Wnt Drug Discovery: Weaving Through the Screens, Patents and Clinical Trials

Phage Selection of Peptide Macrocycles against β-Catenin To Interfere with Wnt Signaling

(2016) Davide Bertoldo et al.   ChemMedChem

The Wnt signaling pathway in cancer

(2016) Yann Duchartre et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Cytotoxic activity of aeroplysinin-1 against colon cancer cells by promoting β-catenin degradation

(2016) Seoyoung Park et al.   FOOD AND CHEMICAL TOXICOLOGY

The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase

(2016) Ryoko Okada-Iwasaki et al.   MOLECULAR CANCER THERAPEUTICS

Visualization of a short-range Wnt gradient in the intestinal stem-cell niche

(2016) Henner F. Farin et al.   NATURE

Organoid culture systems for prostate epithelial and cancer tissue

(2016) Jarno Drost et al.   Nature Protocols

USP6 oncogene promotes Wnt signaling by deubiquitylating Frizzleds

(2016) Babita Madan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Direct Targeting of β-Catenin by a Small Molecule Stimulates Proteasomal Degradation and Suppresses Oncogenic Wnt/β-Catenin Signaling

(2016) So-Young Hwang et al.   Cell Reports

In Vitro Polarization of Colonoids to Create an Intestinal Stem Cell Compartment

(2016) Peter J. Attayek et al.   PLoS One

Cell-based assay for low- and high-scale screening of the Wnt/β-catenin signaling modulators

(2015) Maria Mazur et al.   ANALYTICAL BIOCHEMISTRY

A kinome siRNA screen identifies HGS as a potential target for liver cancers with oncogenic mutations in CTNNB1

(2015) Frédéric Canal et al.   BMC CANCER

Identification of novel osteogenic compounds by an ex-vivo sp7:luciferase zebrafish scale assay

(2015) Erik de Vrieze et al.   BONE

A Small-Molecule Antagonist of the  -Catenin/TCF4 Interaction Blocks the Self-Renewal of Cancer Stem Cells and Suppresses Tumorigenesis

(2015) L. Fang et al.   CANCER RESEARCH

Prospective Derivation of a Living Organoid Biobank of Colorectal Cancer Patients

(2015) Marc van de Wetering et al.   CELL

Structure-based Discovery of Novel Small Molecule Wnt Signaling Inhibitors by Targeting the Cysteine-rich Domain of Frizzled

(2015) Ho-Jin Lee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Pharmacophore Model for Wnt/Porcupine Inhibitors and Its Use in Drug Design

(2015) Anders Poulsen et al.   Journal of Chemical Information and Modeling

Discovery and Optimization of a Porcupine Inhibitor

(2015) Athisayamani Jeyaraj Duraiswamy et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen

(2015) Aurélie Mallinger et al.   JOURNAL OF MEDICINAL CHEMISTRY

9-Hydroxycanthin-6-one, a β-Carboline Alkaloid from Eurycoma longifolia, Is the First Wnt Signal Inhibitor through Activation of Glycogen Synthase Kinase 3β without Depending on Casein Kinase 1α

(2015) Kensuke Ohishi et al.   JOURNAL OF NATURAL PRODUCTS

Gliotoxin Inhibits Proliferation and Induces Apoptosis in Colorectal Cancer Cells

(2015) Junxiong Chen et al.   Marine Drugs

Natural product (−)-gossypol inhibits colon cancer cell growth by targeting RNA-binding protein Musashi-1

(2015) Lan Lan et al.   Molecular Oncology

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

(2015) Trevor Dale et al.   Nature Chemical Biology

Targeting the Wnt pathway in human cancers: Therapeutic targeting with a focus on OMP-54F28

(2015) Phuong N. Le et al.   PHARMACOLOGY & THERAPEUTICS

Targeting RTK Signaling Pathways in Cancer

(2015) Tarik Regad   Cancers

Drug Discovery Approaches to Target Wnt Signaling in Cancer Stem Cells

(2015)   Oncotarget

A Zebrafish Chemical Suppressor Screening Identifies Small Molecule Inhibitors of the Wnt/β-catenin Pathway

(2014) Naoyuki Nishiya et al.   CHEMISTRY & BIOLOGY

Tyrosine phosphorylation of LRP6 by Src and Fer inhibits Wnt/ -catenin signalling

(2014) Q. Chen et al.   EMBO REPORTS

Targeting the Wnt pathway in zebrafish as a screening method to identify novel therapeutic compounds

(2014) Joshua K Robertson et al.   EXPERIMENTAL BIOLOGY AND MEDICINE

Tackling the cancer stem cells — what challenges do they pose?

