ArticlePloS one2013
Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 28 citations in OpenAlex.
- Wnt signaling in breast cancer: biological mechanisms, challenges and opportunities.Molecular cancer · 2020Review
- Pleiotropic roles of tankyrase/PARP proteins in the establishment and maintenance of human naïve pluripotency.Experimental cell research · 2020Review
- PARPs in genome stability and signal transduction: implications for cancer therapy.Biochemical Society transactions · 2018Review
- Regulation of Wnt/β-catenin signalling by tankyrase-dependent poly(ADP-ribosyl)ation and scaffolding.British journal of pharmacology · 2017Review
- The Poly(ADP-ribose) Polymerase Enzyme Tankyrase Antagonizes Activity of the β-Catenin Destruction Complex through ADP-ribosylation of Axin and APC2.The Journal of biological chemistry · 2016Article
- Identifying Family-Member-Specific Targets of Mono-ARTDs by Using a Chemical Genetics Approach.Cell reports · 2016Article
- Disruption of Wnt/β-Catenin Signaling and Telomeric Shortening Are Inextricable Consequences of Tankyrase Inhibition in Human Cells.Molecular and cellular biology · 2015Article
- Identifying Direct Protein Targets of Poly-ADP-Ribose Polymerases (PARPs) Using Engineered PARP Variants-Orthogonal Nicotinamide Adenine Dinucleotide (NAD+) Analog Pairs.Current protocols in chemical biology · 2015Article
- Small-molecule inhibitors of Wnt signaling pathway: towards novel anticancer therapeutics.Future medicinal chemistry · 2015Review
- Chemical Disruption of Wnt-dependent Cell Fate Decision-making Mechanisms in Cancer and Regenerative Medicine.Current medicinal chemistry · 2015Review
- Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors.ACS medicinal chemistry letters · 2014Article
- Tankyrases: structure, function and therapeutic implications in cancer.Current pharmaceutical design · 2014Review
- Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.ACS medicinal chemistry letters · 2013Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Recently a novel inhibitor of Wnt signaling was discovered. The compound, WIKI4, was found to act through tankyrase inhibition and regulate β-catenin levels in many cancer cell lines and human embryonic stem cells. Here we confirm that WIKI4 is a high potency tankyrase inhibitor and that it selectively inhibits tankyrases over other ARTD enzymes tested. The binding mode of the compound to tankyrase 2 was determined by protein X-ray crystallography to 2.4 Å resolution. The structure revealed a novel binding mode to the adenosine subsite of the donor NAD(+) binding groove of the catalytic domain. Our results form a structural basis for further development of potent and selective tankyrase inhibitors based on the WIKI4 scaffold.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.