ArticleeLife2016
Probing the catalytic functions of Bub1 kinase using the small molecule inhibitors BAY-320 and BAY-524.
Article in eLife, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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Who cites it
41 citing papers in PubMed, 69 citations in OpenAlex.
- BUB signaling in cancer and molecular insights into targeted therapies.Communications biology · 2026Review
- hSpindly dynamics modulate spindle assembly checkpoint signaling, promoting resistance to mitotic inhibitors.iScience · 2026Article
- Leveraging the lipoprotein trafficking pathway for the development of novel antimicrobials.RSC chemical biology · 2026Review
- Tumour specific HORMAD1 expression perturbs mitotic arrest and drives sensitivity to mitotic kinase inhibitors.Nature communications · 2026Article
- BUB1 in cancer genetics and oncogenomics: from chromosomal instability to therapeutic vulnerabilities.Frontiers in genetics · 2026Review
- Genome-wide CRISPR screen identifies BUB1 kinase as a druggable vulnerability in malignant pleural mesothelioma.Cell death & disease · 2025Article
- Cyclin A/Cdk1 promotes chromosome alignment and timely mitotic progression.Molecular biology of the cell · 2024Article
- Prognostic and Therapeutic Implications of Cell Division Cycle 20 Homolog in Breast Cancer.Cancers · 2024Article
- Expression of the checkpoint kinase BUB1 is a predictor of response to cancer therapies.Scientific reports · 2024Article
- Age-dependent loss of cohesion protection in human oocytes.Current biology : CB · 2024Article
- Cyclin A/Cdk1 promotes chromosome alignment and timely mitotic progression.bioRxiv : the preprint server for biology · 2023Article
- Inhibition of the serine/threonine kinase BUB1 reverses taxane resistance in prostate cancer.iScience · 2023Article
- Distinct Aurora B pools at the inner centromere and kinetochore have different contributions to meiotic and mitotic chromosome segregation.Molecular biology of the cell · 2023Article
- Distinct Aurora B pools at the inner centromere and kinetochore have different contributions to meiotic and mitotic chromosome segregation.bioRxiv : the preprint server for biology · 2023Article
- Hyper-active RAS/MAPK introduces cancer-specific mitotic vulnerabilities.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Zombies Never Die: The Double Life Bub1 Lives in Mitosis.Frontiers in cell and developmental biology · 2022Review
- Inhibitors of the Bub1 spindle assembly checkpoint kinase: synthesis of BAY-320 and comparison with 2OH-BNPP1.Royal Society open science · 2021Article
- Distinct roles of haspin in stem cell division and male gametogenesis.Scientific reports · 2021Article
- Spindle assembly checkpoint activation and silencing at kinetochores.Seminars in cell & developmental biology · 2021Review
- Mapping Proximity Associations of Core Spindle Assembly Checkpoint Proteins.Journal of proteome research · 2021Article
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The kinase Bub1 functions in the spindle assembly checkpoint (SAC) and in chromosome congression, but the role of its catalytic activity remains controversial. Here, we use two novel Bub1 inhibitors, BAY-320 and BAY-524, to demonstrate potent Bub1 kinase inhibition both in vitro and in intact cells. Then, we compared the cellular phenotypes of Bub1 kinase inhibition in HeLa and RPE1 cells with those of protein depletion, indicative of catalytic or scaffolding functions, respectively. Bub1 inhibition affected chromosome association of Shugoshin and the chromosomal passenger complex (CPC), without abolishing global Aurora B function. Consequently, inhibition of Bub1 kinase impaired chromosome arm resolution but exerted only minor effects on mitotic progression or SAC function. Importantly, BAY-320 and BAY-524 treatment sensitized cells to low doses of Paclitaxel, impairing both chromosome segregation and cell proliferation. These findings are relevant to our understanding of Bub1 kinase function and the prospects of targeting Bub1 for therapeutic applications.
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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.