A novel β-catenin/BCL9 complex inhibitor blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer

Regulation of Wnt Signaling Pathways at the Plasma Membrane and Their Misregulation in Cancer

(2021) Yagmur Azbazdar et al.   Frontiers in Cell and Developmental Biology

miR-15a/16-1 deletion in activated B cells promotes plasma cell and mature B-cell neoplasms

(2021) Tomasz Sewastianik et al.   BLOOD

Role of Cholesterol and Lipid Rafts in Cancer Signaling: A Promising Therapeutic Opportunity?

(2021) Rosa Vona et al.   Frontiers in Cell and Developmental Biology

Low glycaemic diets alter lipid metabolism to influence tumour growth

(2021) Evan C. Lien et al.   NATURE

BCL9 provides multi-cellular communication properties in colorectal cancer by interacting with paraspeckle proteins

(2020) Meng Jiang et al.   Nature Communications

APC controls Wnt-induced β-catenin destruction complex recruitment in human colonocytes

(2020) Taybor W. Parker et al.   Scientific Reports

Loss of the nuclear Wnt pathway effector TCF7L2 promotes migration and invasion of human colorectal cancer cells

(2020) Janna Wenzel et al.   ONCOGENE

Inhibition of β-catenin/B cell lymphoma 9 protein−protein interaction using α-helix–mimicking sulfono-γ-AApeptide inhibitors

(2019) Peng Sang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Pharmacological inhibition of β-catenin/BCL9 interaction overcomes resistance to immune checkpoint blockades by modulating Treg cells

(2019) M. Feng et al.   Science Advances

Wnt/β-Catenin Signaling: The Culprit in Pancreatic Carcinogenesis and Therapeutic Resistance

(2019) Monish Ram Makena et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

VIPER: Visualization Pipeline for RNA-seq, a Snakemake workflow for efficient and complete RNA-seq analysis

(2018) MacIntosh Cornwell et al.   BMC BIOINFORMATICS

Wnt signaling in development and tissue homeostasis

(2018) Zachary Steinhart et al.   DEVELOPMENT

Porcupine inhibitors impair trabecular and cortical bone mass and strength in mice

(2018) Thomas Funck-Brentano et al.   JOURNAL OF ENDOCRINOLOGY

Structure-Based Optimization of Small-Molecule Inhibitors for the β-Catenin/B-Cell Lymphoma 9 Protein–Protein Interaction

(2018) Min Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cholesterol Esterification Inhibition Suppresses Prostate Cancer Metastasis by Impairing the Wnt/β-catenin Pathway

(2018) Hyeon Jeong Lee et al.   MOLECULAR CANCER RESEARCH

APC Mutations as a Potential Biomarker for Sensitivity to Tankyrase Inhibitors in Colorectal Cancer

(2017) Noritaka Tanaka et al.   MOLECULAR CANCER THERAPEUTICS

Safety, Tolerability, and Preliminary Efficacy of the Anti-Fibrotic Small Molecule PRI-724, a CBP/β-Catenin Inhibitor, in Patients with Hepatitis C Virus-related Cirrhosis: A Single-Center, Open-Label, Dose Escalation Phase 1 Trial

(2017) Kiminori Kimura et al.   EBioMedicine

Srebp2: A master regulator of sterol and fatty acid synthesis

(2016) Blair B. Madison   JOURNAL OF LIPID RESEARCH

Wnt signaling in cancer

(2016) T Zhan et al.   ONCOGENE

Structure-Based Design of 1,4-Dibenzoylpiperazines as β-Catenin/B-Cell Lymphoma 9 Protein–Protein Interaction Inhibitors

(2016) John A. Wisniewski et al.   ACS Medicinal Chemistry Letters

Wnt directs the endosomal flux of LDL-derived cholesterol and lipid droplet homeostasis

(2015) C. C. Scott et al.   EMBO REPORTS

Rational Design of Selective Small-Molecule Inhibitors for β-Catenin/B-Cell Lymphoma 9 Protein–Protein Interactions

(2015) Logan R. Hoggard et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Altering cancer transcriptomes using epigenomic inhibitors

