A novel tankyrase inhibitor decreases canonical Wnt signaling in colon carcinoma cells and reduces tumor growth in conditional APC mutant mice.

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Cancer Research

• Publication date

  2012-03-22

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1158/0008-5472.CAN-11-3336PMID 22440753
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Wnt signaling in stem and cancer stem cells.

  2013cited by this paper
• [1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.

  2012cited by this paper
• Structural basis of selective inhibition of human tankyrases.

  2012cited by this paper
• The intestinal stem cell signature identifies colorectal cancer stem cells and predicts disease relapse.

  2011cited by this paper
• Regulation of β‐Catenin Nuclear Dynamics by GSK‐3β Involves a LEF‐1 Positive Feedback Loop

  2011cited by this paper
• Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth.

  2011cited by this paper
• Subcellular Spatial Regulation of Canonical Wnt Signaling at the Primary Cilium

  2011cited by this paper
• Ubiquitin Ligase RNF146 Regulates Tankyrase and Axin to Promote Wnt Signaling

  2011cited by this paper
• RNF146 is a poly(ADP-ribose)-directed E3 ligase that regulates axin degradation and Wnt signalling

  2011cited by this paper
• New avenues to target Wnt/β-catenin signaling.

  2011cited by this paper
• Wnt signaling and colon carcinogenesis: Beyond APC

  2011cited by this paper
• O2 regulates stem cells through Wnt/β-catenin signalling

  2010cited by this paper
• Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α.

  2010cited by this paper
• Drug Discovery Approaches to Target Wnt Signaling in Cancer Stem Cells

  2010cited by this paper
• Interaction between human-breast cancer metastasis and bone microenvironment through activated hepatocyte growth factor/Met and beta-catenin/Wnt pathways.

  2010cited by this paper
• Interplay of cadherin-mediated cell adhesion and canonical Wnt signaling.

  2010cited by this paper
• Wnt signaling in stem and cancer stem cells.

  2010cited by this paper
• 2,4-Diamino-quinazolines as inhibitors of beta-catenin/Tcf-4 pathway: Potential treatment for colorectal cancer.

  2009cited by this paper
• The anti-helminthic niclosamide inhibits Wnt/Frizzled1 signaling.

  2009cited by this paper
• Wnt/beta-catenin signaling: components, mechanisms, and diseases.

  2009cited by this paper
• A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation.

  2009cited by this paper
• PARsing the phrase "all in for Axin"- Wnt pathway targets in cancer.

  2009cited by this paper
• Crypt stem cells as the cells-of-origin of intestinal cancer

  2009cited by this paper
• Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

  2009influential reference
• Genetic interaction of PGE2 and Wnt signaling regulates developmental specification of stem cells and regeneration.

  2009cited by this paper
• Tankyrase function at telomeres, spindle poles, and beyond.

  2008influential reference
• Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer

  2008cited by this paper
• Identification of stem cells in small intestine and colon by marker gene Lgr5

  2007cited by this paper
• Mining the Wnt pathway for cancer therapeutics

  2007cited by this paper
• Gli1 acts through Snail and E-cadherin to promote nuclear signaling by beta-catenin.

  2007cited by this paper
• Correlations between mutation site in APC and phenotype of familial adenomatous polyposis (FAP): a review of the literature.

  2007cited by this paper
• Adenomatous polyposis coli (APC) differentially regulates beta-catenin phosphorylation and ubiquitination in colon cancer cells.

  2006cited by this paper
• Mitotic phosphorylation of tankyrase, a PARP that promotes spindle assembly, by GSK3.

  2006influential reference
• Wnt/beta-catenin signaling in development and disease.

  2006cited by this paper
• Adenomatous Polyposis Coli (APC) Is Required for Normal Development of Skin and Thymus

  2006cited by this paper
• β-Catenin destruction complex: insights and questions from a structural perspective

  2006influential reference
• Adenomatous Polyposis Coli (APC) Differentially Regulates β-Catenin Phosphorylation and Ubiquitination in Colon Cancer Cells*

  2006cited by this paper
• Identification of a specific inhibitor of the dishevelled PDZ domain.

