Dual kinase-bromodomain inhibitors for rationally designed polypharmacology (Q27681935)

9

0 references

Panagis Filippakopoulos

5

0 references

Susanne Müller

object named as

Susanne Müller

2

0 references

Stefan Knapp

object named as

Stefan Knapp

15

0 references

Alison O'Mahony

3

object named as

Alison O'Mahony

0 references

author name string

Pietro Ciceri

1

0 references

Oleg Fedorov

4

0 references

Jeremy P Hunt

6

0 references

Elisabeth A Lasater

7

0 references

Gabriel Pallares

8

0 references

Christopher Wells

10

0 references

Sarah Martin

11

0 references

Lisa M Wodicka

12

0 references

Neil P Shah

13

0 references

Daniel K Treiber

The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains

14

0 references

publication date

April 2014

0 references

published in

Nature Chemical Biology

0 references

volume

10

0 references

issue

4

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page(s)

305-12

0 references

cites work

1 reference

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RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

20 March 2017

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Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

20 March 2017

1 reference

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Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains

20 March 2017

1 reference

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2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors

20 March 2017

1 reference

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Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations

20 March 2017

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A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation

20 March 2017

1 reference

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

20 March 2017

1 reference

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

20 March 2017

1 reference

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Hallmarks of Cancer: The Next Generation

20 March 2017

1 reference

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Specific CLK Inhibitors from a Novel Chemotype for Regulation of Alternative Splicing

20 March 2017

1 reference

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Suppression of inflammation by a synthetic histone mimic

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Selective inhibition of BET bromodomains

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors

20 March 2017

1 reference

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BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity

20 March 2017

1 reference

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Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design

20 March 2017

1 reference

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Selectivity-determining residues in Plk1

20 March 2017

1 reference

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A protein kinase involved in the regulation of inflammatory cytokine biosynthesis

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Optimal description of a protein structure in terms of multiple groups undergoing TLS motion

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Likelihood-enhanced fast translation functions

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Coot: model-building tools for molecular graphics

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Refinement of macromolecular structures by the maximum-likelihood method

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Automated protein model building combined with iterative structure refinement

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

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

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Rapid measurement of binding constants and heats of binding using a new titration calorimeter

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Comprehensive analysis of kinase inhibitor selectivity

7 April 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Targeting MYC dependence in cancer by inhibiting 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=3998711

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

7 April 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1

7 April 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

PI3K pathway dependencies in endometrioid endometrial cancer cell lines

7 April 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

PFI-1, a highly selective protein interaction inhibitor, targeting BET 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=3998711

Transient exposure to quizartinib mediates sustained inhibition of FLT3 signaling while specifically inducing apoptosis in FLT3-activated leukemia cells

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Inhibition of BET bromodomain targets genetically diverse glioblastoma

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Kinase inhibitors: a new class of antirheumatic drugs

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Roles of p38 MAPKs in invasion and metastasis

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Kinase inhibitor selectivity profiling using differential scanning fluorimetry

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Bromodomains as therapeutic targets

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45 myeloma cells

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast gro

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Use of kinase inhibitors to dissect signaling pathways.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3998711

Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.

29 September 2017

1 reference

https://api.crossref.org/works/10.1038/NCHEMBIO.1471

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1038/NCHEMBIO.1471

Chemical target and pathway toxicity mechanisms defined in primary human cell systems

21 January 2018

1 reference

https://api.crossref.org/works/10.1038/NCHEMBIO.1471

Real-time and quantitative imaging of mammalian stress granules and processing bodies.

21 January 2018

1 reference

https://api.crossref.org/works/10.1038/NCHEMBIO.1471

Compensatory pathways in oncogenic kinase signaling and resistance to targeted therapies: six degrees of separation

21 January 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/24584101

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

The evolving war on cancer

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/24584101

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Evaluation of single-crystal X-ray diffraction data from a position-sensitive detector

1 reference

https://api.crossref.org/works/10.1038/NCHEMBIO.1471

inferred from DOI database lookup

7 January 2021

based on heuristic

Identifiers

DOI

10.1038/NCHEMBIO.1471

1 reference

Dimensions Publication ID

1037857835

0 references

1 reference

1 reference

PubMed publication ID

24584101

1 reference