Therapeutic Inhibition of Myc in Cancer. Structural Bases and Computer-Aided Drug Discovery Approaches

G-quadruplex virtual drug screening: A review

(2018) Robert C. Monsen et al.   BIOCHIMIE

Ensemble Docking in Drug Discovery

(2018) Rommie E. Amaro et al.   BIOPHYSICAL JOURNAL

Design of Modular G-quadruplex Ligands

(2018) Ana Rita Duarte et al.   ChemMedChem

Clinical and molecular features of treatment-related neuroendocrine prostate cancer

(2018) Shusuke Akamatsu et al.   INTERNATIONAL JOURNAL OF UROLOGY

Discovery of a New Four-Leaf Clover-Like Ligand as a Potent c-MYC Transcription Inhibitor Specifically Targeting the Promoter G-Quadruplex

(2018) Ming-Hao Hu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cryo-EM in drug discovery: achievements, limitations and prospects

(2018) Jean-Paul Renaud et al.   NATURE REVIEWS DRUG DISCOVERY

The Expanding World of N-MYC–Driven Tumors

(2018) David S. Rickman et al.   Cancer Discovery

A selective high affinity MYC-binding compound inhibits MYC:MAX interaction and MYC-dependent tumor cell proliferation

(2018) Alina Castell et al.   Scientific Reports

Identification of a novel c-Myc inhibitor with antitumor effects on multiple myeloma cells

(2018) Ruosi Yao et al.   BIOSCIENCE REPORTS

Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer

(2018) Lavinia A. Carabet et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Crystal structure of the major quadruplex formed in the promoter region of the human c-MYC oncogene

(2018) Sascha Stump et al.   PLoS One

The MYC transcription factor network: balancing metabolism, proliferation and oncogenesis

(2018) Patrick A. Carroll et al.   Frontiers of Medicine

Chemical and structural studies provide a mechanistic basis for recognition of the MYC G-quadruplex

(2018) David R. Calabrese et al.   Nature Communications

Targeting the MYC Oncogene in Burkitt Lymphoma through HSP90 Inhibition

(2018) Candace Poole et al.   Cancers

CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours

(2017) Hong Xu et al.   Nature Communications

MYC Deregulation in Primary Human Cancers

(2017) Manpreet Kalkat et al.   Genes

MYC Modulation around the CDK2/p27/SKP2 Axis

(2017) Per Hydbring et al.   Genes

c-Myc Antagonises the Transcriptional Activity of the Androgen Receptor in Prostate Cancer Affecting Key Gene Networks

(2017) Stefan J. Barfeld et al.   EBioMedicine

Quadruplex nucleic acids as targets for anticancer therapeutics

(2017) Stephen Neidle   Nature Reviews Chemistry

Targeting MYC in cancer therapy: RNA processing offers new opportunities

(2016) Cheryl M. Koh et al.   BIOESSAYS

Hit Identification of a Novel Dual Binder forh-telo/c-mycG-Quadruplex by a Combination of Pharmacophore Structure-Based Virtual Screening and Docking Refinement

(2016) Roberta Rocca et al.   ChemMedChem

Ordering of mutations in acute myeloid leukemia with partial tandem duplication of MLL (MLL-PTD)

(2016) Q-Y Sun et al.   LEUKEMIA

Overexpression of c-myc is associated with adverse clinical features and worse overall survival in multiple myeloma

(2016) Agoston Gyula Szabo et al.   LEUKEMIA & LYMPHOMA

Divergent clonal evolution of castration-resistant neuroendocrine prostate cancer

(2016) Himisha Beltran et al.   NATURE MEDICINE

OmoMYC blunts promoter invasion by oncogenic MYC to inhibit gene expression characteristic of MYC-dependent tumors

(2016) L A Jung et al.   ONCOGENE

MYC-nick promotes cell migration by inducing fascin expression and Cdc42 activation

(2016) Sarah Anderson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study

(2016) Céline Berthon et al.   Lancet Haematology

Structure-based Inhibitor Design for the Intrinsically Disordered Protein c-Myc

(2016) Chen Yu et al.   Scientific Reports

Small Molecule Microarrays Enable the Identification of a Selective, Quadruplex-Binding Inhibitor of MYC Expression

(2015) Kenneth M. Felsenstein et al.   ACS Chemical Biology

Myc and its interactors take shape

(2015) William B. Tu et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Small-molecule inhibitors of the Myc oncoprotein

(2015) Steven Fletcher et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

AIMing towards improved antitumor efficacy

(2015) Matthew J. Weaver et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of a selective G-quadruplex DNA binder using a multistep virtual screening approach