  2005cited by this paper
• Quercetin, a potent inhibitor against beta-catenin/Tcf signaling in SW480 colon cancer cells.

  2005cited by this paper
• Small-molecule antagonists of the oncogenic Tcf/beta-catenin protein complex.

  2004cited by this paper
• Epigenetic inactivation of SFRP genes allows constitutive WNT signaling in colorectal cancer

  2004cited by this paper
• A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected].

  2004cited by this paper
• Small-molecule antagonists of the oncogenic Tcf/β-catenin protein complex

  2004cited by this paper
• A small molecule inhibitor of -cateninCREB-binding protein transcription

  2004cited by this paper
• Phosphorylation of β-Catenin at S33, S37, or T41 Can Occur in the Absence of Phosphorylation at T45 in Colon Cancer Cells

  2003cited by this paper
• Phosphorylation of beta-catenin at S33, S37, or T41 can occur in the absence of phosphorylation at T45 in colon cancer cells.

  2003cited by this paper
• Molecular targets of lithium action

  2003influential reference
• Molecular targets of lithium action.

  2003cited by this paper
• Control of beta-catenin phosphorylation/degradation by a dual-kinase mechanism.

  2002cited by this paper
• The beta-catenin/TCF-4 complex imposes a crypt progenitor phenotype on colorectal cancer cells.

  2002cited by this paper
• Control of -Catenin Phosphorylation/Degradation by a Dual-Kinase Mechanism

  2002cited by this paper
• Faculty Opinions recommendation of Beta-catenin and TCF mediate cell positioning in the intestinal epithelium by controlling the expression of EphB/ephrinB.

  2002cited by this paper
• Development of High Throughput Screening Assays Using Fluorescence Polarization: Nuclear Receptor-Ligand-Binding and Kinase/Phosphatase Assays

  2000cited by this paper
• The SCFbeta-TRCP-ubiquitin ligase complex associates specifically with phosphorylated destruction motifs in IkappaBalpha and beta-catenin and stimulates IkappaBalpha ubiquitination in vitro.

  1999cited by this paper
• Beta-catenin regulates expression of cyclin D1 in colon carcinoma cells.

  1999cited by this paper
• The SCFβ-TRCP–ubiquitin ligase complex associates specifically with phosphorylated destruction motifs in IκBα and β-catenin and stimulates IκBα ubiquitination in vitro

  1999cited by this paper
• Downregulation of beta-catenin by human Axin and its association with the APC tumor suppressor, beta-catenin and GSK3 beta.

  1998influential reference
• Downregulation of β-catenin by human Axin and its association with the APC tumor suppressor, β-catenin and GSK3β

  1998cited by this paper
• A dominant mutation that predisposes to multiple intestinal neoplasia in the mouse.

  1990cited by this paper

• A nuclear isoform of hydroxyacyl-COA dehydrogenase inhibits tumor progression in colorectal cancer

  2026cites this paper
• Roles of ADP-Ribosyltransferases in Cancer

  2026cites this paper
• Tankyrases and Their Binding Proteins: Origins of Their Roles in Diverse Cellular Pathways.

  2026cites this paper
• Synthesis of triazolopyrimidinone- and imidazotriazinone-based tankyrase inhibitors: Identification of Basroparib (STP1002) as a clinical candidate.

  2026cites this paper
• Cancer Stem Cells in Human Gastrointestinal and Hepatic Cancers

  2025cites this paper
• Unveiling the potential of tankyrase I inhibitors for the treatment of type 2 diabetes mellitus: A hybrid approach using network pharmacology, 2D structural similarity, molecular docking, MD simulation and in-vitro studies.

  2025cites this paper
• A potent and selective TNKS2 inhibitor for tumor-selective WNT suppression

  2025cites this paper
• A Review of Potential Agents for Colon Cancer Interception in FAP Patients: Evidence from Preclinical Studies in APCMin/+ Mice

  2025cites this paper
• Emerging regulatory mechanisms and functions of biomolecular condensates: implications for therapeutic targets

  2025cites this paper
• Tankyrase activity is essential for asymmetric division and chromosome segregation in oocyte meiosis.

