Modulating the wnt signaling pathway with small molecules

Identification of small-molecule compounds targeting the dishevelled PDZ domain by virtual screening and binding studies

(2016) Jiwon Choi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Small molecule inhibitors of the Dishevelled-CXXC5 interaction are new drug candidates for bone anabolic osteoporosis therapy

(2016) H.-Y. Kim et al.   EMBO Molecular Medicine

The Poly(ADP-ribose) Polymerase Enzyme Tankyrase Antagonizes Activity of the β-Catenin Destruction Complex through ADP-ribosylation of Axin and APC2

(2016) Heather E. Croy et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Docking Screens for Novel Ligands Conferring New Biology

(2016) John J. Irwin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Experimental inhibition of porcupine-mediated Wnt O-acylation attenuates kidney fibrosis

(2016) Babita Madan et al.   KIDNEY INTERNATIONAL

Structure–activity studies of Wnt/β-catenin inhibition in the Niclosamide chemotype: Identification of derivatives with improved drug exposure

(2015) Robert A. Mook et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Silencing dishevelled-1 sensitizes paclitaxel-resistant human ovarian cancer cellsviaAKT/GSK-3β/β-catenin signalling

(2015) Kun Zhang et al.   CELL PROLIFERATION

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

Wnt addiction of genetically defined cancers reversed by PORCN inhibition

(2015) B Madan et al.   ONCOGENE

Derricin and Derricidin Inhibit Wnt/β-Catenin Signaling and Suppress Colon Cancer Cell Growth In Vitro

(2015) Barbara F. Fonseca et al.   PLoS One

Inhibition of the Tcf/beta-catenin complex increases apoptosis and impairs adrenocortical tumor cell proliferation and adrenal steroidogenesis

(2015) Letícia F. Leal et al.   Oncotarget

E7449: A dual inhibitor of PARP1/2 and tankyrase1/2 inhibits growth of DNA repair deficient tumors and antagonizes Wnt signaling

(2015) Sharon McGonigle et al.   Oncotarget

Wnt-C59 arrests stemness and suppresses growth of nasopharyngeal carcinoma in mice by inhibiting the Wnt pathway in the tumor microenvironment

(2015) Yue Cheng et al.   Oncotarget

Canonical Wnt Pathway Inhibitor ICG-001 Induces Cytotoxicity of Multiple Myeloma Cells in Wnt-Independent Manner

(2015) Eileen R. Grigson et al.   PLoS One

Intervening in β-Catenin Signaling by Sulindac Inhibits S100A4-Dependent Colon Cancer Metastasis

(2015) Ulrike Stein et al.   NEOPLASIA

Osteoblast-Specific Krm2 Overexpression and Lrp5 Deficiency Have Different Effects on Fracture Healing in Mice

(2014) Astrid Liedert et al.   PLoS One

Secreted Frizzled-related protein potentiation versus inhibition of Wnt3a/β-catenin signaling

(2013) Charles P. Xavier et al.   CELLULAR SIGNALLING

Wnt signaling in stem and cancer stem cells

(2013) Jane D Holland et al.   CURRENT OPINION IN CELL BIOLOGY

XAV939, a tankyrase 1 inhibitior, promotes cell apoptosis in neuroblastoma cell lines by inhibiting Wnt/β-catenin signaling pathway

(2013) Xiao-Hong Tian et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

The Development of Highly Potent Inhibitors for Porcupine

(2013) Xiaolei Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Sulindac sulfide inhibits sarcoendoplasmic reticulum Ca2+ATPase, induces endoplasmic reticulum stress response, and exerts toxicity in glioma cells: Relevant similarities to and important differences from celecoxib

(2013) M.C. White et al.   JOURNAL OF NEUROSCIENCE RESEARCH

Sulindac Selectively Inhibits Colon Tumor Cell Growth by Activating the cGMP/PKG Pathway to Suppress Wnt/ -Catenin Signaling

