ArticleBioMed research international2014
Inhibition of Nek2 by small molecules affects proteasome activity.
Article in BioMed research international, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 20 citations in OpenAlex.
- Licofelone-Loaded Poly(d,l-Lactide-Co-Glycolide) Nanoparticles to Enhance Therapeutic Action: A Novel Approach for the Topical Management of Irritant Contact Dermatitis.AAPS PharmSciTech · 2026Article
- Identification of a novel spirocyclic Nek2 inhibitor using high throughput virtual screening.Bioorganic & medicinal chemistry letters · 2023Article
- Article
- In Mitosis You Are Not: The NIMA Family of Kinases inInternational journal of molecular sciences · 2022Review
- Nek2 Kinase Signaling in Malaria, Bone, Immune and Kidney Disorders to Metastatic Cancers and Drug Resistance: Progress on Nek2 Inhibitor Development.Molecules (Basel, Switzerland) · 2022Review
- TRIP13 modulates protein deubiquitination and accelerates tumor development and progression of B cell malignancies.The Journal of clinical investigation · 2021Article
- In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases.MedChemComm · 2018Review
- Overexpression of NIMA-related kinase 2 is associated with poor prognoses in malignant glioma.Journal of neuro-oncology · 2017Article
- Molecular modeling and docking of small molecule inhibitors against NEK2.Bioinformation · 2016Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
Abstract
backgroundNek2 is a serine/threonine kinase localized to the centrosome. It promotes cell cycle progression from G2 to M by inducing centrosome separation. Recent studies have shown that high Nek2 expression is correlated with drug resistance in multiple myeloma patients. MATERIALS AND
methodsTo investigate the role of Nek2 in bortezomib resistance, we ectopically overexpressed Nek2 in several cancer cell lines, including multiple myeloma lines. Small-molecule inhibitors of Nek2 were discovered using an in-house library of compounds. We tested the inhibitors on proteasome and cell cycle activity in several cell lines.
resultsProteasome activity was elevated in Nek2-overexpressing cell lines. The Nek2 inhibitors inhibited proteasome activity in these cancer cell lines. Treatment with these inhibitors resulted in inhibition of proteasome-mediated degradation of several cell cycle regulators in HeLa cells, leaving them arrested in G2/M. Combining these Nek2 inhibitors with bortezomib increased the efficacy of bortezomib in decreasing proteasome activity in vitro. Treatment with these novel Nek2 inhibitors successfully mitigated drug resistance in bortezomib-resistant multiple myeloma.
conclusionNek2 plays a central role in proteasome-mediated cell cycle regulation and in conferring resistance to bortezomib in cancer cells. Taken together, our results introduce Nek2 as a therapeutic target in bortezomib-resistant multiple myeloma.
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