  2025cites this paper
• In Silico and In Vitro Analyses of Strawberry-Derived Extracts in Relation to Key Compounds’ Metabolic and Anti-Tumor Effects

  2025cites this paper
• SALL2-Mediated Suppression of WNT Signaling Through Transcriptional Control of AXIN2 in Colorectal Cancer Cells

  2025cites this paper
• A machine learning-Assisted QSAR and integrative computational combined with network pharmacology approach for rational identification of tankyrase inhibitors in colon adenocarcinoma

  2025cites this paper
• CRC management: Emerging trends in early detection, diagnosis, biomarkers, treatment, and prevention.

  2025cites this paper
• Wnt signaling pathways in biology and disease: mechanisms and therapeutic advances

  2025cites this paper
• Thiourea compounds as multifaceted bioactive agents in medicinal chemistry.

  2025cites this paper
• Wnt/β-Catenin Signaling Regulates Hepatitis B Virus cccDNA Levels

  2025cites this paper
• JPI-547, a Dual Inhibitor of PARP/Tankyrase, Shows Antitumor Activity Against Pancreatic Cancers with Homologous Recombination Repair Deficiency or Wnt-Addiction

  2025cites this paper
• WNT signaling in cancer: molecular mechanisms and potential therapies

  2025cites this paper
• Understanding Tankyrase Inhibitors and Their Role in the Management of Different Cancer.

  2025cites this paper
• Structural stability-guided scaffold hopping and computational modeling of tankyrase inhibitors targeting colorectal cancer

  2025cites this paper
• The involvement of the Wnt/β-catenin signaling cascade in fibrosis progression and its therapeutic targeting by relaxin.

  2024cites this paper
• Signaling pathways in colorectal cancer: implications for the target therapies

  2024cites this paper
• Development of a new flippase-dependent mouse model for red fluorescence-based isolation of KrasG12D oncogene-expressing tumor cells

  2024cites this paper
• Unlocking longevity: the role of telomeres and its targeting interventions

  2024cites this paper
• Regulation of PARP1/2 and the tankyrases: emerging parallels.

  2024cites this paper
• Identification of Honokiol‐Based Scaffold to Design Tankyrase 1/2 Inhibitors by In Silico and In Vitro Studies

  2024cites this paper
• Targeting ErbB and tankyrase1/2 prevent the emergence of drug-tolerant persister cells in ALK-positive lung cancer

  2024cites this paper
• Tankyrase1/2 inhibitor XAV-939 reverts EMT and suggests that PARylation partially regulates aerobic activities in human hepatocytes and HepG2 cells.

  2024cites this paper
• Wnt/β-catenin signaling pathway in carcinogenesis and cancer therapy

  2024cites this paper
• APC/PIK3CA mutations and β-catenin status predict tankyrase inhibitor sensitivity of patient-derived colorectal cancer cells

  2023cites this paper
• Targeting Transcription Factors in Cancer: From "Undruggable" to "Druggable".

  2023cites this paper
• A New Wave of Targeting ‘Undruggable’ Wnt Signaling for Cancer Therapy: Challenges and Opportunities

  2023cites this paper
• Tankyrase: a promising therapeutic target with pleiotropic action

  2023cites this paper
• Wnt/β-Catenin Signaling Pathway in the Development and Progression of Colorectal Cancer

  2023cites this paper
• RSPO2 as Wnt signaling enabler: Important roles in cancer development and therapeutic opportunities

  2023cites this paper
• The Role of WNT Pathway Mutations in Cancer Development and an Overview of Therapeutic Options

  2023cites this paper
• A novel TNKS/USP25 inhibitor blocks the Wnt pathway to overcome multi-drug resistance in TNKS-overexpressing colorectal cancer

  2023cites this paper
• Precision medicine in nasopharyngeal carcinoma: comprehensive review of past, present, and future prospect

  2023cites this paper
• Signaling pathways and their potential therapeutic utility in esophageal squamous cell carcinoma

  2022cites this paper
• The Tankyrase Inhibitor OM-153 Demonstrates Antitumor Efficacy and a Therapeutic Window in Mouse Models

  2022cites this paper
• Telomerase in Cancer: Function, Regulation, and Clinical Translation

  2022cites this paper
• Discovery of 2-(isoxazol-5-yl)phenyl 3,4-dihydroxybenzoate as a potential inhibitor for the Wnt/β-catenin pathway.

