Potent inhibition of DOT1L as treatment of MLL-fusion leukemia (Q27678800)

2

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Carly A Therkelsen

3

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Aravind Basavapathruni

4

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Lei Jin

5

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P Ann Boriack-Sjodin

6

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Christina J Allain

7

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Christine R Klaus

8

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Alejandra Raimondi

9

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Margaret Porter Scott

10

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Nigel J Waters

11

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Richard Chesworth

12

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Mikel P Moyer

13

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Robert A Copeland

14

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Victoria M Richon

15

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Roy M Pollock

Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L

16

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language of work or name

English

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publication date

8 August 2013

0 references

published in

Blood

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volume

122

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issue

6

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page(s)

1017-25

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cites work

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Function of leukemogenic mixed lineage leukemia 1 (MLL) fusion proteins through distinct partner protein complexes

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MLL-rearranged leukemia is dependent on aberrant H3K79 methylation by DOT1L.

29 September 2017

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DOT1L, the H3K79 methyltransferase, is required for MLL-AF9-mediated leukemogenesis

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Histone H3 Lysine 79 Methyltransferase Dot1 Is Required for Immortalization by MLL Oncogenes

29 September 2017

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29 September 2017

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MLL-AF9 and MLL-ENL alter the dynamic association of transcriptional regulators with genes critical for leukemia

29 September 2017

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29 September 2017

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MLL-AF9-induced leukemogenesis requires coexpression of the wild-type Mll allele.

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29 September 2017

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H3K79 methylation profiles define murine and human MLL-AF4 leukemias

29 September 2017

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A role for the MLL fusion partner ENL in transcriptional elongation and chromatin modification

29 September 2017

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The mixed-lineage leukemia fusion partner AF4 stimulates RNA polymerase II transcriptional elongation and mediates coordinated chromatin remodeling

29 September 2017

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Dot1a-AF9 complex mediates histone H3 Lys-79 hypermethylation and repression of ENaCalpha in an aldosterone-sensitive manner

29 September 2017

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Binding to nonmethylated CpG DNA is essential for target recognition, transactivation, and myeloid transformation by an MLL oncoprotein

29 September 2017

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MLL: a histone methyltransferase disrupted in leukemia

29 September 2017

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The Oncogenic Capacity of HRX-ENL Requires the Transcriptional Transactivation Activity of ENL and the DNA Binding Motifs of HRX

29 September 2017

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11q23 translocations split the "AT-hook" cruciform DNA-binding region and the transcriptional repression domain from the activation domain of the mixed-lineage leukemia (MLL) gene

29 September 2017

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29 September 2017

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Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

29 September 2017

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Leukemogenic MLL fusion proteins bind across a broad region of the Hox a9 locus, promoting transcription and multiple histone modifications

2 June 2018

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27 November 2018

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