A New Way Forward in Cancer Drug Discovery: Inhibiting the SWI/SNF Chromatin Remodelling Complex

Small molecule therapeutics targeting F-box proteins in cancer

(2016) Yuan Liu et al.   SEMINARS IN CANCER BIOLOGY

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor

(2015) Peter G. K. Clark et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

SWI/SNF Chromatin Remodeling and Human Malignancies

(2015) Julien Masliah-Planchon et al.   Annual Review of Pathology-Mechanisms of Disease

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies

(2015) Bhavatarini Vangamudi et al.   CANCER RESEARCH

Structure and organization of chromatin fiber in the nucleus

(2015) Guohong Li et al.   FEBS LETTERS

Mutant p53 cooperates with the SWI/SNF chromatin remodeling complex to regulateVEGFR2in breast cancer cells

(2015) Neil T. Pfister et al.   GENES & DEVELOPMENT

The SWI/SNF ATPases Are Required for Triple Negative Breast Cancer Cell Proliferation

(2015) Qiong Wu et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

(2015) Natalie H. Theodoulou et al.   JOURNAL OF MEDICINAL CHEMISTRY

SWI/SNF-mutant cancers depend on catalytic and non-catalytic activity of EZH2

(2015) Kimberly H Kim et al.   NATURE MEDICINE

Targeting protein–protein interactions (PPIs) of transcription factors: Challenges of intrinsically disordered proteins (IDPs) and regions (IDRs)

(2015) Susan Sammak et al.   PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY

Finding cancer’s weakest link

(2015) Nicole Michel Sodir et al.   Oncotarget

FBI1/Akirin2 promotes tumorigenicity and metastasis of Lewis lung carcinoma cells

(2014) Yuko Komiya et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Essential role of BRG, the ATPase subunit of BAF chromatin remodeling complexes, in leukemia maintenance

(2014) M. Buscarlet et al.   BLOOD

Vulnerabilities of Mutant SWI/SNF Complexes in Cancer

(2014) Katherine C. Helming et al.   CANCER CELL

Mutant p53 in Cancer: New Functions and Therapeutic Opportunities

(2014) Patricia A.J. Muller et al.   CANCER CELL

CARM1 Methylates Chromatin Remodeling Factor BAF155 to Enhance Tumor Progression and Metastasis

(2014) Lu Wang et al.   CANCER CELL

Akirin2 is critical for inducing inflammatory genes by bridging I B-  and the SWI/SNF complex

(2014) S. Tartey et al.   EMBO JOURNAL

Small-Molecule Inhibitors of the MDM2–p53 Protein–Protein Interaction (MDM2 Inhibitors) in Clinical Trials for Cancer Treatment

(2014) Yujun Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

ARID1B is a specific vulnerability in ARID1A-mutant cancers

(2014) Katherine C Helming et al.   NATURE MEDICINE

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

Functional epigenetics approach identifies BRM/SMARCA2 as a critical synthetic lethal target in BRG1-deficient cancers

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

Mechanisms and Functions of ATP-Dependent Chromatin-Remodeling Enzymes

(2013) Geeta J. Narlikar et al.   CELL

Reversible Disruption of mSWI/SNF (BAF) Complexes by the SS18-SSX Oncogenic Fusion in Synovial Sarcoma

(2013) Cigall Kadoch et al.   CELL

Molecular Pathways: SWI/SNF (BAF) Complexes Are Frequently Mutated in Cancer--Mechanisms and Potential Therapeutic Insights

(2013) X. Wang et al.   CLINICAL CANCER RESEARCH

Role of SWI/SNF in acute leukemia maintenance and enhancer-mediated Myc regulation

(2013) J. Shi et al.   GENES & DEVELOPMENT

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

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

Targeted disruption of the EZH2–EED complex inhibits EZH2-dependent cancer

(2013) Woojin Kim et al.   Nature Chemical Biology

MAX Inactivation in Small Cell Lung Cancer Disrupts MYC-SWI/SNF Programs and Is Synthetic Lethal with BRG1

(2013) O. A. Romero et al.   Cancer Discovery

Rational Design of Small-Molecule Inhibitors for β-Catenin/T-Cell Factor Protein–Protein Interactions by Bioisostere Replacement

(2012) Binxun Yu et al.   ACS Chemical Biology

BAF60 A, B, and Cs of muscle determination and renewal

(2012) P. L. Puri et al.   GENES & DEVELOPMENT

Targeted Disruption of the BCL9/ -Catenin Complex Inhibits Oncogenic Wnt Signaling

(2012) K. Takada et al.   Science Translational Medicine

Regulation of chromatin by histone modifications

(2011) Andrew J Bannister et al.   CELL RESEARCH

ATP-dependent chromatin remodeling: genetics, genomics and mechanisms

(2011) Diana C Hargreaves et al.   CELL 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

Mammalian SWI/SNF-A Subunit BAF250/ARID1 Is an E3 Ubiquitin Ligase That Targets Histone H2B

(2010) X. S. Li et al.   MOLECULAR AND CELLULAR BIOLOGY

Loss of the tumor suppressor Snf5 leads to aberrant activation of the Hedgehog-Gli pathway

(2010) Zainab Jagani et al.   NATURE MEDICINE

BAF60a Interacts with p53 to Recruit the SWI/SNF Complex

(2008) Jaehak Oh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Modelling Myc inhibition as a cancer therapy

(2008) Laura Soucek et al.   NATURE