Therapeutic targeting of “undruggable” MYC

MYC as a Target for Cancer Treatment

(2021) Michael J Duffy et al.   CANCER TREATMENT REVIEWS

A bacterial protease depletes c-MYC and increases survival in mouse models of bladder and colon cancer

(2021) Daniel S. C. Butler et al.   NATURE BIOTECHNOLOGY

Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo

(2021) Christian Dubiella et al.   Nature Chemical Biology

Direct Phosphorylation and Stabilization of MYC by Aurora B Kinase Promote T-cell Leukemogenesis

(2020) Jue Jiang et al.   CANCER CELL

MYC, MYCL, and MYCN as therapeutic targets in lung cancer

(2020) Daniel Massó-Vallés et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Improved protein structure prediction using potentials from deep learning

(2020) Andrew W. Senior et al.   NATURE

Selective PP2A Enhancement through Biased Heterotrimer Stabilization

(2020) Daniel Leonard et al.   CELL

CUDC‐907, a novel dual PI3K and HDAC inhibitor, in prostate cancer: Antitumour activity and molecular mechanism of action

(2020) Cheng Hu et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Identification of a potent and selective covalent Pin1 inhibitor

(2020) Benika J. Pinch et al.   Nature Chemical Biology

MYC protein stability is negatively regulated by BRD4

(2020) Ballachanda N. Devaiah et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective USP7 inhibition elicits cancer cell killing through a p53-dependent mechanism

(2020) Nathan J. Schauer et al.   Scientific Reports

BET protein inhibitor JQ1 downregulates chromatin accessibility and suppresses metastasis of gastric cancer via inactivating RUNX2/NID1 signaling

(2020) Siqi Zhou et al.   Oncogenesis

The E3 ligase HUWE1 inhibition as a therapeutic strategy to target MYC in multiple myeloma

(2020) Lisa J. Crawford et al.   ONCOGENE

Partitioning of cancer therapeutics in nuclear condensates

(2020) Isaac A. Klein et al.   SCIENCE

Dissecting transcriptional amplification by MYC

(2020) Zuqin Nie et al.   eLife

MYC Antisense Oligonucleotide Impedes Tumorigenesis and Elicits Oncogene Addiction in Autochthonous Transgenic Mouse models of Hepatocellular and Renal Cell Carcinoma

(2020) Renumathy Dhanasekaran et al.   Molecular Therapy-Nucleic Acids

In vitro anticancer activity of fluphenazine, perphenazine and prochlorperazine. A review

(2020) Michał Otręba et al.   JOURNAL OF APPLIED TOXICOLOGY

Skp2 depletion reduces tumor-initiating properties and promotes apoptosis in synovial sarcoma

(2020) Jichuan Wang et al.   Translational Oncology

PROTAC Bromodomain Inhibitor ARV-825 Displays Anti-Tumor Activity in Neuroblastoma by Repressing Expression of MYCN or c-Myc

(2020) Zhiheng Li et al.   Frontiers in Oncology

Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity

(2019) Erin R. Aho et al.   Cell Reports

Intrinsic cell-penetrating activity propels Omomyc from proof of concept to viable anti-MYC therapy

(2019) Marie-Eve Beaulieu et al.   Science Translational Medicine

Randomized Phase III Study of Alisertib or Investigator’s Choice (Selected Single Agent) in Patients With Relapsed or Refractory Peripheral T-Cell Lymphoma

(2019) Owen A. O’Connor et al.   JOURNAL OF CLINICAL ONCOLOGY

The first-in-human study of the pan-PIM kinase inhibitor PIM447 in patients with relapsed and/or refractory multiple myeloma

(2019) Marc S. Raab et al.   LEUKEMIA

Acquired Resistance to BET-PROTACs(Proteolysis Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 ligase Complexes

(2019) Lu Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Crystal Structures and Nuclear Magnetic Resonance Studies of the Apo Form of the c-MYC:MAX bHLHZip Complex Reveal a Helical Basic Region in the Absence of DNA

(2019) Susan Sammak et al.   BIOCHEMISTRY

Mission Possible: Advances in MYC Therapeutic Targeting in Cancer

(2019) Brittany L. Allen-Petersen et al.   BIODRUGS

Omomyc reveals new mechanisms to inhibit the MYC oncogene

(2019) Mark J. Demma et al.   MOLECULAR AND CELLULAR BIOLOGY

Small-Molecule MYC Inhibitors Suppress Tumor Growth and Enhance Immunotherapy

(2019) Huiying Han et al.   CANCER CELL

Multiple direct interactions of TBP with the MYC oncoprotein

(2019) Yong Wei et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Interaction of the oncoprotein transcription factor MYC with its chromatin cofactor WDR5 is essential for tumor maintenance

(2019) Lance R. Thomas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5–MYC Protein–Protein Interaction

(2019) Jonathan D. Macdonald et al.   JOURNAL OF MEDICINAL CHEMISTRY

Formation of a structurally-stable conformation by the intrinsically disordered MYC:TRRAP complex

