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Small-molecule inhibitors of the Myc oncoprotein

Journal Article · · Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms

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Sponsoring Organization:
USDOE Office of Nuclear Energy (NE)
OSTI ID:
1357067
Journal Information:
Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms, Journal Name: Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms Journal Issue: 5 Vol. 1849; ISSN 1874-9399
Publisher:
ElsevierCopyright Statement
Country of Publication:
Netherlands
Language:
English

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Multiple Independent Binding Sites for Small-Molecule Inhibitors on the Oncoprotein c-Myc journal June 2009
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MYC inactivation uncovers pluripotent differentiation and tumour dormancy in hepatocellular cancer journal October 2004
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C-myc overexpression and p53 loss cooperate to promote genomic instability journal February 1999
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c-Myc depletion inhibits proliferation of human tumor cells at various stages of the cell cycle journal October 2007
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Identification of small molecules that induce apoptosis in a Myc-dependent manner and inhibit Myc-driven transformation journal April 2006
Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts journal March 2002
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Two-pronged Binding with Bromodomain-containing Protein 4 Liberates Positive Transcription Elongation Factor b from Inactive Ribonucleoprotein Complexes journal November 2011
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Targeted expression of MYCN causes neuroblastoma in transgenic mice journal June 1997
IAPs block apoptotic events induced by caspase-8 and cytochrome c by direct inhibition of distinct caspases journal April 1998
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Endogenous Myc maintains the tumor microenvironment journal April 2011
Inhibition of Myc family proteins eradicates KRas-driven lung cancer in mice journal March 2013
Multiple Ras-dependent phosphorylation pathways regulate Myc protein stability journal October 2000
Binding of c-Myc to chromatin mediates mitogen-induced acetylation of histone H4 and gene activation journal August 2001
The potential role of Aurora kinase inhibitors in haematological malignancies: Review journal October 2011
In Vitro Cytotoxicity and In Vivo Efficacy, Pharmacokinetics, and Metabolism of 10074-G5, a Novel Small-Molecule Inhibitor of c-Myc/Max Dimerization journal August 2010
Stabilizers of the Max Homodimer Identified in Virtual Ligand Screening Inhibit Myc Function journal June 2009
Sustained Loss of a Neoplastic Phenotype by Brief Inactivation of MYC journal July 2002
CANCER: Enhanced: Addiction to Oncogenes--the Achilles Heal of Cancer journal July 2002
Divergent Transcription from Active Promoters journal December 2008
A SUMOylation-Dependent Transcriptional Subprogram Is Required for Myc-Driven Tumorigenesis journal December 2011
Cancer Genome Landscapes journal March 2013
Potential of the Synthetic Lethality Principle journal November 2013
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Hypoxia-Inducible Factor 1 and Dysregulated c-Myc Cooperatively Induce Vascular Endothelial Growth Factor and Metabolic Switches Hexokinase 2 and Pyruvate Dehydrogenase Kinase 1 journal September 2007
Brd4 Recruits P-TEFb to Chromosomes at Late Mitosis To Promote G1 Gene Expression and Cell Cycle Progression journal November 2007
BRD4 Coordinates Recruitment of Pause Release Factor P-TEFb and the Pausing Complex NELF/DSIF To Regulate Transcription Elongation of Interferon-Stimulated Genes journal April 2013
The Brd4 Extraterminal Domain Confers Transcription Activation Independent of pTEFb by Recruiting Multiple Proteins, Including NSD3 journal May 2011
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PER and TIM Inhibit the DNA Binding Activity of aDrosophila CLOCK-CYC/dBMAL1 Heterodimer without Disrupting Formation of the Heterodimer: a Basis for Circadian Transcription journal August 1999
The Max Network Gone Mad journal February 2001
The c-MYC Oncoprotein Is a Substrate of the Acetyltransferases hGCN5/PCAF and TIP60 journal December 2004
