Evidence map›Paper›PMID 40601435›Full record

ArticleACS chemical biology2025

Mediator Kinase Inhibitor Selectivity and Activity in Colorectal Cancer.

Maria J Ortiz-Ruiz, Olajumoke Popoola, Konstantinos Mitsopoulos, Robert Te-Poele, Rahul S Samant, Gary Box, Will Court, Alexis De Haven Brandon, Sharon Gowan, Aurelie Mallinger and 11 more

Abstract read
In one paragraph

Article in ACS chemical biology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

  1. Article
  2. Review
  3. Review
  4. Article
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

21 authors.

Maria J Ortiz-RuizCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Olajumoke PopoolaCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0003-0452-0401
Konstantinos MitsopoulosCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Robert Te-PoeleCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0009-0001-3596-6572
Rahul S SamantCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0003-1952-259X
Gary BoxCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Will CourtCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Alexis De Haven BrandonCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Sharon GowanCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Aurelie MallingerCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Toby RoeCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Kate SwabeyCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Melanie ValentiCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Bissan Al-LazikaniCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Julian BlaggCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Christina EsdarThe Healthcare Business of Merck KGaA, 64293 Darmstadt, Germany.
Kai SchiemannThe Healthcare Business of Merck KGaA, 64293 Darmstadt, Germany.
Dirk WienkeThe Healthcare Business of Merck KGaA, 64293 Darmstadt, Germany.
Suzanne A EcclesCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.
Paul WorkmanCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0003-1659-3034
Paul A ClarkeCentre for Cancer Drug Discovery, The Institute of Cancer Research, London SM2 5NG, U.K.ORCID 0000-0001-9342-1290

Funding

Cancer Research UK C2739/A22897Cancer Research UK C309/A11566Wellcome Trust
6 · The paper itself

Abstract

The Mediator complex is a regulator of gene expression, influencing chromatin structure and RNA polymerase II-mediated transcription. Its activity is controlled by a protein kinase module, which includes cyclin-dependent kinases 8 and 19, that phosphorylates RNA polymerase II and transcription factors to regulate gene expression. Using orthogonal approaches combining chemical and genetic tools, we demonstrated the selectivity of our small-molecule inhibitors derived from 3,4,5-trisubstituted pyridine and 3-methyl-1

Indexed as

Antineoplastic AgentsColorectal NeoplasmsCyclin-Dependent Kinase 8Cyclin-Dependent KinasesMediator ComplexProtein Kinase InhibitorsAnimalsCell Line, TumorCell ProliferationCyclin-Dependent Kinase-Activating KinaseHumansMicePhosphorylationPyridinesXenograft Model Antitumor AssaysAntineoplastic AgentsCDK19 protein, humanCDK8 protein, humanCyclin-Dependent Kinase 8Cyclin-Dependent Kinase-Activating KinaseCyclin-Dependent KinasesMediator ComplexProtein Kinase InhibitorsPyridines

Identifiers

PMID40601435
PMCPMC12281475

What OpenQuestion 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 OpenQuestion graph.