ArticleJournal of medicinal chemistry2017
Inhibitory Kappa B Kinase α (IKKα) Inhibitors That Recapitulate Their Selectivity in Cells against Isoform-Related Biomarkers.
Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
22 citing papers in PubMed, 36 citations in OpenAlex.
- Differential Effects of a First-in-Class IKKCalcified tissue international · 2026Article
- The roles of IKKα in normal physiology and cancer.Cell communication and signaling : CCS · 2026Review
- Double trouble: cytosolic and nuclear IKKα in cancer.Open biology · 2025Review
- Investigating Natural Product Inhibitors of IKKα: Insights from Integrative In Silico and Experimental Validation.Molecules (Basel, Switzerland) · 2025Article
- Synthesis of electrophile-tethered preQBeilstein journal of organic chemistry · 2025Article
- The path less traveled: the non-canonical NF-κB pathway in systemic lupus erythematosus.Frontiers in immunology · 2025Review
- Defective kinase activity of IKKα leads to combined immunodeficiency and disruption of immune tolerance in humans.Nature communications · 2024Article
- Design and Synthesis of Novel Aminoindazole-pyrrolo[2,3-Molecules (Basel, Switzerland) · 2024Article
- Cimicifugoside H-2 as an Inhibitor of IKK1/Alpha: A Molecular Docking and Dynamic Simulation Study.Biomolecules · 2024Article
- NFκB signalling in colorectal cancer: Examining the central dogma of IKKα and IKKβ signalling.Heliyon · 2024Review
- The allure of targets for novel drugs.RSC medicinal chemistry · 2024Review
- Synthesis and Structure Elucidation of Glutamyl-Queuosine.Journal of the American Chemical Society · 2023Article
- Spatial expression of IKK-alpha is associated with a differential mutational landscape and survival in primary colorectal cancer.British journal of cancer · 2022Article
- Review
- Inhibitory feedback control of NF-κB signalling in health and disease.The Biochemical journal · 2021Review
- Regulation of Bcl-XL by non-canonical NF-κB in the context of CD40-induced drug resistance in CLL.Cell death and differentiation · 2021Article
- Review
- Targeting TRAF3IP2, Compared to Rab27, is More Effective in Suppressing the Development and Metastasis of Breast Cancer.Scientific reports · 2020Article
- Targeting IKKα kinase to prevent tumor progression and therapy resistance.Cancer drug resistance (Alhambra, Calif.) · 2020Review
- Inhibitory-κB Kinase (IKK) α and Nuclear Factor-κB (NFκB)-Inducing Kinase (NIK) as Anti-Cancer Drug Targets.Cells · 2018Review
Corrections and comments
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Authors and funding
24 authors at 2 institutions in 1 country.
Funding
Abstract
IKKβ plays a central role in the canonical NF-kB pathway, which has been extensively characterized. The role of IKKα in the noncanonical NF-kB pathway, and indeed in the canonical pathway as a complex with IKKβ, is less well understood. One major reason for this is the absence of chemical tools designed as selective inhibitors for IKKα over IKKβ. Herein, we report for the first time a series of novel, potent, and selective inhibitors of IKKα. We demonstrate effective target engagement and selectivity with IKKα in U2OS cells through inhibition of IKKα-driven p100 phosphorylation in the noncanonical NF-kB pathway without affecting IKKβ-dependent IKappa-Bα loss in the canonical pathway. These compounds represent the first chemical tools that can be used to further characterize the role of IKKα in cellular signaling, to dissect this from IKKβ and to validate it in its own right as a target in inflammatory diseases.
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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.