Evidence map›Paper›PMID 30620559›Full record

ArticleACS chemical biology2019

Activity-Based Protein Profiling Identifies α-Ketoamides as Inhibitors for Phospholipase A2 Group XVI.

Juan Zhou, Elliot D Mock, Andrea Martella, Vasudev Kantae, Xinyu Di, Lindsey Burggraaff, Marc P Baggelaar, Karol Al-Ayed, Alexander Bakker, Bogdan I Florea and 8 more

Open access · hybridAbstract readLetter
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS chemical biology, 2019. 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
1.5field-weighted citation impact, top 17% 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, 28 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

18 authors at 1 institution in 1 country.

Juan ZhouDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.ORCID 0000-0002-1181-7134
Elliot D MockDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.ORCID 0000-0002-1500-2856
Andrea MartellaDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.ORCID 0000-0002-4680-7702
Vasudev KantaeDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.ORCID 0000-0001-8541-0882
Xinyu DiDepartment of Analytical BioSciences and Metabolomics, Leiden Academic Centre for Drug Research , Leiden University , Leiden , The Netherlands.
Lindsey BurggraaffDepartment of Computational Drug Discovery, Leiden Academic Centre for Drug Research , Leiden University , Leiden , The Netherlands.
Marc P BaggelaarDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Karol Al-AyedDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Alexander BakkerDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Bogdan I FloreaDepartment of Bio-Organic Synthesis, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Sebastian H GrimmDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.ORCID 0000-0002-8832-8259
Hans den DulkDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Chun T LiDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Laura MulderDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Herman S OverkleeftDepartment of Bio-Organic Synthesis, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.
Thomas HankemeierDepartment of Analytical BioSciences and Metabolomics, Leiden Academic Centre for Drug Research , Leiden University , Leiden , The Netherlands.
Gerard J P van WestenDepartment of Computational Drug Discovery, Leiden Academic Centre for Drug Research , Leiden University , Leiden , The Netherlands.
Mario van der SteltDepartment of Molecular Physiology, Leiden Institute of Chemistry , Leiden University , Leiden , The Netherlands.ORCID 0000-0002-1029-5717
Leiden University · NL

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Phospholipase A2, group XVI (PLA2G16) is a thiol hydrolase from the HRASLS family that regulates lipolysis in adipose tissue and has been identified as a host factor enabling the cellular entry of picornaviruses. Chemical tools are essential to visualize and control PLA2G16 activity, but they have not been reported to date. Here, we show that MB064, which is a fluorescent lipase probe, also labels recombinant and endogenously expressed PLA2G16. Competitive activity-based protein profiling (ABPP) using MB064 enabled the discovery of α-ketoamides as the first selective PLA2G16 inhibitors. LEI110 was identified as a potent PLA2G16 inhibitor ( K

Indexed as

AmidesAnimalsEnzyme InhibitorsHumansPhospholipases A2ProteinsAmidesEnzyme InhibitorsPhospholipases A2Proteins

Identifiers

PMID30620559
PMCPMC6379856
OpenAlexW2909240363

What OpenQuestion holds

Textmetadata
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.