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Last update 08 May 2025

BUB1B

Last update 08 May 2025

Basic Info

Synonyms

BUB1 mitotic checkpoint serine/threonine kinase B, Bub1A, BUB1B

+ [10]

Introduction

Essential component of the mitotic checkpoint. Required for normal mitosis progression. The mitotic checkpoint delays anaphase until all chromosomes are properly attached to the mitotic spindle. One of its checkpoint functions is to inhibit the activity of the anaphase-promoting complex/cyclosome (APC/C) by blocking the binding of CDC20 to APC/C, independently of its kinase activity. The other is to monitor kinetochore activities that depend on the kinetochore motor CENPE. Required for kinetochore localization of CENPE. Negatively regulates PLK1 activity in interphase cells and suppresses centrosome amplification. Also implicated in triggering apoptosis in polyploid cells that exit aberrantly from mitotic arrest. May play a role for tumor suppression.

Drugs associated with BUB1B

BUB1B Inhibitor(Volastra Therapeutics)

Target

BUB1B

Mechanism

BUB1B inhibitors

Active Org.

Volastra Therapeutics, Inc.

Originator Org.

Volastra Therapeutics, Inc.

Active Indication

Neoplasms

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with BUB1B

100 Translational Medicine associated with BUB1B

0 Patents (Medical) associated with BUB1B

1,262

Literatures (Medical) associated with BUB1B

31 Dec 2025·Journal of Enzyme Inhibition and Medicinal Chemistry

Design and synthesis of novel HDAC6 inhibitor dimer as HDAC6 degrader for cancer treatment by palladium catalysed dimerisation

Article

Author: Yu, Chao-Wu ; Lin, Ching ; Hsu, Yu-Tung ; Wu, Sian-Siou ; Fan, Kuo-Chen ; Hsu, Jui-Ling ; Guh, Jih-Hwa ; Lin, Miao-Hsia

The enigmatic histone deacetylase 6 (HDAC6) is one of a kind among its family. Recent reports revealed that HDAC6 CD1 exhibits E3 ligase activity. Inspired by these researches, we attempted to develop drugs targeting HDAC6 via novel mechanism. Herein, we report a palladium catalysed transformation and purification method for hydroxamic acid dimers, and series of HDAC6 inhibitor-based dimer showing outstanding biological activities and capability of inducing auto-degradation. Our proof-of-concept was highlighted with 2-amino benzamide-based HDAC6 inhibitor dimers that exhibit great HDAC6 inhibition activity (3.9-15.4 nM), good HDAC1/6 selectivity (95-577), and excellent cytotoxicity against human hormone-resistant prostate cancer (HRPC) PC-3 and non-small cell lung cancer (NSCLC) A549 cell lines (5.9-11.3 and 6.6-17.9 μM, respectively) while simultaneously inducing HDAC6 degradation. These dimers not only induce apoptosis and autophagy but also interfere with kinetochore attachment by the detection of BUBR1 phosphorylation at S670.

01 Jun 2025·Computers in Biology and Medicine

FDA-approved Levophed as an alternative multitargeted therapeutic against cervical cancer transferase, cell cycle, and regulatory proteins

Article

Author: Gupta, Dinesh ; Bano, Nagmi ; Ahmad, Shaban ; Raza, Khalid

Despite the availability of Pap tests and HPV vaccines, Cervical Cancer continues to be a significant factor contributing to women's deaths. It poses severe consequences to women's health. The disease's severity lies in its potential to progress silently in its early stages, mainly detected in its advanced stage, and clinical treatment is challenging due to drug resistance. This study aims to identify multitargeted lead molecules based on the interactome of Cervical Cancer-related crucial genes, which can help develop drug-resistant therapies. We have considered 9 crucial Cervical Cancer genes, namely BUBR1, CCNB1, FEN1, MAD2, MCM10, MCM6, ITGB8, POLE, and TPX2, to perform gene network analysis and Gene Ontology enrichment studies to identify the potential hub genes and their role. Further, we performed multitarget screening using multisampling algorithms HTVS, SP, and XP to screen the protein products of the 9 genes for their binding affinity for the FDA-approved drugs library. The binding affinities of the compounds were evaluated using MM\GBSA that identified multitargeted potential inhibitor as a Levophed for Cervical Cancer, and the docking results showed a range of MM/GBSA scores, varying from -8.35 to -5.38 kcal/mol for docking, and -43.41 to -19.37 kcal/mol for MM/GBSA scoring. The protein residues that interact the most with Levophed are ALA, THR, ILE, ASN, GLY, ASP, LEU, LYS, VAL, GLN, PRO, CYS, GLU, and TYR. The pharmacokinetic properties and WaterMap computations also support the idea that the compound can potentially become a drug candidate. Furthermore, all 9 complexes were simulated for 100ns, resulting in cumulative deviation and fluctuation of <2 Å, with many intermolecular interactions and binding free energy computations supporting the studies. The study shows that Levophed could treat Cervical Cancer without encountering drug resistance- however, experimental studies are needed to confirm the accuracy.

01 Jun 2025·Phytomedicine

Integrating thermal proteome profiling and virtual screening to reveal the mechanism of Bletilla striata against osteoclast-driven osteoporosis

Article

Author: Tu, Yanbei ; Li, Yanfang ; Mu, Wen ; Dai, Guiyu ; Yang, Ying

BACKGROUNDOsteoclast (OC) overactivation and increased bone resorption are central factors contributing to osteoporosis (OP). Bletilla striata (Thunb.) Reichb. f. is known for its hemostatic properties, however, its therapeutic potential and underlying mechanisms in OC-dependent OP remain unclear.PURPOSEThis study aimed to evaluate the anti-OP effects of Bletilla striata extract (BSE) and elucidate its mechanisms of action (MoAs) through an innovative integrated strategy combining isothermal thermal proteome profiling (TPP) and structure-based virtual screening (SBVS).RESULTSBSE treatment significantly decreased bone loss in ovariectomized rats, as evidenced by micro-CT and pathological analyses. This effect was attributed to inhibition of OC formation by BSE. BSE markedly blocked RANKL-induced OC differentiation, inhibited F-actin ring formation, and decreased the expression of marker genes and proteins including NFATc1, CTSK, and MMP-9. Using an isothermal TPP strategy, 110 proteins were identified as the direct targets of BSE for OC inhibition based on proteome-level thermal stability analysis (fold change > 2.0). Subsequently, using label-free quantitative proteomics, 159 proteins were identified as indirect response proteins resulting from the interaction between BSE and direct targets. The SBVS approach was employed to establish a one-to-one correspondence between the chemical ingredients in BSE and the direct targets revealed by isothermal TPP. Based on these data, an "active ingredient-direct target-indirect response signal" interaction network was constructed, which revealed the key targets (ATM, PIK3R1, BUB1B, and NR3C1) and active ingredients (phenanthrene dimers and steroids) of BSE responsible for inhibiting OC formation.CONCLUSIONThis study not only highlights the therapeutic potential of BSE for treating OP but also provides a novel methodological framework for interpreting the MoAs of complex Traditional Chinese Medicine (TCM) extracts. By integrating isothermal TPP and SBVS, this study offers new insights into the mechanism of TCM.

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