Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

By F. Wang, J. Travins, B. Delabarre, V. Penard-Lacronique, S. Schalm, Erica Hansen, K. Straley, A. Kernytsky, Wei Liu, C. Gliser and 21 more. Science, 2013

775 citations recorded by the source corpus.

Subfields: Cancer Research, Genetics, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/521076efcf846af52ea67523e849d52e06030f70

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Cancer Research

1. Huafeng Zhang
2. M. V. Vander Heiden
3. D. Y. Gui
4. Alba Luengo
5. Ping Gao
6. Chuan He
7. Elaine R. Mardis
8. Linchong Sun

In Genetics

1. Chuan He
2. Richard K. Wilson
3. Malachi Griffith
4. Obi L. Griffith
5. Elaine R. Mardis
6. M. V. Vander Heiden
7. Jerzy K. Kulski

In Molecular Biology

1. Chuan He
2. Elaine R. Mardis
3. Jianjun Chen
4. Huafeng Zhang
5. Huilin Huang
6. Hengyou Weng
7. D. Y. Gui
8. Alba Luengo

Citations in the corpus

• The role of mutations in epigenetic regulators in myeloid malignancies (2012, background): “Based on these successful preclinical efforts, a phase I clinical trial of EPZ-5657, a DOT1L inhibitor, is currently underway in leukemia patients (136, 137).”
• Enasidenib in mutant IDH2 relapsed or refractory acute myeloid leukemia. (2017, neutral): “Age, median (range), y 67 (19-100) 67 (19-100) 70 (19-100)”
• SciClone: Inferring Clonal Architecture and Tracking the Spatial and Temporal Patterns of Tumor Evolution (2014, background): “Hence, this clonal mutation is an attractive target for small molecule inhibitors, such as those reactive against IDH2 R140Q [53].”
• Metabolic reprogramming and epigenetic modifications on the path to cancer (2021, background): “Treatment of TF-1 human erythroleukemia cells and primary human AML cells with AGI-6780 induces cellular differentiation (Wang et al., 2013).”
• R-2HG Exhibits Anti-tumor Activity by Targeting FTO/m6A/MYC/CEBPA Signaling (2017, background): “Because IDH mutants block cell differentiation and promote tumor transformation, and inhibition of mutant IDH (IDHi) can reverse this effect, R-2HG (as the major metabolic product of IDH mutants) has been regarded as an oncometabolite (Figueroa et al., 2010; Lu et al., 2012; Rohle et al., 2013;Wang ”
• Targeting Metabolism for Cancer Therapy (2017, background): “These epigenetic changes caused by D-2HG contribute to cancer phenotypes (Losman et al., 2013; Rohle et al., 2013; Saha et al., 2014; Wang et al., 2013), and have been proposed to promote oncogenesis by preventing normal cellular differentiation (Losman and Kaelin, 2013).”
• Cholangiocarcinoma — evolving concepts and therapeutic strategies (2017, neutral): “Small­molecule inhibitors of mutant IDH1 or IDH2 have shown favourable efficacy in preclinical studies 123,124 ; consequently, orally bio available inhibitors have entered clinical trials.”