(2015) Jin-Qiang Hou et al.   CHEMICAL COMMUNICATIONS

Targeting intrinsically disordered proteins in rational drug discovery

(2015) Susmitha Ambadipudi et al.   Expert Opinion on Drug Discovery

ZINC 15 – Ligand Discovery for Everyone

(2015) Teague Sterling et al.   Journal of Chemical Information and Modeling

Perturbation of the c-Myc–Max Protein–Protein Interaction via Synthetic α-Helix Mimetics

(2015) Kwan-Young Jung et al.   JOURNAL OF MEDICINAL CHEMISTRY

NF- B2/p52:c-Myc:hnRNPA1 Pathway Regulates Expression of Androgen Receptor Splice Variants and Enzalutamide Sensitivity in Prostate Cancer

(2015) N. Nadiminty et al.   MOLECULAR CANCER THERAPEUTICS

Small Molecule MYC Inhibitor Conjugated to Integrin-Targeted Nanoparticles Extends Survival in a Mouse Model of Disseminated Multiple Myeloma

(2015) D. Soodgupta et al.   MOLECULAR CANCER THERAPEUTICS

Abstract A49: Clinically efficacy of the BET bromodomain inhibitor TEN-010 in an open-label substudy with patients with documented NUT-midline carcinoma (NMC)

(2015) Geoffrey I. Shapiro et al.   MOLECULAR CANCER THERAPEUTICS

Interaction with WDR5 Promotes Target Gene Recognition and Tumorigenesis by MYC

(2015) Lance R. Thomas et al.   MOLECULAR CELL

Spatial genomic heterogeneity within localized, multifocal prostate cancer

(2015) Paul C Boutros et al.   NATURE GENETICS

Chemical intervention of the NM23-H2 transcriptional programme onc-MYCvia a novel small molecule

(2015) Chan Shan et al.   NUCLEIC ACIDS RESEARCH

MYC, Metabolism, and Cancer

(2015) Z. E. Stine et al.   Cancer Discovery

Structurally diverse c-Myc inhibitors share a common mechanism of action involving ATP depletion

(2015) Huabo Wang et al.   Oncotarget

Direct inhibition of c-Myc-Max heterodimers by celastrol and celastrol-inspired triterpenoids

(2015) Huabo Wang et al.   Oncotarget

Reversible Linkage of Two Distinct Small Molecule Inhibitors of Myc Generates a Dimeric Inhibitor with Improved Potency That Is Active in Myc Over-Expressing Cancer Cell Lines

(2015) Jutta Wanner et al.   PLoS One

Antitumor activity of the c-Myc inhibitor KSI-3716 in gemcitabine-resistant bladder cancer

(2015) Ho Kyung Seo et al.   Oncotarget

Disruption of Myc-Max Heterodimerization with Improved Cell-Penetrating Analogs of the Small Molecule 10074-G5

(2015) Huabo Wang et al.   Oncotarget

Drugging MYCN through an Allosteric Transition in Aurora Kinase A

(2014) William Clay Gustafson et al.   CANCER CELL

Discovery of Methyl 4′-Methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1′-biphenyl]-3-carboxylate, an Improved Small-Molecule Inhibitor of c-Myc-Max Dimerization

(2014) Jay Chauhan et al.   ChemMedChem

Stress-induced cleavage of Myc promotes cancer cell survival

(2014) M. Conacci-Sorrell et al.   GENES & DEVELOPMENT

Small Molecules Targeting c-Myc Oncogene: Promising Anti-Cancer Therapeutics

(2014) Bing-Jia Chen et al.   International Journal of Biological Sciences

Sin3b Interacts with Myc and Decreases Myc Levels

(2014) Pablo Garcia-Sanz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

In silico identification of novel ligands for G-quadruplex in the c-MYC promoter

(2014) Hyun-Jin Kang et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Therapeutic Effects of an Anti-Myc Drug on Mouse Pancreatic Cancer

