ArticleChemical science2016
Specific inhibition of CK2α from an anchor outside the active site.
Article in Chemical science, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
What it found
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The trial behind it
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Who cites it
32 citing papers in PubMed, 71 citations in OpenAlex.
- Selective Inhibition of CK2: Emerging Strategies and Future Directions.Journal of medicinal chemistry · 2026Review
- Probing Allosteric Kinase Modulators as Next Game-Changers in Fighting Neurodegeneration.Journal of medicinal chemistry · 2026Review
- Towards the targeted protein degradation of CK2: design and synthesis of CAM4066-based PROTACs.Beilstein journal of organic chemistry · 2026Article
- Exploiting the Cryptic αD Pocket of Casein Kinase 2α (CK2α) to Deliver Highly Potent and Selective Type 1 Inhibitors.Journal of medicinal chemistry · 2025Article
- Targeting Casein Kinase 2 and Histone Deacetylase with a Dual Inhibitor Effectively Reduces Tumor Growth in a Triple-Negative Breast Cancer Xenograft Model.ACS pharmacology & translational science · 2025Article
- Recent Advances in the Discovery of CK2 Inhibitors.ACS omega · 2024Review
- Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors.Nature chemical biology · 2024Article
- Scoping Pleiotropy of CK2 in Musculoskeletal Disorders for a Novel Targeting Approach.Kinases and phosphatases · 2024Article
- Cancer selective cell death induction by a bivalent CK2 inhibitor targeting the ATP site and the allosteric αD pocket.iScience · 2024Article
- CK2 Chemical Probes: Past, Present, and Future.Kinases and phosphatases · 2023Article
- A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action.RSC medicinal chemistry · 2022Article
- Crystal structure of the Rho-associated coiled-coil kinase 2 inhibitor belumosudil bound to CK2α.Acta crystallographica. Section F, Structural biology communications · 2022Article
- Development of small cyclic peptides targeting the CK2α/β interface.Chemical communications (Cambridge, England) · 2022Article
- Mechanism of CK2 Inhibition by a Ruthenium-Based Polyoxometalate.Frontiers in molecular biosciences · 2022Article
- Targeting Protein Kinases in Blood Cancer: Focusing on CK1α and CK2.International journal of molecular sciences · 2021Review
- Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study.Molecules (Basel, Switzerland) · 2021Review
- Proposed Allosteric Inhibitors Bind to the ATP Site of CK2α.Journal of medicinal chemistry · 2020Article
- Recent Advances in the Discovery of CK2 Allosteric Inhibitors: From Traditional Screening to Structure-Based Design.Molecules (Basel, Switzerland) · 2020Review
- Identification and Biological Evaluation of CK2 Allosteric Fragments through Structure-Based Virtual Screening.Molecules (Basel, Switzerland) · 2020Article
- Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors.Scientific reports · 2019Article
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
The development of selective inhibitors of protein kinases is challenging because of the significant conservation of the ATP binding site. Here, we describe a new mechanism by which the protein kinase CK2α can be selectively inhibited using features outside the ATP site. We have identified a new binding site for small molecules on CK2α adjacent to the ATP site and behind the αD loop, termed the αD pocket. An elaborated fragment anchored in this site has been linked with a low affinity fragment binding in the ATP site, creating a novel and selective inhibitor (CAM4066) that binds CK2α with a
Identifiers
What OpenQuestion holds
Registered trials
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.