  2022cites this paper
• Clinical significancy of WNT pathway inhibition in various cancers

  2022cites this paper
• Biologically Active 2-oxazolidinone Derivatives beyond Antibacterial Activities.

  2022cites this paper
• Deubiquitination of TNKS1 Regulates Wnt/β-Catenin to Affect the Expression of USP25 to Promote the Progression of Glioma

  2022cites this paper
• Talaverrucin A, Heterodimeric Oxaphenalenone from Antarctica Sponge-Derived Fungus Talaromyces sp. HDN151403, Inhibits Wnt/β-Catenin Signaling Pathway.

  2022cites this paper
• Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer.

  2022cites this paper
• β-Catenin signaling in hepatocellular carcinoma

  2022cites this paper
• Molecular mechanisms of Wnt/β-catenin activation in HCC

  2022cites this paper
• Stabilizing and upregulating Axin with tankyrase inhibitor reverses 5-fluorouracil chemoresistance and proliferation by targeting the WNT/caveolin-1 axis in colorectal cancer cells

  2022cites this paper
• Molecular Patterns Based on Immunogenomic Signatures Stratify the Prognosis of Colon Cancer

  2022cites this paper
• Tankyrase-selective inhibitor STP1002 shows preclinical antitumour efficacy without on-target toxicity in the gastrointestinal tract.

  2022cites this paper
• Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

  2021cites this paper
• Interplay between ADP-ribosyltransferases and essential cell signaling pathways controls cellular responses

  2021cites this paper
• 1 Cell Permeable Stapled Peptide Inhibitor of Wnt Signaling that Targets β-Catenin Protein ‒ Protein Interactions

  2021cites this paper
• Modulating undruggable targets to overcome cancer therapy resistance.

  2021cites this paper
• The Wnt signaling pathway in tumorigenesis, pharmacological targets, and drug development for cancer therapy

  2021cites this paper
• Inhibition of Wnt/β-Catenin Signaling Sensitizes Esophageal Cancer Cells to Chemoradiotherapy

  2021cites this paper
• The Adenoviral E1B-55k Protein Present in HEK293 Cells Mediates Abnormal Accumulation of Key WNT Signaling Proteins in Large Cytoplasmic Aggregates

  2021cites this paper
• Optimization of a Screening Hit toward M2912, an Oral Tankyrase Inhibitor with Antitumor Activity in Colorectal Cancer Models.

  2021cites this paper
• Wnt/β-catenin signaling pathway in uterine leiomyoma: role in tumor biology and targeting opportunities

  2021cites this paper
• Discovery of 1-Benzoyl 4-Phenoxypiperidines as Small-Molecule Inhibitors of the β-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction.

  2021cites this paper
• Wnt/β-catenin signaling in cancers and targeted therapies

  2021cites this paper
• Small-Molecule Inhibitors Targeting the Canonical WNT Signaling Pathway for the Treatment of Cancer.

  2021cites this paper
• Mild hyperthermia-enhanced chemo-photothermal synergistic therapy using doxorubicin-loaded gold nanovesicles

  2021cites this paper
• Identification of response signatures for tankyrase inhibitor treatment in tumor cell lines

  2021cites this paper
• Potential Role of Traditional Chinese Medicines by Wnt/β-Catenin Pathway Compared With Targeted Small Molecules in Colorectal Cancer Therapy

  2021cites this paper
• A perspective on medicinal chemistry approaches towards adenomatous polyposis coli and Wnt signal based colorectal cancer inhibitors.

