Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy (Q28269627)

Panagis Filippakopoulos

12

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Andrew Bannister

Andrew Bannister

16

0 references

Susanne Müller

Susanne Müller

29

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Stefan Knapp

Stefan Knapp

37

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Heidi Olzscha

Heidi Olzscha

7

0 references

Paul E. Brennan

Paul E Brennan

26

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Rab K Prinjha

35

Rab Prinjha

0 references

Ka Hing Che

15

Ka Hing Che

0 references

Dave Lugo

21

Dave Lugo

0 references

Carl Philpott

10

Martin Philpott

0 references

Sarah Picaud

1

Sarah Picaud

0 references

Jürg Schwaller

36

Jürg Schwaller

0 references

Anthony Tumber

11

Anthony Tumber

0 references

Chas Bountra

25

Chas Bountra

0 references

Alison O'Mahony

27

Alison O'Mahony

0 references

Octovia P Monteiro

8

Octovia Monteiro

0 references

Clarence Yapp

13

Clarence Yapp

0 references

Angeliki Thanasopoulou

3

Angeliki Thanasopoulou

0 references

Katharina Leonards

4

Katharina Leonards

0 references

Marjeta Urh

32

Marjeta Urh

0 references

Danette Daniels

31

Danette L Daniels

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author name string

Oleg Fedorov

2

0 references

Katherine Jones

5

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Julia Meier

6

0 references

Sarah Martin

9

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Christopher Wells

14

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Samuel Robson

17

0 references

Umesh Kumar

18

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Nigel Parr

19

0 references

Kevin Lee

20

0 references

Philip Jeffrey

22

0 references

Simon Taylor

23

0 references

Matteo L Vecellio

24

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Sharlene Velichko

28

0 references

Duncan Hay

30

0 references

Nicholas B La Thangue

Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains

33

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language of work or name

English

0 references

publication date

1 December 2015

0 references

published in

Cancer Research

0 references

volume

75

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issue

23

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page(s)

5106-19

0 references

cites work

1 reference

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20 March 2017

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Targeting bromodomains: epigenetic readers of lysine acetylation

20 March 2017

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20 March 2017

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Structure of the p300 catalytic core and implications for chromatin targeting and HAT regulation

20 March 2017

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20 March 2017

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Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

20 March 2017

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20 March 2017

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A Small Molecule Binding to the Coactivator CREB-Binding Protein Blocks Apoptosis in Cardiomyocytes

20 March 2017

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20 March 2017

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Selective inhibition of BET bromodomains

20 March 2017

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Global transcriptional coactivators CREB-binding protein and p300 are highly essential collectively but not individually in peripheral B cells

20 March 2017

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Structural mechanism of the bromodomain of the coactivator CBP in p53 transcriptional activation

20 March 2017

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BAFF-R, a newly identified TNF receptor that specifically interacts with BAFF

20 March 2017

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CREB binding protein interacts with nucleoporin-specific FG repeats that activate transcription and mediate NUP98-HOXA9 oncogenicity

20 March 2017

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Gene dosage-dependent embryonic development and proliferation defects in mice lacking the transcriptional integrator p300

20 March 2017

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RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

20 March 2017

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Drug combination studies and their synergy quantification using the Chou-Talalay method

7 April 2017

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Inducible in vivo silencing of Brd4 identifies potential toxicities of sustained BET protein inhibition

7 April 2017

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Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching

29 September 2017

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BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma

29 September 2017

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Differential gene expression of activating Fcγ receptor classifies active tuberculosis regardless of human immunodeficiency virus status or ethnicity

29 September 2017

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PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains

29 September 2017

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Mammalian two-hybrid assays for studies of interaction of p300 with transcription factors

29 September 2017

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A histone acetyltransferase p300 inhibitor C646 induces cell cycle arrest and apoptosis selectively in AML1-ETO-positive AML cells

29 September 2017

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The transcriptional coactivator Cbp regulates self-renewal and differentiation in adult hematopoietic stem cells.

29 September 2017

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Kinase inhibitor selectivity profiling using differential scanning fluorimetry

29 September 2017

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3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

29 September 2017

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The leukemogenicity of AML1-ETO is dependent on site-specific lysine acetylation

29 September 2017

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Life and death of transcriptional co-activator p300.

29 September 2017

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Oncogenesis by sequestration of CBP/p300 in transcriptionally inactive hyperacetylated chromatin domains

29 September 2017

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The STAT3 NH2-terminal domain stabilizes enhanceosome assembly by interacting with the p300 bromodomain.

29 September 2017

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29 September 2017

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Differential binding modes of the bromodomains of CREB-binding protein (CBP) and p300 with acetylated MyoD

29 September 2017

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Acetylation of p53 at lysine 373/382 by the histone deacetylase inhibitor depsipeptide induces expression of p21(Waf1/Cip1).

29 September 2017

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Conditional MLL-CBP targets GMP and models therapy-related myeloproliferative disease.

29 September 2017

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Characterization of genomic breakpoints in MLL and CBP in leukemia patients with t(11;16).

29 September 2017

1 reference

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29 September 2017

1 reference

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29 September 2017

1 reference

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Gene dose-dependent control of hematopoiesis and hematologic tumor suppression by CBP

29 September 2017

1 reference

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Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4948672

Interaction of c-Myb with p300 is required for the induction of acute myeloid leukemia (AML) by human AML oncogenes.

2 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4948672

Impairing MLL-fusion gene-mediated transformation by dissecting critical interactions with the lens epithelium-derived growth factor (LEDGF/p75).

27 November 2018

1 reference

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Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4948672

Systematic in vivo structure-function analysis of p300 in hematopoiesis

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4948672

ELDA: extreme limiting dilution analysis for comparing depleted and enriched populations in stem cell and other assays

27 November 2018

1 reference

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Mechanism of p300 specific histone acetyltransferase inhibition by small molecules

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4948672

Loss of CBP causes T cell lymphomagenesis in synergy with p27Kip1 insufficiency.

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4948672

All patients with the T(11;16)(q23;p13.3) that involves MLL and CBP have treatment-related hematologic disorders

27 November 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/26552700

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/26552700

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1158/0008-5472.CAN-15-0236

1 reference

1 reference

1 reference

PubMed publication ID

26552700

1 reference