Evidence map›Paper›PMID 41524954›Full record

ArticleJournal of medicinal chemistry2026

Unhooking the Hook: Optimization of the Aurora A Targeting PROTAC

Jack A O'Hanlon, Katrin Gutsche, Juliane Elisabeth Müller, Nihar Ranjan Prusty, Amin Mirza, Theodoros I Roumeliotis, Hengzhang Yang, Mark Stubbs, Stephen T Hallett, Lorenz Eing and 9 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Review
  2. Article
  3. 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

19 authors.

Jack A O'HanlonCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0009-0001-0454-027X
Katrin GutscheCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0003-0578-1443
Juliane Elisabeth MüllerInstitute of Biochemistry, University of Kiel, Rudolf-Höber-Straße 1, Kiel 24118, Germany.ORCID 0009-0009-6051-4402
Nihar Ranjan PrustyCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0003-3322-1566
Amin MirzaCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0009-0002-7891-8295
Theodoros I RoumeliotisFunctional Proteomics Group, Institute of Cancer Research, Chester Beatty Laboratories, 237 Fulham Road, SW3 6JB London, U.K.ORCID 0000-0002-3354-5643
Hengzhang YangCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Mark StubbsCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0001-7855-9435
Stephen T HallettCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0003-3189-3828
Lorenz EingChair of Biochemistry and Molecular Biology, University of Würzburg, Am Hubland, Würzburg 97074, Germany.ORCID 0000-0002-1902-7428
Peter Craig McAndrewCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0002-1366-088X
Jyoti Sharma ChoudharyFunctional Proteomics Group, Institute of Cancer Research, Chester Beatty Laboratories, 237 Fulham Road, SW3 6JB London, U.K.ORCID 0000-0003-0881-5477
Yann-Vaï Le BihanCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0002-6850-9706
John CaldwellCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0001-9141-5452
Rob L M van MontfortCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0002-5688-3450
Paul WorkmanCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0003-1659-3034
Elmar WolfInstitute of Biochemistry, University of Kiel, Rudolf-Höber-Straße 1, Kiel 24118, Germany.ORCID 0000-0002-5299-6335
Gary K NewtonCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0002-2721-0089
Lindsay E EvansCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0002-6950-9329

Funding

Wellcome Trust
6 · The paper itself

Abstract

Proteolysis TArgeting Chimeras (PROTACs) can be used to target both the catalytic and noncatalytic functions of a protein, which can be particularly beneficial for proteins with important scaffolding functions like Aurora A. However, instability, poor selectivity profiles, and the hook effect often limit the applicability of PROTACs as chemical probes. In this study, we report the development of

Indexed as

Antineoplastic AgentsAurora Kinase AProtein Kinase InhibitorsAdaptor Proteins, Signal TransducingCell Line, TumorHumansProteolysisProteolysis Targeting ChimeraStructure-Activity RelationshipUbiquitin-Protein LigasesAdaptor Proteins, Signal TransducingAntineoplastic AgentsAURKA protein, humanAurora Kinase ACRBN protein, humanProtein Kinase InhibitorsProteolysis Targeting ChimeraUbiquitin-Protein Ligases

Identifiers

PMID41524954
PMCPMC12833858

What Socratic holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

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 Socratic graph.