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Cancer epigenetics drug discovery and development: the challenge of hitting the mark
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scholarly article
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PubMed
title
Cancer epigenetics drug discovery and development: the challenge of hitting the mark
(English)
1 reference
stated in
PubMed
main subject
drug discovery
0 references
cancer epigenetics
1 reference
based on heuristic
inferred from title
author name string
Robert M. Campbell
series ordinal
1
1 reference
stated in
Crossref
Peter J. Tummino
series ordinal
2
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stated in
Crossref
language of work or name
English
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stated in
PubMed
publication date
January 2014
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stated in
PubMed
published in
Journal of Clinical Investigation
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stated in
PubMed
volume
124
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stated in
PubMed
issue
1
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stated in
PubMed
page(s)
64-9
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stated in
PubMed
cites work
A decade of exploring the cancer epigenome - biological and translational implications
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PubMed Central
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A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells
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21 March 2017
Selective inhibition of BET bromodomains
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PubMed Central
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21 March 2017
Genomic analysis using high-density single nucleotide polymorphism-based oligonucleotide arrays and multiplex ligation-dependent probe amplification provides a comprehensive analysis of INI1/SMARCB1 in malignant rhabdoid tumors
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PubMed Central
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21 March 2017
The bromodomain protein Brd4 is a positive regulatory component of P-TEFb and stimulates RNA polymerase II-dependent transcription
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PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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21 March 2017
CpG island methylator phenotype in colorectal cancer
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PubMed Central
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BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models
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21 March 2017
Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit
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21 March 2017
Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L
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PubMed Central
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21 March 2017
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
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PubMed Central
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21 March 2017
Selective Inhibitors of Histone Methyltransferase DOT1L: Design, Synthesis, and Crystallographic Studies
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PubMed Central
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21 March 2017
Discovery and characterization of small molecule inhibitors of the BET family bromodomains
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21 March 2017
Suppression of inflammation by a synthetic histone mimic
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21 March 2017
Role of the polycomb protein EED in the propagation of repressive histone marks
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PubMed Central
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21 March 2017
Somatic mutations of the histone methyltransferase gene EZH2 in myelodysplastic syndromes
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21 March 2017
The SWI/SNF genetic blockade: effects in cell differentiation, cancer and developmental diseases
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PubMed Central
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21 March 2017
BET bromodomain inhibition as a therapeutic strategy to target c-Myc
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21 March 2017
Causes and consequences of microRNA dysregulation in cancer
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21 March 2017
Demystified molecular pathology of NUT midline carcinomas
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21 March 2017
Recruitment of P-TEFb for stimulation of transcriptional elongation by the bromodomain protein Brd4
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PubMed Central
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21 March 2017
Truncating mutations of hSNF5/INI1 in aggressive paediatric cancer
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PubMed Central
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21 March 2017
Misguided transcriptional elongation causes mixed lineage leukemia
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21 March 2017
Methylation of H3-lysine 79 is mediated by a new family of HMTases without a SET domain
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21 March 2017
Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)
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7 April 2017
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations
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7 April 2017
Epigenetic protein families: a new frontier for drug discovery
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PubMed Central
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7 April 2017
Targeting MYC dependence in cancer by inhibiting BET bromodomains
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PubMed Central
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7 April 2017
CpG island methylator phenotype underlies sporadic microsatellite instability and is tightly associated with BRAF mutation in colorectal cancer
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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7 April 2017
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
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PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.
1 reference
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PubMed Central
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28 September 2017
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1
1 reference
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PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains
1 reference
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PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Interplay between the cancer genome and epigenome
1 reference
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Bromo-deaza-SAH: a potent and selective DOT1L inhibitor
1 reference
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PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Targeting MYCN in neuroblastoma by BET bromodomain inhibition
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain
1 reference
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PubMed Central
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28 September 2017
Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation
1 reference
stated in
PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l.
1 reference
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
1 reference
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PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Targeting epigenetic readers in cancer.
1 reference
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PubMed Central
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28 September 2017
Combination epigenetic therapy has efficacy in patients with refractory advanced non-small cell lung cancer
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28 September 2017
Epigenetic resensitization to platinum in ovarian cancer
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PubMed Central
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28 September 2017
NSD2 links dimethylation of histone H3 at lysine 36 to oncogenic programming
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PubMed Central
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28 September 2017
MLL-rearranged leukemia is dependent on aberrant H3K79 methylation by DOT1L.
1 reference
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28 September 2017
Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.
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28 September 2017
SWI/SNF nucleosome remodellers and cancer.
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PubMed Central
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28 September 2017
Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation
1 reference
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas
1 reference
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PubMed Central
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28 September 2017
The MMSET histone methyl transferase switches global histone methylation and alters gene expression in t(4;14) multiple myeloma cells.
1 reference
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PubMed Central
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28 September 2017
Epigenetic antagonism between polycomb and SWI/SNF complexes during oncogenic transformation
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PubMed Central
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28 September 2017
Histone lysine methylation and demethylation pathways in cancer
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Brd4 engagement from chromatin targeting to transcriptional regulation: selective contact with acetylated histone H3 and H4.
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
Quantitative mass spectrometry of histones H3.2 and H3.3 in Suz12-deficient mouse embryonic stem cells reveals distinct, dynamic post-translational modifications at Lys-27 and Lys-36
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
The target of the NSD family of histone lysine methyltransferases depends on the nature of the substrate
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
The molecular biology of mixed lineage leukemia
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PubMed Central
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28 September 2017
The multiple myeloma associated MMSET gene contributes to cellular adhesion, clonogenic growth, and tumorigenicity.
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PubMed Central
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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3871251
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28 September 2017
A role for the MLL fusion partner ENL in transcriptional elongation and chromatin modification
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28 September 2017
The mixed-lineage leukemia fusion partner AF4 stimulates RNA polymerase II transcriptional elongation and mediates coordinated chromatin remodeling
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PubMed Central
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28 September 2017
Ten years and counting: so what do we know about t(4;14)(p16;q32) multiple myeloma.
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28 September 2017
Chromosomal translocations involving the MLL gene: molecular mechanisms
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28 September 2017
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors
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31 May 2018
Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens
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31 May 2018
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31 May 2018
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28 November 2018
BRD-NUT oncoproteins: a family of closely related nuclear proteins that block epithelial differentiation and maintain the growth of carcinoma cells.
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28 November 2018
Biochemical characterization of human SET and MYND domain-containing protein 2 methyltransferase
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12 December 2020
based on heuristic
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Excessive CpG island hypermethylation in cancer cell lines versus primary human malignancies
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Identifiers
DOI
10.1172/JCI71605
1 reference
stated in
Consolidated OpenCitations Corpus – April 2017
OpenCitations bibliographic resource ID
4833671
OpenCitations bibliographic resource ID
4833671
1 reference
stated in
Consolidated OpenCitations Corpus – April 2017
OpenCitations bibliographic resource ID
4833671
PMCID
3871251
1 reference
stated in
Consolidated OpenCitations Corpus – April 2017
OpenCitations bibliographic resource ID
4833671
PubMed ID
24382391
1 reference
stated in
Consolidated OpenCitations Corpus – April 2017
OpenCitations bibliographic resource ID
4833671
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