(2014) Dimitris Stellas et al.   JNCI-Journal of the National Cancer Institute

Brd4 activates P-TEFb for RNA polymerase II CTD phosphorylation

(2014) Friederike Itzen et al.   NUCLEIC ACIDS RESEARCH

Targeting of the MYCN Protein with Small Molecule c-MYC Inhibitors

(2014) Inga Müller et al.   PLoS One

Inhibitor of MYC identified in a Krohnke pyridine library

(2014) J. R. Hart et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

MYC Degradation

(2014) A. S. Farrell et al.   Cold Spring Harbor Perspectives in Medicine

MYC and the Control of Apoptosis

(2014) S. B. McMahon   Cold Spring Harbor Perspectives in Medicine

Therapeutic Strategies to Inhibit MYC

(2014) M. R. McKeown et al.   Cold Spring Harbor Perspectives in Medicine

MYC Activation Is a Hallmark of Cancer Initiation and Maintenance

(2014) M. Gabay et al.   Cold Spring Harbor Perspectives in Medicine

MYC Cofactors: Molecular Switches Controlling Diverse Biological Outcomes

(2014) S. R. Hann   Cold Spring Harbor Perspectives in Medicine

An Overview of MYC and Its Interactome

(2014) M. Conacci-Sorrell et al.   Cold Spring Harbor Perspectives in Medicine

Small Molecule Inhibitors of Aurora-A Induce Proteasomal Degradation of N-Myc in Childhood Neuroblastoma

(2013) Markus Brockmann et al.   CANCER CELL

A Pt(ii)–Dip complex stabilizes parallel c-myc G-quadruplex

(2013) Jintao Wang et al.   CHEMICAL COMMUNICATIONS

Binding Site Detection and Druggability Prediction of Protein Targets for Structure- Based Drug Design

(2013) Yaxia Yuan et al.   CURRENT PHARMACEUTICAL DESIGN

Inhibition of Myc family proteins eradicates KRas-driven lung cancer in mice

(2013) L. Soucek et al.   GENES & DEVELOPMENT

Intravesical Instillation of c-MYC Inhibitor KSI-3716 Suppresses Orthotopic Bladder Tumor Growth

(2013) Kyung-Chae Jeong et al.   JOURNAL OF UROLOGY

Domain-specific c-Myc ubiquitylation controls c-Myc transcriptional and apoptotic activity

(2013) Q. Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Neuroblastoma and MYCN

(2013) M. Huang et al.   Cold Spring Harbor Perspectives in Medicine

Coordination of Nutrient Availability and Utilization by MAX- and MLX-Centered Transcription Networks

(2013) J. M. O'Shea et al.   Cold Spring Harbor Perspectives in Medicine

MYC, Metabolism, Cell Growth, and Tumorigenesis

(2013) C. V. Dang   Cold Spring Harbor Perspectives in Medicine

Ligand Clouds around Protein Clouds: A Scenario of Ligand Binding with Intrinsically Disordered Proteins

(2013) Fan Jin et al.   PLoS Computational Biology

Pharmacophore identification of c-Myc inhibitor 10074-G5

(2012) Jeremy L. Yap et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Addiction to c-MYC in multiple myeloma

(2012) T. Holien et al.   BLOOD

Distinct Transcriptional Programs Mediated by the Ligand-Dependent Full-Length Androgen Receptor and Its Splice Variants in Castration-Resistant Prostate Cancer

(2012) R. Hu et al.   CANCER RESEARCH

Transcriptional Amplification in Tumor Cells with Elevated c-Myc

(2012) Charles Y. Lin et al.   CELL

MYC on the Path to Cancer

(2012) Chi V. Dang   CELL

Occurrence, Biogenesis, and Synthesis of Biologically Active Carbazole Alkaloids

(2012) Arndt W. Schmidt et al.   CHEMICAL REVIEWS

Recent Progress and Future Potential for Metal Complexes as Anticancer Drugs Targeting G-quadruplex DNA

(2012) J. Zhang et al.   CURRENT MEDICINAL CHEMISTRY

Synergistic Applications of MD and NMR for the Study of Biological Systems

(2012) Olivier Fisette et al.   JOURNAL OF BIOMEDICINE AND BIOTECHNOLOGY

ZINC: A Free Tool to Discover Chemistry for Biology

(2012) John J. Irwin et al.   Journal of Chemical Information and Modeling

Surflex-Dock: Docking benchmarks and real-world application

(2012) Russell Spitzer et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Quantifying the chemical beauty of drugs

(2012) G. Richard Bickerton et al.   Nature Chemistry

The Impact of Small Molecule Binding on the Energy Landscape of the Intrinsically Disordered Protein C-Myc

(2012) Julien Michel et al.   PLoS One

Correction: Discovery of a Natural Product-Like c-myc G-Quadruplex DNA Groove-Binder by Molecular Docking

(2012) Dik-Lung Ma et al.   PLoS One

Inhibition of Cell Proliferation by Quindoline Derivative (SYUIQ-05) through its Preferential Interaction withc-mycPromoter G-Quadruplex