(2013) N. Li et al.   MOLECULAR CANCER THERAPEUTICS

Mutational Analysis of Sclerostin Shows Importance of the Flexible Loop and the Cystine-Knot for Wnt-Signaling Inhibition

(2013) Verena Boschert et al.   PLoS One

The Roles of Notch3 on the Cell Proliferation and Apoptosis Induced by CHIR99021 in NSCLC Cell Lines: A Functional Link between Wnt and Notch Signaling Pathways

(2013) Chunyan Li et al.   PLoS One

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

Sustained Wnt/β-Catenin Signaling Rescues High Glucose Induction of Transforming Growth Factor-β1-Mediated Renal Fibrosis

(2012) Cheng Ho et al.   AMERICAN JOURNAL OF THE MEDICAL SCIENCES

Expression of canonical WNT/β-CATENIN signaling components in the developing human lung

(2012) Mingfeng Zhang et al.   BMC DEVELOPMENTAL BIOLOGY

GSK3b-inhibitor lithium chloride enhances activation of Wnt canonical signaling and osteoblast differentiation on hydrophilic titanium surfaces

(2012) C. Galli et al.   CLINICAL ORAL IMPLANTS RESEARCH

Wnt/beta-Catenin Signaling and Small Molecule Inhibitors

(2012) Andrey Voronkov et al.   CURRENT PHARMACEUTICAL DESIGN

Three decades of Wnts: a personal perspective on how a scientific field developed

(2012) Roel Nusse et al.   EMBO JOURNAL

Characterization of the Interaction of Sclerostin with the Low Density Lipoprotein Receptor-related Protein (LRP) Family of Wnt Co-receptors

(2012) Gill Holdsworth et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Wnt Signaling and Injury Repair

(2012) J. L. Whyte 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

Inhibition of glycogen synthase kinase 3  induces dermal fibrosis by activation of the canonical Wnt pathway

(2011) C. Bergmann et al.   ANNALS OF THE RHEUMATIC DISEASES

Antihelminth Compound Niclosamide Downregulates Wnt Signaling and Elicits Antitumor Responses in Tumors with Activating APC Mutations

(2011) T. Osada et al.   CANCER RESEARCH

Synthesis of Potent Dishevelled PDZ Domain Inhibitors Guided by Virtual Screening and NMR Studies

(2011) Jufang Shan et al.   Chemical Biology & Drug Design

Ubiquitin Ligase RNF146 Regulates Tankyrase and Axin to Promote Wnt Signaling

(2011) Marinella G. Callow et al.   PLoS One

Identification of Transmembrane Protein 88 (TMEM88) as a Dishevelled-binding Protein

(2010) Ho-Jin Lee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Pyrvinium, a Potent Small Molecule Wnt Inhibitor, Promotes Wound Repair and Post-MI Cardiac Remodeling

(2010) Sarika Saraswati et al.   PLoS One

Inhibition of Wnt/ -catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis

(2010) W. R. Henderson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Sulindac Inhibits Canonical Wnt Signaling by Blocking the PDZ Domain of the Protein Dishevelled

(2009) Ho-Jin Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Identification of tripeptides recognized by the PDZ domain of Dishevelled

(2009) Ho-Jin Lee et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Chemical and Structural Biology to Direct the Repurposing of Sulindac

(2009) Jeffrey R. Simard et al.   ChemMedChem

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

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

Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

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

Wnt/ -Catenin Signaling Contributes to Activation of Normal and Tumorigenic Liver Progenitor Cells

(2008) W. Yang et al.   CANCER RESEARCH

Optimizing Dvl PDZ domain inhibitor by exploring chemical space

(2008) Jufang Shan et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Targeted Disruption of the Wnt Regulator Kremen Induces Limb Defects and High Bone Density

(2008) K. Ellwanger et al.   MOLECULAR AND CELLULAR BIOLOGY

The role of Wnt signaling in neuronal dysfunction in Alzheimer's Disease

(2008) Nibaldo C Inestrosa et al.   Molecular Neurodegeneration