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A pharmacogenomic approach validates AG-221 as an effective and on-target therapy in IDH2 mutant AML.

作者信息

Kats L M, Vervoort S J, Cole R, Rogers A J, Gregory G P, Vidacs E, Li J, Nagaraja R, Yen K E, Johnstone R W

机构信息

Cancer Therapeutics Program, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia.

The Sir Peter MacCallum Department of Oncology, University of Melbourne, Parkville, VIC, Australia.

出版信息

Leukemia. 2017 Jun;31(6):1466-1470. doi: 10.1038/leu.2017.84. Epub 2017 Mar 10.

DOI:10.1038/leu.2017.84
PMID:28280273
Abstract
摘要

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A pharmacogenomic approach validates AG-221 as an effective and on-target therapy in IDH2 mutant AML.一种药物基因组学方法验证了AG-221作为异柠檬酸脱氢酶2(IDH2)突变的急性髓系白血病(AML)的有效且靶向治疗药物。
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本文引用的文献

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Mutant IDH1 Downregulates ATM and Alters DNA Repair and Sensitivity to DNA Damage Independent of TET2.突变型异柠檬酸脱氢酶1(IDH1)下调共济失调毛细血管扩张突变基因(ATM),并改变DNA修复及对DNA损伤的敏感性,且与四氢叶酸还原酶2(TET2)无关。
Cancer Cell. 2016 Aug 8;30(2):337-348. doi: 10.1016/j.ccell.2016.05.018. Epub 2016 Jul 14.
2
Genomic Classification and Prognosis in Acute Myeloid Leukemia.急性髓系白血病的基因组分类与预后
N Engl J Med. 2016 Jun 9;374(23):2209-2221. doi: 10.1056/NEJMoa1516192.
3
Evidence for Clinical Differentiation and Differentiation Syndrome in Patients With Acute Myeloid Leukemia and IDH1 Mutations Treated With the Targeted Mutant IDH1 Inhibitor, AG-120.
致癌性 IDH1 突变导致的脂质合成失调是一种可靶向的合成致死脆弱性。
Cancer Discov. 2023 Feb 6;13(2):496-515. doi: 10.1158/2159-8290.CD-21-0218.
4
Preclinical efficacy against acute myeloid leukaemia of SH1573, a novel mutant IDH2 inhibitor approved for clinical trials in China.SH1573是一种新型突变型异柠檬酸脱氢酶2(IDH2)抑制剂,已在中国获批进行临床试验,其对急性髓系白血病的临床前疗效。
Acta Pharm Sin B. 2021 Jun;11(6):1526-1540. doi: 10.1016/j.apsb.2021.03.005. Epub 2021 Mar 9.
5
Non-genetic heterogeneity, altered cell fate and differentiation therapy.非遗传异质性、细胞命运改变和分化治疗。
EMBO Mol Med. 2021 Mar 5;13(3):e12670. doi: 10.15252/emmm.202012670. Epub 2021 Feb 8.
6
Oncometabolite L-2-hydroxyglurate directly induces vasculogenic mimicry through PHLDB2 in renal cell carcinoma.代谢物 L-2-羟基戊二酸通过 PHLDB2 在肾细胞癌中直接诱导血管生成拟态。
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Distinct clinical and prognostic implication of IDH1/2 mutation and other most frequent mutations in large duct and small duct subtypes of intrahepatic cholangiocarcinoma.IDH1/2 突变和其他常见突变在大导管型和小导管型肝内胆管细胞癌中的不同临床和预后意义。
BMC Cancer. 2020 Apr 15;20(1):318. doi: 10.1186/s12885-020-06804-6.
10
Oncometabolites in renal cancer.肾细胞癌中的代谢物。
Nat Rev Nephrol. 2020 Mar;16(3):156-172. doi: 10.1038/s41581-019-0210-z. Epub 2019 Oct 21.
使用靶向突变型异柠檬酸脱氢酶1(IDH1)抑制剂AG-120治疗的急性髓系白血病伴IDH1突变患者的临床分化及分化综合征证据
Clin Lymphoma Myeloma Leuk. 2016 Aug;16(8):460-5. doi: 10.1016/j.clml.2016.04.006. Epub 2016 May 5.
4
IDH2 inhibition in AML: Finally progress?急性髓系白血病中异柠檬酸脱氢酶2(IDH2)的抑制作用:终于取得进展了吗?
Best Pract Res Clin Haematol. 2015 Jun-Sep;28(2-3):112-5. doi: 10.1016/j.beha.2015.10.016. Epub 2015 Oct 19.
5
Proto-oncogenic role of mutant IDH2 in leukemia initiation and maintenance.突变型异柠檬酸脱氢酶2(IDH2)在白血病起始和维持中的原癌基因作用
Cell Stem Cell. 2014 Mar 6;14(3):329-41. doi: 10.1016/j.stem.2013.12.016. Epub 2014 Jan 16.
6
Cancer-associated IDH2 mutants drive an acute myeloid leukemia that is susceptible to Brd4 inhibition.癌症相关 IDH2 突变驱动急性髓系白血病,对 Brd4 抑制敏感。
Genes Dev. 2013 Sep 15;27(18):1974-85. doi: 10.1101/gad.226613.113.
7
Oncogenic isocitrate dehydrogenase mutations: mechanisms, models, and clinical opportunities.致癌性异柠檬酸脱氢酶突变:机制、模型和临床机会。
Cancer Discov. 2013 Jul;3(7):730-41. doi: 10.1158/2159-8290.CD-13-0083. Epub 2013 Jun 24.
8
Genomic and epigenomic landscapes of adult de novo acute myeloid leukemia.成人新发急性髓系白血病的基因组和表观基因组图谱。
N Engl J Med. 2013 May 30;368(22):2059-74. doi: 10.1056/NEJMoa1301689. Epub 2013 May 1.
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Transformation by the (R)-enantiomer of 2-hydroxyglutarate linked to EGLN activation.(R)-2-羟基戊二酸通过激活 EGLN 发生的转变。
Nature. 2012 Feb 15;483(7390):484-8. doi: 10.1038/nature10898.
10
Leukemic IDH1 and IDH2 mutations result in a hypermethylation phenotype, disrupt TET2 function, and impair hematopoietic differentiation.白血病 IDH1 和 IDH2 突变导致超甲基化表型,破坏 TET2 功能,并损害造血分化。
Cancer Cell. 2010 Dec 14;18(6):553-67. doi: 10.1016/j.ccr.2010.11.015. Epub 2010 Dec 9.