutations in Cancer.” Cancer Cell 34, no. 2 (August 13, 2018): 186–95. https://doi.org/10.1016/j.ccell.2018.04.011.
Waitkus MS, Diplas BH, Yan H. Biological Role and Therapeutic Potential of IDH Mutations in Cancer. Cancer Cell. 2018 Aug 13;34(2):186–95.
Waitkus, Matthew S., et al. “Biological Role and Therapeutic Potential of IDH Mutations in Cancer.” Cancer Cell, vol. 34, no. 2, Aug. 2018, pp. 186–95. Pubmed, doi:10.1016/j.ccell.2018.04.011.
Waitkus MS, Diplas BH, Yan H. Biological Role and Therapeutic Potential of IDH Mutations in Cancer. Cancer Cell. 2018 Aug 13;34(2):186–195.
Published In
Cancer Cell
DOI
EISSN
1878-3686
Publication Date
August 13, 2018
Volume
34
Issue
2
Start / End Page
186 / 195
Location
United States
Related Subject Headings
- TOR Serine-Threonine Kinases
- Oncology & Carcinogenesis
- Neoplasms
- Mutation
- Mice
- Leukemia, Myeloid, Acute
- Isocitrate Dehydrogenase
- Humans
- Glioma
- Animals