Myc Stimulates Nuclearly Encoded Mitochondrial Genes and Mitochondrial Biogenesis journal July 2005
Formation of an Active Tissue-Specific Chromatin Domain Initiated by Epigenetic Marking at the Embryonic Stem Cell Stage journal March 2005
Origins of Specificity in Protein-DNA Recognition journal June 2010
Intrinsically Disordered Proteins in Human Diseases: Introducing the D 2 Concept journal June 2008
MicroRNA Let-7a Down-regulates MYC and Reverts MYC-Induced Growth in Burkitt Lymphoma Cells journal October 2007
BRD4 Sustains Melanoma Proliferation and Represents a New Target for Epigenetic Therapy journal August 2013
Improved low molecular weight Myc-Max inhibitors journal September 2007
BH3 Mimetics: Status of the Field and New Developments journal August 2013
Cancer-Associated Fibroblasts Drive the Progression of Metastasis through both Paracrine and Mechanical Pressure on Cancer Tissue journal September 2012
Molecular pathogenesis and clinical management of Fanconi anemia journal November 2012
CXCR4 downregulation of let-7a drives chemoresistance in acute myeloid leukemia journal May 2013
Therapeutic Targeting of Myc journal June 2010
Myc Roles in Hematopoiesis and Leukemia journal June 2010
MYC and Breast Cancer journal June 2010
Transcriptional Repression: The Dark Side of Myc journal June 2010
MYC and Prostate Cancer journal June 2010
Role of c-MYC in alternative activation of human macrophages and tumor-associated macrophage biology journal January 2012
Addiction to c-MYC in multiple myeloma journal September 2012
Outcome modeling with CRLF2, IKZF1, JAK, and minimal residual disease in pediatric acute lymphoblastic leukemia: a Children's Oncology Group Study journal April 2012
BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia journal October 2012
c-Myc hot spot mutations in lymphomas result in inefficient ubiquitination and decreased proteasome-mediated turnover journal March 2000
Mechanisms of Action of and Resistance to Antitubulin Agents: Microtubule Dynamics, Drug Transport, and Cell Death journal March 1999
c-myc in the hematopoietic lineage is crucial for its angiogenic function in the mouse embryo journal July 2008
let-7 MicroRNA Functions as a Potential Growth Suppressor in Human Colon Cancer Cells journal January 2006
B-RAF and N-RAS Mutations Are Preserved during Short Time In Vitro Propagation and Differentially Impact Prognosis journal February 2007
Mitochondrial Structure, Function and Dynamics Are Temporally Controlled by c-Myc journal May 2012
The Impact of Small Molecule Binding on the Energy Landscape of the Intrinsically Disordered Protein C-Myc journal July 2012
In Vivo Inhibition of c-MYC in Myeloid Cells Impairs Tumor-Associated Macrophage Maturation and Pro-Tumoral Activities journal September 2012
Small-molecule inhibitors of the p53-HDM2 interaction for the treatment of cancer journal November 2008
Intrinsic Disorder and Functional Proteomics journal March 2007
Inhibitors of Cell Cycle Kinases: Recent Advances and Future Prospects as Cancer Therapeutics journal January 2012
Disruption of Myc-Max Heterodimerization with Improved Cell-Penetrating Analogs of the Small Molecule 10074-G5 journal June 2013
Discovery of Modulators of Protein-Protein Interactions: Current Approaches and Limitations journal February 2011
Tumor microenvironment and angiogenesis journal January 2008
Recapitulating the α-helix: nonpeptidic, low-molecular-weight ligands for the modulation of helix-mediated protein–protein interactions journal December 2013
Stromal Fibroblasts in Cancer: A Novel Tumor-Promoting Cell Type journal July 2006
The Function and Regulation of the JARID1 Family of Histone H3 Lysine 4 Demethylases: the Myc Connection journal June 2007
P-TEFb is a Crucial Co-Factor for Myc Transactivation journal August 2007
The tumor suppressor p53: Cancer and aging journal April 2008
MYC, microRNAs and glutamine addiction in cancers journal October 2009
Insights into the function of the human P-TEFb component CDK9 in the regulation of chromatin modifications and co-transcriptional mRNA processing journal November 2009
CYCLINg through transcription: Post-translational modifications of P-TEFb regulate transcription elongation journal May 2010
P-TEFb stimulates transcription elongation and pre-mRNA splicing through multilateral mechanisms journal March 2010

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