  2021cites this paper
• Tankyrase inhibitors as antitumor agents: a patent update (2013 – 2020)

  2021cites this paper
• Babao Dan (八宝丹) Alleviates 5-Fluorouracil-Induced Intestinal Damage via Wnt/β-Catenin Pathway

  2021cites this paper
• Meta-Analysis and Systematic Review of the Genomics of Mucosal Melanoma

  2021cites this paper
• Evaluation of AXIN1 and AXIN2 as targets of tankyrase inhibition in hepatocellular carcinoma cell lines

  2021cites this paper
• Bioactivity Studies of Hesperidin and XAV939

  2021cites this paper
• Tankyrase Inhibitor for Cardiac Tissue Regeneration: an In-silico Approach

  2021cites this paper
• The multidimensional role of the Wnt/β‐catenin signaling pathway in human malignancies

  2021cites this paper
• Blocking Wnt/β-catenin Signal Amplifies Anti-PD-1 Therapeutic Efficacy by Inhibiting Tumor Growth, Migration, and Promoting Immune Infiltration in Glioblastomas

  2021cites this paper
• Novel Small Molecules against Two Binding Sites of Wnt2 Protein as potential Drug Candidates for Colorectal Cancer: A Structure Based Virtual Screening Approach

  2020cites this paper
• Nanoparticles (NPs)‐Meditated LncRNA AFAP1‐AS1 Silencing to Block Wnt/β‐Catenin Signaling Pathway for Synergistic Reversal of Radioresistance and Effective Cancer Radiotherapy

  2020cites this paper
• Targeting Wnt/β-Catenin Pathway for Drug Therapy

  2020cites this paper
• A Small-Molecule Tankyrase Inhibitor Reduces Glioma Stem Cell Proliferation and Sphere Formation

  2020cites this paper
• Phase Ib Study of Wnt Inhibitor Ipafricept with Gemcitabine and nab-paclitaxel in Patients with Previously Untreated Stage IV Pancreatic Cancer

  2020cites this paper
• Significance of STAT3 in Immune Infiltration and Drug Response in Cancer

  2020cites this paper
• Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor

  2020cites this paper
• Asparagine Hydroxylation is a Reversible Post-translational Modification

  2020cites this paper
• Discovery of Novel Inhibitor for WNT/β-Catenin Pathway by Tankyrase 1/2 Structure-Based Virtual Screening

  2020cites this paper
• Wnt signaling pathway in aging-related tissue fibrosis and therapies.

  2020cites this paper
• Somatic tissue engineering in mouse models reveals an actionable role for WNT pathway alterations in prostate cancer metastasis.

  2020cites this paper
• Transcriptional Regulation of Wnt/β-Catenin Pathway in Colorectal Cancer

  2020cites this paper
• Asparagine hydroxylation is likely to be a reversible post-translational modification

  2020cites this paper
• Role of fibroblast growth factor 4 in the growth and metastasis of colorectal cancer.

  2020cites this paper
• New insights into the core Hippo signaling and biological macromolecules interactions in the biology of solid tumors.

  2020cites this paper
• GHR, PEX5 AND AXIN2 ARE NEW TARGETS FOR MIR-195 IN- VOLVING IN LONGEVITY, INCREASING BIOLOGICAL ACTIVI- TIES AND EMT OF CANCER CELLS FOR HEPATOCELLULAR CARCINOMA CELLS

  2020cites this paper
• Tankyrase inhibition sensitizes melanoma to PD-1 immune checkpoint blockade in syngeneic mouse models

  2020cites this paper
• Antitumor Activity of Indole-3-carbinol in Breast Cancer Cells: Phenotype, Genetic Pattern, and DNA Methylation Inversion

  2020cites this paper
• Potential Telomere-Related Pharmacological Targets.

  2020cites this paper
• Zoning in on Tankyrases: A Brief Review on the Past, Present and Prospective Studies.

  2020cites this paper
• Novel tankyrase inhibitors suppress TDP-43 aggregate formation.

  2020cites this paper
• Targeting Wnt Signaling for Gastrointestinal Cancer Therapy: Present and Evolving Views

  2020cites this paper
• Targeting the Wnt/β-catenin signaling pathway in cancer

  2020cites this paper