Novel inhibitors of the histone methyltransferase DOT1L show potent antileukemic activity in patient-derived xenografts

被引：36

作者：

Perner, Florian ^{[1
,2
,3
]}

Gadrey, Jayant Y. ^{[1
,2
,3
]}

Xiong, Yijun ^{[1
,2
,3
]}

Hatton, Charles ^{[1
,2
,3
]}

Eschle, Benjamin K. ^{[1
,2
,3
]}

Weiss, Andreas ^{[4
]}

Stauffer, Frederic ^{[4
]}

Gaul, Christoph ^{[4
]}

Tiedt, Ralph ^{[4
]}

Perry, Jennifer A. ^{[1
,2
,3
]}

Armstrong, Scott A. ^{[1
,2
,3
]}

Krivtsov, Andrei V. ^{[1
,2
,3
]}

机构：

[1] Dana Farber Canc Inst, Dept Pediat Oncol, Boston, MA 02115 USA

[2] Boston Childrens Hosp, Div Hematol Oncol, Boston, MA USA

[3] Harvard Med Sch, Boston, MA 02115 USA

[4] Novartis Inst Biomed Res, Basel, Switzerland

来源：

BLOOD | 2020年 / 136卷 / 17期

关键词：

GENE-EXPRESSION; MLL; LEUKEMIA;

D O I：

10.1182/blood.2020006113

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

引用

页码：1983 / 1988

页数：7

共 17 条

[1]

Bernt KM, 2011, EPIGENOMICS-UK, V3, P667, DOI [10.2217/EPI.11.98, 10.2217/epi.11.98]

[2] MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1L [J].

Bernt, Kathrin M. ;

Zhu, Nan ;

Sinha, Amit U. ;

Vempati, Sridhar ;

Faber, Joerg ;

Krivtsov, Andrei V. ;

Feng, Zhaohui ;

Punt, Natalie ;

Daigle, Amanda ;

Bullinger, Lars ;

Pollock, Roy M. ;

Richon, Victoria M. ;

Kung, Andrew L. ;

Armstrong, Scott A. .

CANCER CELL, 2011, 20 (01) :66-78

[3] A novel small molecule menin-MLL inhibitor for potential treatment of MLL-rearranged leukemias and NPM1/DNMT3A-mutant AML [J].

Burrows, Francis ;

Wu, Tao ;

Kessler, Linda ;

Li, Shuangwei ;

Zhang, Jingchuan ;

Zarrinkar, Patrick ;

Li, Liansheng ;

Cierpicki, Tomasz ;

Grembecka, Jolanta ;

Ren, Pingda ;

Liu, Yi .

MOLECULAR CANCER THERAPEUTICS, 2018, 17 (01)

[4] Mixed- Phenotype Acute Leukemia Diagnostic Criteria and Pitfalls [J].

Charles, Nathan J. ;

Boyer, Daniel F. .

ARCHIVES OF PATHOLOGY & LABORATORY MEDICINE, 2017, 141 (11) :1462-1468

[5] Targeting DOT1L and HOX gene expression in MLL-rearranged leukemia and beyond [J].

Chen, Chun-Wei ;

Armstrong, Scott A. .

EXPERIMENTAL HEMATOLOGY, 2015, 43 (08) :673-684

[6] DOT1L inhibits SIRT1-mediated epigenetic silencing to maintain leukemic gene expression in MLL-rearranged leukemia [J].

Chen, Chun-Wei ;

Koche, Richard P. ;

Sinha, Amit U. ;

Deshpande, Aniruddha J. ;

Zhu, Nan ;

Eng, Rowena ;

Doench, John G. ;

Xu, Haiming ;

Chu, Scott H. ;

Qi, Jun ;

Wang, Xi ;

Delaney, Christopher ;

Bernt, Kathrin M. ;

Root, David E. ;

Hahn, William C. ;

Bradner, James E. ;

Armstrong, Scott A. .

NATURE MEDICINE, 2015, 21 (04) :335-+

[7] Potent inhibition of DOT1L as treatment of MLL-fusion leukemia [J].

Daigle, Scott R. ;

Olhava, Edward J. ;

Therkelsen, Carly A. ;

Basavapathruni, Aravind ;

Jin, Lei ;

Boriack-Sjodin, P. Ann ;

Allain, Christina J. ;

Klaus, Christine R. ;

Raimondi, Alejandra ;

Scott, Margaret Porter ;

Waters, Nigel J. ;

Chesworth, Richard ;

Moyer, Mikel P. ;

Copeland, Robert A. ;

Richon, Victoria M. ;

Pollock, Roy M. .

BLOOD, 2013, 122 (06) :1017-1025

[8] Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l [J].

Deshpande, Aniruddha J. ;

Chen, Liying ;

Fazio, Maurizio ;

Sinha, Amit U. ;

Bernt, Kathrin M. ;

Banka, Deepti ;

Dias, Stuart ;

Chang, Jenny ;

Olhava, Edward J. ;

Daigle, Scott R. ;

Richon, Victoria M. ;

Pollock, Roy M. ;

Armstrong, Scott A. .

BLOOD, 2013, 121 (13) :2533-2541

[9] Diagnosis and management of AML in adults: 2017 ELN recommendations from an international expert panel [J].

Doehner, Hartmut ;

Estey, Elihu ;

Grimwade, David ;

Amadori, Sergio ;

Appelbaum, Frederick R. ;

Buechner, Thomas ;

Dombret, Herve ;

Ebert, Benjamin L. ;

Fenaux, Pierre ;

Larson, Richard A. ;

Levine, Ross L. ;

Lo-Coco, Francesco ;

Naoe, Tomoki ;

Niederwieser, Dietger ;

Ossenkoppele, Gert J. ;

Sanz, Miguel ;

Sierra, Jorge ;

Tallman, Martin S. ;

Tien, Hwei-Fang ;

Wei, Andrew H. ;

Lowenberg, Bob ;

Bloomfield, Clara D. .

BLOOD, 2017, 129 (04) :424-447

[10] MLL translocations, histone modifications and leukaemia stem-cell development [J].

Krivtsov, Andrei V. ;

Armstrong, Scott A. .

NATURE REVIEWS CANCER, 2007, 7 (11) :823-833

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