(2015) Malaina Gaddis et al.   Epigenetics & Chromatin

Identification of NPC1 as the target of U18666A, an inhibitor of lysosomal cholesterol export and Ebola infection

(2015) Feiran Lu et al.   eLife

The Molecular Signatures Database Hallmark Gene Set Collection

(2015) Arthur Liberzon et al.   Cell Systems

BCL9/9L-β-catenin Signaling is Associated With Poor Outcome in Colorectal Cancer

(2015) Andreas E. Moor et al.   EBioMedicine

Crosstalk between microRNA30a/b/c/d/e-5p and the Canonical Wnt Pathway: Implications for Multiple Myeloma therapy

(2014) J.-J. Zhao et al.   CANCER RESEARCH

miR-30-5p Functions as a Tumor Suppressor and Novel Therapeutic Tool by Targeting the Oncogenic Wnt/β-Catenin/BCL9 Pathway

(2014) Jian-Jun Zhao et al.   CANCER RESEARCH

Small-Molecule Inhibitors of Protein-Protein Interactions: Progressing toward the Reality

(2014) Michelle R. Arkin et al.   CHEMISTRY & BIOLOGY

Biogenesis of the multifunctional lipid droplet: Lipids, proteins, and sites

(2014) Albert Pol et al.   JOURNAL OF CELL BIOLOGY

Chemistry: Chemical con artists foil drug discovery

(2014) Jonathan Baell et al.   NATURE

Can we safely target the WNT pathway?

(2014) Michael Kahn   NATURE REVIEWS DRUG DISCOVERY

Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974

(2013) J. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Wnt/β-Catenin Signaling and Disease

(2012) Hans Clevers et al.   CELL

Drugging Wnt signalling in cancer

(2012) Paul Polakis   EMBO JOURNAL

Inhibition of oncogenic Wnt signaling through direct targeting of  -catenin

(2012) T. N. Grossmann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors

(2012) A. Gurney et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

The  -Catenin Destruction Complex

(2012) J. L. Stamos et al.   Cold Spring Harbor Perspectives in Biology

An intrinsically labile α-helix abutting the BCL9-binding site of β-catenin is required for its inhibition by carnosic acid

(2012) Marc de la Roche et al.   Nature Communications

Design of Triazole-Stapled BCL9 α-Helical Peptides to Target the β-Catenin/B-Cell CLL/lymphoma 9 (BCL9) Protein–Protein Interaction

(2011) Steven A. Kawamoto et al.   JOURNAL OF MEDICINAL CHEMISTRY

β-catenin is dynamically stored and cleared in multiple myeloma by the proteasome–aggresome–autophagosome–lysosome pathway

(2011) K Sukhdeo et al.   LEUKEMIA

Wnt signaling strength regulates normal hematopoiesis and its deregulation is involved in leukemia development

(2011) T C Luis et al.   LEUKEMIA

Bcl9/Bcl9l Are Critical for Wnt-Mediated Regulation of Stem Cell Traits in Colon Epithelium and Adenocarcinomas

(2010) J. Deka et al.   CANCER RESEARCH

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α

(2010) Curtis A Thorne et al.   Nature Chemical Biology

Lentiviral Vectors to Probe and Manipulate the Wnt Signaling Pathway

(2010) Christophe Fuerer et al.   PLoS One

Aurora kinase A is a target of Wnt/ -catenin involved in multiple myeloma disease progression

(2009) J. Dutta-Simmons et al.   BLOOD

BCL9 Promotes Tumor Progression by Conferring Enhanced Proliferative, Metastatic, and Angiogenic Properties to Cancer Cells

(2009) M. Mani et al.   CANCER RESEARCH

Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

(2009) Shih-Min A. Huang et al.   NATURE

Small molecule–mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer

(2009) Baozhi Chen et al.   Nature Chemical Biology

PrimerBank: a resource of human and mouse PCR primer pairs for gene expression detection and quantification

(2009) Athanasia Spandidos et al.   NUCLEIC ACIDS RESEARCH

Cell-Type-Specific Function of BCL9 Involves a Transcriptional Activation Domain That Synergizes with  -Catenin

(2008) C. Sustmann et al.   MOLECULAR AND CELLULAR BIOLOGY