(2019) Edmond J. Feris et al.   PLoS One

Cdh1-mediated Skp2 degradation by dioscin reprogrammes aerobic glycolysis and inhibits colorectal cancer cells growth

(2019) Li Zhou et al.   EBioMedicine

Targeting Pin1 by All-Trans Retinoic Acid (ATRA) Overcomes Tamoxifen Resistance in Breast Cancer via Multifactorial Mechanisms

(2019) Songyin Huang et al.   Frontiers in Cell and Developmental Biology

Phase I studies of AZD1208, a proviral integration Moloney virus kinase inhibitor in solid and haematological cancers

(2018) Jorge Cortes et al.   BRITISH JOURNAL OF CANCER

Therapeutic targeting of PP2A

(2018) Caitlin M. O’Connor et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Enhancer invasion shapes MYCN-dependent transcriptional amplification in neuroblastoma

(2018) Rhamy Zeid et al.   NATURE GENETICS

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells

(2018) Otto Kauko et al.   Science Translational Medicine

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

(2018) Alina Castell et al.   Scientific Reports

The structure of INI1/hSNF5 RPT1 and its interactions with the c-MYC:MAX heterodimer provide insights into the interplay between MYC and the SWI/SNF chromatin remodeling complex

(2018) Susan Sammak et al.   FEBS Journal

FBXW7: a critical tumor suppressor of human cancers

(2018) Chien-Hung Yeh et al.   Molecular Cancer

Prolyl isomerase Pin1: a promoter of cancer and a target for therapy

(2018) Yang Chen et al.   Cell Death & Disease

Down-regulation of Skp2 expression inhibits invasion and lung metastasis in osteosarcoma

(2018) Yidan Zhang et al.   Scientific Reports

Transcription Factors Activate Genes through the Phase-Separation Capacity of Their Activation Domains

(2018) Ann Boija et al.   CELL

Targeting PIM Kinase with PD1 inhibition Improves Immunotherapeutic Antitumor T-cell Response

(2018) Shilpak Chatterjee et al.   CLINICAL CANCER RESEARCH

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

(2018) Lavinia Carabet et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

MYC Protein Interactome Profiling Reveals Functionally Distinct Regions that Cooperate to Drive Tumorigenesis

(2018) Manpreet Kalkat et al.   MOLECULAR CELL

CUDC-907 in relapsed/refractory diffuse large B-cell lymphoma, including patients with MYC-alterations: results from an expanded phase I trial

(2017) Yasuhiro Oki et al.   HAEMATOLOGICA

Activation of tumor suppressor protein PP2A inhibits KRAS-driven tumor growth

(2017) Jaya Sangodkar et al.   JOURNAL OF CLINICAL INVESTIGATION

USP7 small-molecule inhibitors interfere with ubiquitin binding

(2017) Lorna Kategaya et al.   NATURE

Molecular basis of USP7 inhibition by selective small-molecule inhibitors

(2017) Andrew P. Turnbull et al.   NATURE

Lysine-52 stabilizes the MYC oncoprotein through an SCFFbxw7-independent mechanism

(2017) J De Melo et al.   ONCOGENE

A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action

(2017) Elena Campaner et al.   Nature Communications

CUDC-907 in relapsed/refractory diffuse large B-cell lymphoma, including patients with MYC-alterations: results from an expanded phase I trial

(2017) Yasuhiro Oki et al.   HAEMATOLOGICA

Volasertib Versus Chemotherapy in Platinum-Resistant or -Refractory Ovarian Cancer: A Randomized Phase II Groupe des Investigateurs Nationaux pour l'Etude des Cancers de l'Ovaire Study

(2016) Eric Pujade-Lauraine et al.   JOURNAL OF CLINICAL ONCOLOGY

Safety, tolerability, and preliminary activity of CUDC-907, a first-in-class, oral, dual inhibitor of HDAC and PI3K, in patients with relapsed or refractory lymphoma or multiple myeloma: an open-label, dose-escalation, phase 1 trial

(2016) Anas Younes et al.   LANCET ONCOLOGY

Dual HDAC and PI3K Inhibitor CUDC-907 Downregulates MYC and Suppresses Growth of MYC-dependent Cancers

(2016) Kaiming Sun et al.   MOLECULAR CANCER THERAPEUTICS

Polo-like Kinase-1 Regulates Myc Stabilization and Activates a Feedforward Circuit Promoting Tumor Cell Survival

(2016) Daibiao Xiao et al.   MOLECULAR CELL

Ubiquitin-Dependent Turnover of MYC Antagonizes MYC/PAF1C Complex Accumulation to Drive Transcriptional Elongation

(2016) Laura A. Jaenicke et al.   MOLECULAR CELL

HAUSP deubiquitinates and stabilizes N-Myc in neuroblastoma

(2016) Omid Tavana et al.   NATURE MEDICINE

A MYC–aurora kinase A protein complex represents an actionable drug target in p53-altered liver cancer