(2014) Diwakar R. Pattabiraman et al.   NATURE REVIEWS DRUG DISCOVERY

Molecular docking studies of flavonoids for their inhibition pattern against β-catenin and pharmacophore model generation from experimentally known flavonoids to fabricate more potent inhibitors for Wnt signaling pathway

(2014) Sajid Rashid et al.   Pharmacognosy Magazine

Huwe1-Mediated Ubiquitylation of Dishevelled Defines a Negative Feedback Loop in the Wnt Signaling Pathway

(2014) R. E. A. de Groot et al.   Science Signaling

Anti-leprosy drug clofazimine inhibits growth of triple-negative breast cancer cells via inhibition of canonical Wnt signaling

(2013) A.V. Koval et al.   BIOCHEMICAL PHARMACOLOGY

Secreted frizzled related proteins: Implications in cancers

(2013) Rohit Surana et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

Esculetin Suppresses Proliferation of Human Colon Cancer Cells by Directly Targeting  -Catenin

(2013) S.-Y. Lee et al.   Cancer Prevention Research

Indirubin-3′-Oxime Reverses Bone Loss in Ovariectomized and Hindlimb-Unloaded Mice Via Activation of the Wnt/β-Catenin Signaling

(2013) Muhammad Zahoor et al.   JOURNAL OF BONE AND MINERAL RESEARCH

Discovery of Tankyrase Inhibiting Flavones with Increased Potency and Isoenzyme Selectivity

(2013) Mohit Narwal et al.   JOURNAL OF MEDICINAL CHEMISTRY

β-Sitosterol and flavonoids isolated from Bauhinia malabarica found during screening for Wnt signaling inhibitory activity

(2013) Hyun Young Park et al.   Journal of Natural Medicines

Capture and 3D culture of colonic crypts and colonoids in a microarray platform

(2013) Yuli Wang et al.   LAB ON A CHIP

Identification and Characterization of a Small-Molecule Inhibitor of Wnt Signaling in Glioblastoma Cells

(2013) A. De Robertis et al.   MOLECULAR CANCER THERAPEUTICS

Xylogranin B: A Potent Wnt Signal Inhibitory Limonoid from Xylocarpus granatum

(2013) Kazufumi Toume et al.   ORGANIC LETTERS

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

Genomic insights into WNT/β-catenin signaling

(2013) Joseph Rosenbluh et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

High-Throughput Selectivity Assays for Small-Molecule Inhibitors of β-Catenin/T-Cell Factor Protein–Protein Interactions

(2013) Min Zhang et al.   ACS Medicinal Chemistry Letters

Selective Small Molecule Targeting β-Catenin Function Discovered by In Vivo Chemical Genetic Screen

(2013) Jijun Hao et al.   Cell Reports

Wnt/β-Catenin Signaling and Disease

(2012) Hans Clevers et al.   CELL

Platforms for high-throughput screening of Wnt/Frizzled antagonists

(2012) Alexey Koval et al.   DRUG DISCOVERY TODAY

Drugging Wnt signalling in cancer

(2012) Paul Polakis   EMBO JOURNAL

A basal gradient of Wnt and stem-cell number influences regional tumour distribution in human and mouse intestinal tracts

(2012) Simon J Leedham et al.   GUT

Comprehensive molecular characterization of human colon and rectal cancer

(2012)   NATURE

Different APC genotypes in proximal and distal sporadic colorectal cancers suggest distinct WNT/β-catenin signalling thresholds for tumourigenesis

(2012) M Christie et al.   ONCOGENE

Small Molecule-Based Promotion of PKCα-Mediated β-Catenin Degradation Suppresses the Proliferation of CRT-Positive Cancer Cells

(2012) Jungsug Gwak et al.   PLoS One

WIKI4, a Novel Inhibitor of Tankyrase and Wnt/ß-Catenin Signaling

(2012) Richard G. James et al.   PLoS One

Chemical and genetic evidence for the involvement of Wnt antagonist Dickkopf2 in regulation of glucose metabolism

(2012) X. Li 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

Targeting Wnt Pathways in Disease

(2012) Z. F. Zimmerman 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

Wnt Inhibitor Screen Reveals Iron Dependence of  -Catenin Signaling in Cancers

(2011) S. Song et al.   CANCER RESEARCH

Inhibition of Wnt/β-Catenin Signaling by p38 MAP Kinase Inhibitors Is Explained by Cross-Reactivity with Casein Kinase Iδ/ɛ

(2011) Folkert Verkaar et al.   CHEMISTRY & BIOLOGY

FluorinatedN,N-Dialkylaminostilbenes for Wnt Pathway Inhibition and Colon Cancer Repression

(2011) Wen Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Modulation of Wnt/β-catenin signaling and proliferation by a ferrous iron chelator with therapeutic efficacy in genetically engineered mouse models of cancer

