Evidence map›Paper›PMID 40730065›Full record

ArticleEuropean journal of medicinal chemistry2025

Discovery of the first-in-class Aurora B kinase selective degrader.

Xiaoping Hu, Kevin Graciano, Jianping Hu, Chang Liu, Jiuyi Zhang, Ling Xie, Xian Chen, Yan Xiong, Jian Jin, Jia Xu

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

  1. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors.

Xiaoping HuMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Science, Oncological Science and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States.
Kevin GracianoDepartment of Genetics, The University of Alabama at Birmingham, Birmingham, AL, 35294, United States; O'Neal Comprehensive Cancer Center, The University of Alabama at Birmingham, Birmingham, AL, 35233, United States.
Jianping HuMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Science, Oncological Science and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States.
Chang LiuDepartment of Genetics, The University of Alabama at Birmingham, Birmingham, AL, 35294, United States.
Jiuyi ZhangDepartment of Genetics, The University of Alabama at Birmingham, Birmingham, AL, 35294, United States.
Ling XieDepartment of Biochemistry and Biophysics, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, United States.
Xian ChenDepartment of Biochemistry and Biophysics, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, United States.
Yan XiongMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Science, Oncological Science and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States.
Jian JinMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Science, Oncological Science and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States. Electronic address: jian.jin@mssm.edu.
Jia XuDepartment of Genetics, The University of Alabama at Birmingham, Birmingham, AL, 35294, United States; O'Neal Comprehensive Cancer Center, The University of Alabama at Birmingham, Birmingham, AL, 35233, United States. Electronic address: xuj@uab.edu.

Funding

An AVANCE NEO 400 MHz NMR Spectrometer for Chemical Biology and Drug DiscoveryS10OD028504 · OD · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI ZHOU, MING-MING · 2020 to 2020
$599k
An AVANCE NEO 600 MHz NMR Spectrometer System for Structural and Chemical BiologyS10OD025132 · OD · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI ZHOU, MING-MING · 2019 to 2019
$535k
NIH HHS S10 OD025132NIH HHS S10 OD028504
6 · The paper itself

Abstract

Aurora kinases, consisting of Aurora A, B, and C, play critical roles in the regulation of mitosis and are frequently overexpressed in multiple types of cancer. Several Aurora kinase inhibitors have been developed and tested in clinical trials. Additionally, Aurora kinase A (AURKA) degraders and dual degraders of AURKA and Aurora kinase B (AURKB) have been reported. However, no AURKB selective degrader has been reported. Here, we report the discovery of the first-in-class AURKB selective degrader, MS44 (18), a von Hippel-Lindau (VHL) E3 ligase-recruiting proteolysis-targeting chimera (PROTAC), which potently degrades AURKB with a DC

Indexed as

Antineoplastic AgentsAurora Kinase BDrug DiscoveryProtein Kinase InhibitorsProteolysisCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMolecular StructureProteolysis Targeting ChimeraQuinazolinesStructure-Activity RelationshipThiazolesAntineoplastic AgentsAURKB protein, humanAurora Kinase BMS44 compoundProtein Kinase InhibitorsProteolysis Targeting ChimeraQuinazolinesThiazolesAurora BAZD1152DegraderKinasePROTAC

Identifiers

PMID40730065
PMCPMC12379206

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Registered trials

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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.