ArticleBiological research2018
The tankyrase inhibitor G007-LK inhibits small intestine LGR5
Article in Biological research, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Wnt/β-Catenin Signaling Regulates Hepatitis B Virus cccDNA Levels.International journal of molecular sciences · 2025Article
- Rare histologic transformation of a CTNNB1 (β-catenin) mutated prostate cancer with aggressive clinical course.Diagnostic pathology · 2024Article
- A Mouse Model for the Rapid and Binomial Assessment of Putative WNT/β-Catenin Signalling Inhibitors.Biomedicines · 2023Article
- Wnt Signaling Inhibitors and Their Promising Role in Tumor Treatment.International journal of molecular sciences · 2023Review
- Blocking the Wnt/β‑catenin signaling pathway to treat colorectal cancer: Strategies to improve current therapies (Review).International journal of oncology · 2023Review
- The Tankyrase Inhibitor OM-153 Demonstrates Antitumor Efficacy and a Therapeutic Window in Mouse Models.Cancer research communications · 2022Article
- Tankyrases as modulators of pro-tumoral functions: molecular insights and therapeutic opportunities.Journal of experimental & clinical cancer research : CR · 2021Review
- The dual pocket binding novel tankyrase inhibitor K-476 enhances the efficacy of immune checkpoint inhibitor by attracting CD8American journal of cancer research · 2021Article
- Tankyrase inhibition ameliorates lipid disorder via suppression of PGC-1α PARylation in db/db mice.International journal of obesity (2005) · 2020Article
- Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.Journal of medicinal chemistry · 2020Article
- Tankyrase inhibition sensitizes melanoma to PD-1 immune checkpoint blockade in syngeneic mouse models.Communications biology · 2020Article
- Fragment-based screening identifies molecules targeting the substrate-binding ankyrin repeat domains of tankyrase.Scientific reports · 2019Article
- Distinct Colorectal Cancer-Associated APC Mutations Dictate Response to Tankyrase Inhibition.Cancer discovery · 2019Article
- Poly(ADP-ribose)-dependent ubiquitination and its clinical implications.Biochemical pharmacology · 2019Review
- Tankyrase inhibition sensitizes cells to CDK4 blockade.PloS one · 2019Article
- The Effect of Wnt Pathway Modulators on Human iPSC-Derived Pancreatic Beta Cell Maturation.Frontiers in endocrinology · 2019Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
backgroundThe WNT pathway regulates intestinal stem cells and is frequently disrupted in intestinal adenomas. The pathway contains several potential biotargets for interference, including the poly-ADP ribosyltransferase enzymes tankyrase1 and 2. LGR5 is a known WNT pathway target gene and marker of intestinal stem cells. The LGR5
resultsWe treated Lgr5-EGFP-Ires-CreERT2;R26R-Confetti mice with the tankyrase inhibitor G007-LK for up to 3 weeks to assess the effect on duodenal stem cell homeostasis and on the integrity of intestinal epithelium. At the administered doses, G007-LK treatment inhibited WNT signalling in LGR5
conclusionWe show that the tankyrase inhibitor G007-LK is well tolerated by the mice, although proliferation of the LGR5
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