(2011) Tian-Miao Ou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Solution Structure of a 2:1 Quindoline–c-MYC G-Quadruplex: Insights into G-Quadruplex-Interactive Small Molecule Drug Design

(2011) Jixun Dai et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Impaired bortezomib binding to mutant β5 subunit of the proteasome is the underlying basis for bortezomib resistance in leukemia cells

(2011) N E Franke et al.   LEUKEMIA

c-MYC promoter G-quadruplex formed at the 5′-end of NHE III 1 element: insights into biological relevance and parallel-stranded G-quadruplex stability

(2011) Raveendra I. Mathad et al.   NUCLEIC ACIDS RESEARCH

The Action Mechanism of the Myc Inhibitor Termed Omomyc May Give Clues on How to Target Myc for Cancer Therapy

(2011) Mauro Savino et al.   PLoS One

Molecular Characterization of Neuroendocrine Prostate Cancer and Identification of New Drug Targets

(2011) H. Beltran et al.   Cancer Discovery

Dihydroartemisinin accelerates c-MYC oncoprotein degradation and induces apoptosis in c-MYC-overexpressing tumor cells

(2010) Jin-Jian Lu et al.   BIOCHEMICAL PHARMACOLOGY

Pharmacophore-based discovery of triaryl-substituted imidazole as new telomeric G-quadruplex ligand

(2010) Shuo-Bin Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting RNA Polymerase I with an Oral Small Molecule CX-5461 Inhibits Ribosomal RNA Synthesis and Solid Tumor Growth

(2010) Denis Drygin et al.   CANCER RESEARCH

Myc-Nick: A Cytoplasmic Cleavage Product of Myc that Promotes α-Tubulin Acetylation and Cell Differentiation

(2010) Maralice Conacci-Sorrell et al.   CELL

In Vitro Cytotoxicity and In Vivo Efficacy, Pharmacokinetics, and Metabolism of 10074-G5, a Novel Small-Molecule Inhibitor of c-Myc/Max Dimerization

(2010) D. M. Clausen et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Small-molecule inhibitors of c-Myc transcriptional factor suppress proliferation and induce apoptosis of promyelocytic leukemia cell via cell cycle arrest

(2010) Kyung-Chae Jeong et al.   Molecular BioSystems

The c-MYC NHE III1: Function and Regulation

(2009) Verónica González et al.   Annual Review of Pharmacology and Toxicology

Design, synthesis and biological evaluation of a novel class of anticancer agents: Anthracenylisoxazole lexitropsin conjugates

(2009) Xiaochun Han et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Small molecule inhibitors of Myc/Max dimerization and Myc-induced cell transformation

(2009) Jin Shi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Anticancer Activity of CX-3543: A Direct Inhibitor of rRNA Biogenesis

(2009) D. Drygin et al.   CANCER RESEARCH

Stabilization of G-Quadruplex DNA with Platinum(II) Schiff Base Complexes: Luminescent Probe and Down-Regulation of c-mycOncogene Expression

(2009) Peng Wu et al.   CHEMISTRY-A EUROPEAN JOURNAL

Multiple Independent Binding Sites for Small-Molecule Inhibitors on the Oncoprotein c-Myc

(2009) Dalia I. Hammoudeh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

NM23-H2 may play an indirect role in transcriptional activation of c-myc gene expression but does not cleave the nuclease hypersensitive element III1

(2009) T. S. Dexheimer et al.   MOLECULAR CANCER THERAPEUTICS

Stabilizers of the Max Homodimer Identified in Virtual Ligand Screening Inhibit Myc Function

(2009) H. Jiang et al.   MOLECULAR PHARMACOLOGY

Efficacy, pharmacokinetics, tisssue distribution, and metabolism of the Myc–Max disruptor, 10058-F4 [Z,E]-5-[4-ethylbenzylidine]-2-thioxothiazolidin-4-one, in mice

(2008) Jianxia Guo et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Myc-Mediated Transcriptional Repression by Recruitment of Histone Deacetylase

(2008) J. F. Kurland et al.   CANCER RESEARCH

Structural Rationale for the Coupled Binding and Unfolding of the c-Myc Oncoprotein by Small Molecules

(2008) Ariele Viacava Follis et al.   CHEMISTRY & BIOLOGY

Modelling Myc inhibition as a cancer therapy

(2008) Laura Soucek et al.   NATURE

Metastases suppressor NM23-H2 interaction with G-quadruplex DNA within c-MYC promoter nuclease hypersensitive element induces c-MYC expression

(2008) Ram Krishna Thakur et al.   NUCLEIC ACIDS RESEARCH