(2016) Daniel Dauch et al.   NATURE MEDICINE

BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin

(2016) Ballachanda N Devaiah et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structural basis of N-Myc binding by Aurora-A and its destabilization by kinase inhibitors

(2016) Mark W. Richards et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Miz-1 and Max compete to engage c-Myc: implication for the mechanism of inhibition of c-Myc transcriptional activity by Miz-1

(2016) Mikaël Bédard et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin

(2016) Ballachanda N Devaiah et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Growth suppression by MYC inhibition in small cell lung cancer cells with TP53 and RB1 inactivation

(2016) Francesco Paolo Fiorentino et al.   Oncotarget

MYCL is a target of a BET bromodomain inhibitor, JQ1, on growth suppression efficacy in small cell lung cancer cells

(2016) Fuyumi Kato et al.   Oncotarget

PIAS1 Promotes Lymphomagenesis through MYC Upregulation

(2016) Andrea Rabellino et al.   Cell Reports

Myc and its interactors take shape

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

The spliceosome is a therapeutic vulnerability in MYC-driven cancer

(2015) Tiffany Y.-T. Hsu et al.   NATURE

Active Pin1 is a key target of all-trans retinoic acid in acute promyelocytic leukemia and breast cancer

(2015) Shuo Wei et al.   NATURE MEDICINE

Pre-Anchoring of Pin1 to Unphosphorylated c-Myc in a Fuzzy Complex Regulates c-Myc Activity

(2015) Sara Helander et al.   STRUCTURE

HAUSP regulates c-MYC expression via de-ubiquitination of TRRAP

(2015) Seemana Bhattacharya et al.   CELLULAR ONCOLOGY

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

(2015) Ho Kyung Seo et al.   Oncotarget

Cdc6 cooperates with c-Myc to promote genome instability and epithelial to mesenchymal transition (EMT) in zebrafish

(2015) Ching-Hung Chen et al.   Oncotarget

Drugging MYCN through an Allosteric Transition in Aurora Kinase A

(2014) William Clay Gustafson et al.   CANCER CELL

Tumor cell-specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase

(2014) S. Peter et al.   EMBO Molecular Medicine

Sin3b Interacts with Myc and Decreases Myc Levels

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

PIM Kinase Inhibitor AZD1208 for Treatment of MYC-Driven Prostate Cancer

(2014) Austin N. Kirschner et al.   JNCI-Journal of the National Cancer Institute

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 inhibition is effective against glioma and reveals a role for Myc in proficient mitosis

(2014) Daniela Annibali et al.   Nature Communications

MYC Degradation

(2014) A. S. Farrell 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

An Overview of MYC and Its Interactome

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

A Small-Molecule Inhibitor of PIM Kinases as a Potential Treatment for Urothelial Carcinomas

(2014) Jason M. Foulks et al.   NEOPLASIA

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

(2013) Markus Brockmann et al.   CANCER CELL

Pharmacological Inactivation of Skp2 SCF Ubiquitin Ligase Restricts Cancer Stem Cell Traits and Cancer Progression

(2013) Chia-Hsin Chan et al.   CELL

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

Transcriptional Amplification in Tumor Cells with Elevated c-Myc

(2012) Charles Y. Lin et al.   CELL

Molecular Pathways: The Complexity of the Epigenome in Cancer and Recent Clinical Advances

(2012) M. Conte et al.   CLINICAL CANCER RESEARCH

Triggering Fbw7-Mediated Proteasomal Degradation of c-Myc by Oridonin Induces Cell Growth Inhibition and Apoptosis

(2012) H.-L. Huang et al.   MOLECULAR CANCER THERAPEUTICS

Deregulated MYC expression induces dependence upon AMPK-related kinase 5

(2012) Lidan Liu et al.   NATURE

Targeting Synthetic Lethal Interactions between Myc and the eIF4F Complex Impedes Tumorigenesis

(2012) Chen-Ju Lin et al.   Cell Reports

Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia

(2011) B. Lowenberg et al.   BLOOD

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Clinical evaluation of AZD1152, an i.v. inhibitor of Aurora B kinase, in patients with solid malignant tumors

(2010) D. S. Boss et al.   ANNALS OF ONCOLOGY

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

E3 ubiquitin ligase Mule ubiquitinates Miz1 and is required for TNF -induced JNK activation

(2010) Y. Yang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2009) H. Jiang et al.   MOLECULAR PHARMACOLOGY

Myc-Mediated Transcriptional Repression by Recruitment of Histone Deacetylase

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

Modelling Myc inhibition as a cancer therapy

(2008) Laura Soucek et al.   NATURE

The HECT-domain ubiquitin ligase Huwe1 controls neural differentiation and proliferation by destabilizing the N-Myc oncoprotein

(2008) Xudong Zhao et al.   NATURE CELL BIOLOGY

Pim kinase-dependent inhibition of c-Myc degradation

(2008) Y Zhang et al.   ONCOGENE