Evidence map›Paper›PMID 31941153›Full record

ArticleMolecules (Basel, Switzerland)2020

In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds.

Sean N O'Byrne, John W Scott, Joseph R Pilotte, André da S Santiago, Christopher G Langendorf, Jonathan S Oakhill, Benjamin J Eduful, Rafael M Couñago, Carrow I Wells, William J Zuercher and 2 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
2.2field-weighted citation impact, top 12% 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

19 citing papers in PubMed, 37 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

12 authors at 3 institutions in 3 countries.

Sean N O'ByrneStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
John W ScottSt Vincent's Institute and Department of Medicine, The University of Melbourne, 41 Victoria Parade, Fitzroy 3065, Australia.
Joseph R PilotteStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
André da S SantiagoCentro de Química Medicinal (CQMED), Centro de Biologia Molecular e Engenharia Genética (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas, SP 13083-875, Brazil.
Christopher G LangendorfSt Vincent's Institute and Department of Medicine, The University of Melbourne, 41 Victoria Parade, Fitzroy 3065, Australia.
Jonathan S OakhillSt Vincent's Institute and Department of Medicine, The University of Melbourne, 41 Victoria Parade, Fitzroy 3065, Australia.
Benjamin J EdufulStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Rafael M CouñagoCentro de Química Medicinal (CQMED), Centro de Biologia Molecular e Engenharia Genética (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas, SP 13083-875, Brazil.
Carrow I WellsStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
William J ZuercherStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Timothy M WillsonStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
David H DrewryStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
University of North Carolina at Chapel Hill · USThe University of Melbourne · AUUniversidade Estadual de Campinas (UNICAMP) · BR

Funding

Virology Research Program (Program 4)P30CA016086 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI David Darr · 1985 to 2026
$201.5M
Creation of in vivo active chemical probes for CAMKK2 to treat cancerR01CA218442 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI DREWRY, DAVID HAROLD · 2017 to 2019
$2.0M
Characterization of an understudied kinase, NEK5, in acquisition of a mesenchymaland migratory cell phenotypeR03TR003386 · NCATS · TULANE UNIVERSITY OF LOUISIANA · PI BUROW, MATTHEW E., DREWRY, DAVID HAROLD · 2020 to 2020
$167k
NCATS NIH HHS R03 TR003386NCI NIH HHS P30 CA016086NCI NIH HHS R01 CA218442NIH HHS 1U24DK116204-01NIH HHS R01CA218442
6 · The paper itself

Abstract

The calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) activates CAMK1, CAMK4, AMPK, and AKT, leading to numerous physiological responses. The deregulation of CAMKK2 is linked to several diseases, suggesting the utility of CAMKK2 inhibitors for oncological, metabolic and inflammatory indications. In this work, we demonstrate that STO-609, frequently described as a selective inhibitor for CAMKK2, potently inhibits a significant number of other kinases. Through an analysis of literature and public databases, we have identified other potent CAMKK2 inhibitors and verified their activities in differential scanning fluorimetry and enzyme inhibition assays. These inhibitors are potential starting points for the development of selective CAMKK2 inhibitors and will lead to tools that delineate the roles of this kinase in disease biology

Indexed as

Calcium-Calmodulin-Dependent Protein Kinase KinaseAnimalsBenzimidazolesHumansNaphthalimidesProtein Kinase InhibitorsBenzimidazolesCalcium-Calmodulin-Dependent Protein Kinase KinaseCAMKK2 protein, humanNaphthalimidesProtein Kinase InhibitorsSTO 609CAMKK2chemical probeskinasekinase inhibitorsoncologySTO-609

Identifiers

PMID31941153
PMCPMC7024175
OpenAlexW2999167819

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.