Evidence map›Paper›PMID 34417202›Full record

ArticleCancer research2021

A Conformation Selective Mode of Inhibiting SRC Improves Drug Efficacy and Tolerability.

Carolin Temps, Daniel Lietha, Emily R Webb, Xue-Feng Li, John C Dawson, Morwenna Muir, Kenneth G Macleod, Teresa Valero, Alison F Munro, Rafael Contreras-Montoya and 11 more

Open access · hybridAbstract read
In one paragraph

Article in Cancer research, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.

0numbers the graph read from it
0cells of the map it votes in
32citing papers in PubMed
2.6field-weighted citation impact, top 9% of its field
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

32 citing papers in PubMed, 50 citations in OpenAlex.

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  9. Locking CBL TKBD in its native conformation presents a novel therapeutic opportunity in mutant CBL-dependent leukemia.Molecular therapy : the journal of the American Society of Gene Therapy · 2025
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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 at 4 institutions in 2 countries.

Carolin TempsCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.
Daniel LiethaMargarita Salas Center for Biological Research (CIB), Spanish National Research Council (CSIC), Madrid, Spain.
Emily R Webb *Cancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.ORCID 0000-0001-9339-4544
Xue-Feng Li *MRC Centre for Reproductive Health, University of Edinburgh, Edinburgh, United Kingdom.
John C Dawson *Cancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.ORCID 0000-0001-5713-1026
Morwenna MuirCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.ORCID 0000-0001-5835-3886
Kenneth G MacleodCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.
Teresa ValeroCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.ORCID 0000-0002-3625-311X
Alison F MunroCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.
Rafael Contreras-MontoyaCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.
Juan R Luque-OrtegaMargarita Salas Center for Biological Research (CIB), Spanish National Research Council (CSIC), Madrid, Spain.ORCID 0000-0003-3206-7480
Craig FraserCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.
Henry BeethamCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.
Christina SchoenherrCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.ORCID 0000-0002-0983-6168
Maria LopalcoEdinburgh Innovations Ltd., Edinburgh, United Kingdom.
Mark J ArendsCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.ORCID 0000-0002-6826-8770
Margaret C FrameCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.
Bin-Zhi QianMRC Centre for Reproductive Health, University of Edinburgh, Edinburgh, United Kingdom.
Valerie G BruntonCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.ORCID 0000-0002-7778-8794
Neil O CarragherCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom.
Asier Unciti-BrocetaCancer Research UK Edinburgh Centre, Institute of Genetics & Cancer, University of Edinburgh, Edinburgh, United Kingdom. asier.ub@ed.ac.uk.ORCID 0000-0003-1029-2855
Edinburgh Cancer Research · GBMRC Centre for Reproductive Health · GBNational Research Council · LKSurgical Innovations (United Kingdom) · GB

Funding

Cancer Research UK 15703Cancer Research UK 17367Cancer Research UK A15703Cancer Research UK A17367Wellcome Trust
6 · The paper itself

Abstract

Despite the approval of several multikinase inhibitors that target SRC and the overwhelming evidence of the role of SRC in the progression and resistance mechanisms of many solid malignancies, inhibition of its kinase activity has thus far failed to improve patient outcomes. Here we report the small molecule eCF506 locks SRC in its native inactive conformation, thereby inhibiting both enzymatic and scaffolding functions that prevent phosphorylation and complex formation with its partner FAK. This mechanism of action resulted in highly potent and selective pathway inhibition in culture and

Indexed as

AnimalsApoptosisBone NeoplasmsBreast NeoplasmsCell ProliferationFemaleFocal Adhesion Kinase 1HumansMiceMice, Inbred BALB CMice, NudePiperidinesProtein ConformationProtein Kinase InhibitorsProto-Oncogene Proteins c-ablPyrazoleseCF506 compoundFocal Adhesion Kinase 1PiperidinesProtein Kinase InhibitorsProto-Oncogene Proteins c-ablPTK2 protein, humanPyrazolesPyrimidinesSmall Molecule Librariessrc-Family Kinases

Identifiers

PMID34417202
PMCPMC7611940
OpenAlexW3194825531

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.