(2011) G S Coombs et al.   ONCOGENE

A Systematic Screen for Micro-RNAs Regulating the Canonical Wnt Pathway

(2011) Roman Anton et al.   PLoS One

An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway

(2011) F. C. Gonsalves et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

AV-65, a novel Wnt/β-catenin signal inhibitor, successfully suppresses progression of multiple myeloma in a mouse model

(2011) H Yao et al.   Blood Cancer Journal

Identification of 2,3,6-trisubstituted quinoxaline derivatives as a Wnt2/β-catenin pathway inhibitor in non-small-cell lung cancer cell lines

(2010) Sang-Bum Lee et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evaluation of anti-Wnt/β-catenin signaling agents by pGL4-TOP transfected stable cells with a luciferase reporter system

(2010) K.A. Chuang et al.   BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH

A Useful Approach to Identify Novel Small-Molecule Inhibitors of Wnt-Dependent Transcription

(2010) K. Ewan et al.   CANCER RESEARCH

Targeting Wnt Signaling in Colon Cancer Stem Cells

(2010) E. M. F. de Sousa et al.   CLINICAL CANCER RESEARCH

Colorectal cancers show distinct mutation spectra in members of the canonical WNT signaling pathway according to their anatomical location and type of genetic instability

(2010) Cristina Albuquerque et al.   GENES CHROMOSOMES & CANCER

WLS-dependent secretion of WNT3A requires Ser209 acylation and vacuolar acidification

(2010) G. S. Coombs et al.   JOURNAL OF CELL SCIENCE

2-Methoxy-1,4-naphthoquinone isolated from Impatiens balsamina in a screening program for activity to inhibit Wnt signaling

(2010) Naomi Mori et al.   Journal of Natural Medicines

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

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

Inhibitory mechanisms of two Uncaria tomentosa extracts affecting the Wnt-signaling pathway

(2010) Carmen Magdalena Gurrola-Díaz et al.   PHYTOMEDICINE

Wnt Isoform-Specific Interactions with Coreceptor Specify Inhibition or Potentiation of Signaling by LRP6 Antibodies

(2010) Yan Gong et al.   PLoS One

Wnt Signaling, Lgr5, and Stem Cells in the Intestine and Skin

(2009) Andrea Haegebarth et al.   AMERICAN JOURNAL OF PATHOLOGY

Murrayafoline A attenuates the Wnt/β-catenin pathway by promoting the degradation of intracellular β-catenin proteins

(2009) Hyuk Choi et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

The Anti-Helminthic Niclosamide Inhibits Wnt/Frizzled1 Signaling

(2009) Minyong Chen et al.   BIOCHEMISTRY

Quercetin Inhibit Human SW480 Colon Cancer Growth in Association with Inhibition of Cyclin D1and Survivin Expression through Wnt/β-Catenin Signaling Pathway

(2009) Bao-En Shan et al.   CANCER INVESTIGATION

The Tortoise and the Hair: Slow-Cycling Cells in the Stem Cell Race

(2009) Elaine Fuchs   CELL

Vascular Endothelial Growth Factor Receptor-1 Is Synthetic Lethal to Aberrant  -Catenin Activation in Colon Cancer

(2009) S. Naik et al.   CLINICAL CANCER RESEARCH

Wnt/β-Catenin Signaling: Components, Mechanisms, and Diseases

(2009) Bryan T. MacDonald et al.   DEVELOPMENTAL CELL

Discovery and Characterization of a Small Molecule Inhibitor of the PDZ Domain of Dishevelled

(2009) David Grandy et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Drugging the Wnt Pathway: Problems And Progress

(2009) K. Garber   JNCI-Journal of the National Cancer Institute

Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

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

Proximal events in Wnt signal transduction

(2009) Stephane Angers et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Wnt signaling in development and disease

(2009) Jennifer L. Freese et al.   NEUROBIOLOGY OF DISEASE

Ethacrynic Acid Exhibits Selective Toxicity to Chronic Lymphocytic Leukemia Cells by Inhibition of the Wnt/β-Catenin Pathway

(2009) Desheng Lu et al.   PLoS One

Bruton's Tyrosine Kinase Revealed as a Negative Regulator of Wnt- -Catenin Signaling

(2009) R. G. James et al.   Science Signaling

Psammaplin A as a general activator of cell-based signaling assays via HDAC inhibition and studies on some bromotyrosine derivatives

(2008) Malcolm W.B. McCulloch et al.   BIOORGANIC & MEDICINAL CHEMISTRY

New Wnt/β-Catenin Signaling Inhibitors Isolated fromEleutherine palmifolia

(2008) Xiaofan Li et al.   Chemistry-An Asian Journal

A small-molecule inhibitor of Tcf/ -catenin signaling down-regulates PPAR  and PPAR  activities

(2008) S. Handeli et al.   MOLECULAR CANCER THERAPEUTICS