ArticleBioorganic & medicinal chemistry2017
A fragment-based approach leading to the discovery of a novel binding site and the selective CK2 inhibitor CAM4066.
Article in Bioorganic & medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed.
- Selective Inhibition of CK2: Emerging Strategies and Future Directions.Journal of medicinal chemistry · 2026Review
- Targeting Human Protein Kinase CK2 by a Library of Indeno[1,2-b]Indoles: Contribution of Thermal Shift Assay to Pre-Screening and Co-Crystallization to Post-Screening.Archiv der Pharmazie · 2026Article
- Probing Allosteric Kinase Modulators as Next Game-Changers in Fighting Neurodegeneration.Journal of medicinal chemistry · 2026Review
- Discovery of BMS-159, an Orally Active Imidazotriazine Pan-CK2 Inhibitor for the Treatment of Cancer.ACS medicinal chemistry letters · 2026Article
- An Integrative Computational Pipeline for CK2 Inhibitor Discovery in Triple-Negative Breast Cancer Using Virtual Screening, Molecular Dynamics, Machine Learning, and Density Functional Theory.Pharmaceuticals (Basel, Switzerland) · 2026Article
- 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
- Recent Advances in the Discovery of CK2 Inhibitors.ACS omega · 2024Review
- 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
- 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
- Alternaria toxins as casein kinase 2 inhibitors and possible consequences for estrogenicity: a hybrid in silico/in vitro study.Archives of toxicology · 2020Article
- Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion.Chemical science · 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
- Review
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Authors and funding
7 authors.
Funding
Abstract
Recently we reported the discovery of a potent and selective CK2α inhibitor CAM4066. This compound inhibits CK2 activity by exploiting a pocket located outside the ATP binding site (αD pocket). Here we describe in detail the journey that led to the discovery of CAM4066 using the challenging fragment linking strategy. Specifically, we aimed to develop inhibitors by linking a high-affinity fragment anchored in the αD site to a weakly binding warhead fragment occupying the ATP site. Moreover, we describe the remarkable impact that molecular modelling had on the development of this novel chemical tool. The work described herein shows potential for the development of a novel class of CK2 inhibitors.
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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.