Evidence map›Paper›PMID 36614307›Full record

ArticleInternational journal of molecular sciences2023

The Inhibitory Properties of a Novel, Selective LMTK3 Kinase Inhibitor.

Alessandro Agnarelli, Andrea Lauer Betrán, Athanasios Papakyriakou, Viviana Vella, Mark Samuels, Panagiotis Papanastasopoulos, Christina Giamas, Erika J Mancini, Justin Stebbing, John Spencer and 3 more

Open access · goldAbstract read
In one paragraph

Article in International journal of molecular sciences, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.6field-weighted citation impact, top 18% 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

7 citing papers in PubMed, 7 citations in OpenAlex.

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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

13 authors at 3 institutions in 2 countries.

Alessandro AgnarelliDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.ORCID 0000-0003-3218-3836
Andrea Lauer BetránDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.
Athanasios PapakyriakouInstitute of Biosciences and Applications, National Centre for Scientific Research "Demokritos", 15341 Athens, Greece.ORCID 0000-0003-3931-6232
Viviana VellaDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.ORCID 0000-0003-1000-3443
Mark SamuelsDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.
Panagiotis PapanastasopoulosDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.
Christina GiamasDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.
Erika J ManciniDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.
Justin StebbingDepartment of Surgery and Cancer, Imperial College, London SW7 2BX, UK.
John SpencerSussex Drug Discovery Centre, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.ORCID 0000-0001-5231-8836
Chiara CilibrasiDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.ORCID 0000-0002-4986-1800
Angeliki DitsiouDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.ORCID 0000-0003-3743-8447
Georgios GiamasDepartment of Biochemistry and Biomedicine, School of Life Sciences, University of Sussex, Brighton BN1 9QG, UK.ORCID 0000-0002-4417-2707
University of Sussex · GBImperial College London · GBNational Centre of Scientific Research "Demokritos" · GR

Funding

Action Against Cancer G1868
6 · The paper itself

Abstract

Recently, the oncogenic role of lemur tyrosine kinase 3 (LMTK3) has been well established in different tumor types, highlighting it as a viable therapeutic target. In the present study, using in vitro and cell-based assays coupled with biophysical analyses, we identify a highly selective small molecule LMTK3 inhibitor, namely C36. Biochemical/biophysical and cellular studies revealed that C36 displays a high in vitro selectivity profile and provides notable therapeutic effect when tested in the National Cancer Institute (NCI)-60 cancer cell line panel. We also report the binding affinity between LMTK3 and C36 as demonstrated via microscale thermophoresis (MST). In addition, C36 exhibits a mixed-type inhibition against LMTK3, consistent with the inhibitor overlapping with both the adenosine 5'-triphosphate (ATP)- and substrate-binding sites. Treatment of different breast cancer cell lines with C36 led to decreased proliferation and increased apoptosis, further reinforcing the prospective value of LMTK3 inhibitors for cancer therapy.

Indexed as

Protein Kinase InhibitorsProtein Serine-Threonine KinasesCell Line, TumorHumansMembrane ProteinsProspective StudiesLMTK3 protein, humanMembrane ProteinsProtein Kinase InhibitorsProtein Serine-Threonine Kinasesbreast cancerkinase inhibitorLMTK3

Identifiers

PMID36614307
PMCPMC9821308
OpenAlexW4313585076

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.