Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains (Q28242369)

19

0 references

Panagis Filippakopoulos

Panagis Filippakopoulos

15

0 references

Susanne Müller

Susanne Müller

17

0 references

Stuart J. Conway

Stuart J Conway

11

0 references

Stefan Knapp

Stefan Knapp

18

0 references

Paul E. Brennan

20

Paul E Brennan

0 references

Carl Philpott

8

Martin Philpott

0 references

Sarah Picaud

7

Sarah Picaud

0 references

Mark E Bunnage

16

Mark E Bunnage

0 references

Anthony Tumber

13

Anthony Tumber

0 references

Cynthia Tallant

5

Cynthia Tallant

0 references

Catherine Rogers

10

Catherine M Rogers

0 references

Octovia P Monteiro

9

Octovia P Monteiro

0 references

Clarence Yapp

14

Clarence Yapp

0 references

author name string

Duncan A Hay

1

0 references

Oleg Fedorov

2

0 references

Sarah Martin

3

0 references

Dean C Singleton

4

0 references

Christopher Wells

6

0 references

Timothy P C Rooney

Journal of the American Chemical Society

12

0 references

language of work or name

English

0 references

publication date

2 July 2014

0 references

published in

0 references

volume

136

0 references

issue

26

0 references

page(s)

9308-19

0 references

cites work

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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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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

20 March 2017

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Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

20 March 2017

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Histone recognition and large-scale structural analysis of the human bromodomain family

20 March 2017

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Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides

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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BET bromodomain inhibition as a therapeutic strategy to target c-Myc

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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Suppression of inflammation by a synthetic histone mimic

20 March 2017

1 reference

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Selective inhibition of BET bromodomains

20 March 2017

1 reference

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The role of human bromodomains in chromatin biology and gene transcription

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Open access chemical and clinical probes to support drug discovery

20 March 2017

1 reference

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Inhibition of p53 transcriptional activity: a potential target for future development of therapeutic strategies for primary demyelination

20 March 2017

1 reference

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Structural Basis of Site-Specific Histone Recognition by the Bromodomains of Human Coactivators PCAF and CBP/p300

20 March 2017

1 reference

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

20 March 2017

1 reference

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Bromodomain: an acetyl-lysine binding domain

20 March 2017

1 reference

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CREB-binding protein and p300 in transcriptional regulation

20 March 2017

1 reference

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Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

20 March 2017

1 reference

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20 March 2017

Surfing the p53 network

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

CBP/p300 in cell growth, transformation, and development

20 March 2017

1 reference

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Redox-regulated recruitment of the transcriptional coactivators CREB-binding protein and SRC-1 to hypoxia-inducible factor 1alpha

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Molecular mechanisms of transcription activation by HLF and HIF1alpha in response to hypoxia: their stabilization and redox signal-induced interaction with CBP/p300.

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

p53 sites acetylated in vitro by PCAF and p300 are acetylated in vivo in response to DNA damage

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Activation of p53 sequence-specific DNA binding by acetylation of the p53 C-terminal domain

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Recruitment of p300/CBP in p53-dependent signal pathways

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

p53, the cellular gatekeeper for growth and division

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

The CBP co-activator is a histone acetyltransferase

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

The transcriptional coactivators p300 and CBP are histone acetyltransferases

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Regulation of transcription by hypoxia requires a multiprotein complex that includes hypoxia-inducible factor 1, an adjacent transcription factor, and p300/CREB binding protein

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

An essential role for p300/CBP in the cellular response to hypoxia

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

DNA damage activates p53 through a phosphorylation-acetylation cascade

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Ligand efficiency: a useful metric for lead selection

7 April 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

p300/CBP proteins: HATs for transcriptional bridges and scaffolds

7 April 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

7 April 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Setting expectations in molecular optimizations: Strengths and limitations of commonly used composite parameters

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

The bromodomain interaction module

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Place your BETs: the therapeutic potential of bromodomains

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

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

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Rational design of cyclic peptide modulators of the transcriptional coactivator CBP: a new class of p53 inhibitors

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

p53-mediated neuronal cell death in ischemic brain injury

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Target gene context influences the transcriptional requirement for the KAT3 family of CBP and p300 histone acetyltransferases.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

p53-Induced apoptosis and inhibitors of p53.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Rapid assessment of a novel series of selective CB(2) agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Target structure-based discovery of small molecules that block human p53 and CREB binding protein association

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

The p53 response: emerging levels of co-factor complexity.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Prospective therapeutic applications of p53 inhibitors

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

CBP and p300: HATs for different occasions

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

p53 inhibitors preserve dopamine neurons and motor function in experimental parkinsonism

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

p53-Mdm2--the affair that never ends

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

p300/CBP/p53 interaction and regulation of the p53 response

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

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=4183655

Signal transduction in hypoxic cells: inducible nuclear translocation and recruitment of the CBP/p300 coactivator by the hypoxia-inducible factor-1alpha

2 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction

2 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

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=4183655

BRD-NUT oncoproteins: a family of closely related nuclear proteins that block epithelial differentiation and maintain the growth of carcinoma cells.

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Suppression of tumor growth through disruption of hypoxia-inducible transcription

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4183655

Role of p53 in neurotoxicity induced by the endoplasmic reticulum stress agent tunicamycin in organotypic slice cultures of rat spinal cord

27 November 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/24946055

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/JA412434F

1 reference

release_q7is46e6wzd7fnk3varlwcvlu4

2056352

Fatcat ID

1 reference

Fatcat

https://api.fatcat.wiki/v0/release/q7is46e6wzd7fnk3varlwcvlu4

mapped directly with Wikidata item

24 November 2022

based on heuristic

2056352

1 reference

1 reference

1 reference