ArticleJournal of medicinal chemistry2020
Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.
Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 41 citations in OpenAlex.
- Antitumor activity and structure-activity relationship of poly (ADP-ribose) polymerase (PARP)-based dual inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2026Review
- Replacement soaking for human tankyrase 2 enables studies on substrate analogues and inhibitors.Acta crystallographica. Section D, Structural biology · 2026Article
- Development of di-arylated 1,2,4-triazole-based derivatives as therapeutic agents against breast cancer: synthesis and biological evaluation.RSC medicinal chemistry · 2024Article
- Catalytic Asymmetric Synthesis of AtropisomericThe Journal of organic chemistry · 2023Article
- High-throughput determination of enantiopurity in atroposelective synthesis of aryl triazoles.Chemical science · 2023Article
- Synthesis and Cytotoxic Activity of 1,2,4-Triazolo-LinkedMolecules (Basel, Switzerland) · 2022Article
- The Tankyrase Inhibitor OM-153 Demonstrates Antitumor Efficacy and a Therapeutic Window in Mouse Models.Cancer research communications · 2022Article
- The zinc-binding motif in tankyrases is required for the structural integrity of the catalytic ADP-ribosyltransferase domain.Open biology · 2022Article
- Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II.Journal of medicinal chemistry · 2021Article
- WNT as a Driver and Dependency in Cancer.Cancer discovery · 2021Review
- Identification of response signatures for tankyrase inhibitor treatment in tumor cell lines.iScience · 2021Article
- Tankyrases as modulators of pro-tumoral functions: molecular insights and therapeutic opportunities.Journal of experimental & clinical cancer research : CR · 2021Review
- Bioinformatic Analysis of the Nicotinamide Binding Site in Poly(ADP-Ribose) Polymerase Family Proteins.Cancers · 2021Article
- A Small-Molecule Tankyrase Inhibitor Reduces Glioma Stem Cell Proliferation and Sphere Formation.Cancers · 2020Article
Corrections and comments
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Authors and funding
14 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tankyrases 1 and 2 are central biotargets in the WNT/β-catenin signaling and Hippo signaling pathways. We have previously developed tankyrase inhibitors bearing a 1,2,4-triazole moiety and binding predominantly to the adenosine binding site of the tankyrase catalytic domain. Here we describe a systematic structure-guided lead optimization approach of these tankyrase inhibitors. The central 1,2,4-triazole template and
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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.