ArticleThe Journal of cell biology2012
A small-molecule inhibitor of Haspin alters the kinetochore functions of Aurora B.
Article in The Journal of cell biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 papers.
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Who cites it
64 citing papers in PubMed, 114 citations in OpenAlex.
- 5-Iodotubercidin inhibits epithelial to mesenchymal transition by inhibiting IKK/NFκB-dependent gene expression.The Journal of biological chemistry · 2026Article
- A pivot-tether model for nucleosome recognition by the chromosomal passenger complex.EMBO reports · 2025Article
- Haspin kinase binds to a nucleosomal DNA supergroove.Nature structural & molecular biology · 2025Article
- A ComprehensiveJournal of medicinal chemistry · 2024Article
- Structure of the human KMN complex and implications for regulation of its assembly.Nature structural & molecular biology · 2024Article
- Cell cycle responses to Topoisomerase II inhibition: Molecular mechanisms and clinical implications.The Journal of cell biology · 2023Review
- Release of Histone H3K4-reading transcription factors from chromosomes in mitosis is independent of adjacent H3 phosphorylation.Nature communications · 2023Article
- 5-Iodotubercidin sensitizes cells to RIPK1-dependent necroptosis by interfering with NFκB signaling.Cell death discovery · 2023Article
- In Silico Discovery of 5'-Modified 7-Deoxy-7-ethynyl-4'-thioadenosine as a HASPIN Inhibitor and Its Synergistic Anticancer Effect with the PLK1 Inhibitor.ACS central science · 2023Article
- Novel inhibitors of microtubule organization and phragmoplast formation in diverse plant species.Life science alliance · 2023Article
- Dissecting the roles of Haspin and VRK1 in histone H3 phosphorylation during mitosis.Scientific reports · 2022Article
- 5-Iodotubercidin inhibits SARS-CoV-2 RNA synthesis.Antiviral research · 2022Article
- Halogen Bonding in Haspin-Halogenated Tubercidin Complexes: Molecular Dynamics and Quantum Chemical Calculations.Molecules (Basel, Switzerland) · 2022Article
- Kinase PLK1 regulates the disassembly of the lateral elements and the assembly of the inner centromere during the diakinesis/metaphase I transition in male mouse meiosis.Frontiers in cell and developmental biology · 2022Article
- Epigenetic-Mediated Regulation of Gene Expression for Biological Control and Cancer: Cell and Tissue Structure, Function, and Phenotype.Results and problems in cell differentiation · 2022Review
- Epigenetic-Mediated Regulation of Gene Expression for Biological Control and Cancer: Fidelity of Mechanisms Governing the Cell Cycle.Results and problems in cell differentiation · 2022Article
- Distinct roles of haspin in stem cell division and male gametogenesis.Scientific reports · 2021Article
- Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family.Molecules (Basel, Switzerland) · 2021Article
- Chemical tools for dissecting cell division.Nature chemical biology · 2021Review
- CRISPR/Cas9 screening identifies a kinetochore-microtubule dependent mechanism for Aurora-A inhibitor resistance in breast cancer.Cancer communications (London, England) · 2021Article
4 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 3 countries.
Funding
Abstract
By phosphorylating Thr3 of histone H3, Haspin promotes centromeric recruitment of the chromosome passenger complex (CPC) during mitosis. Aurora B kinase, a CPC subunit, sustains chromosome bi-orientation and the spindle assembly checkpoint (SAC). Here, we characterize the small molecule 5-iodotubercidin (5-ITu) as a potent Haspin inhibitor. In vitro, 5-ITu potently inhibited Haspin but not Aurora B. Consistently, 5-ITu counteracted the centromeric localization of the CPC without affecting the bulk of Aurora B activity in HeLa cells. Mislocalization of Aurora B correlated with dephosphorylation of CENP-A and Hec1 and SAC override at high nocodazole concentrations. 5-ITu also impaired kinetochore recruitment of Bub1 and BubR1 kinases, and this effect was reversed by concomitant inhibition of phosphatase activity. Forcing localization of Aurora B to centromeres in 5-ITu also restored Bub1 and BubR1 localization but failed to rescue the SAC override. This result suggests that a target of 5-ITu, possibly Haspin itself, may further contribute to SAC signaling downstream of Aurora B.
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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.