Evidence map›Paper›PMID 27522578›Full record

ArticleBioorganic & medicinal chemistry2016

2-Oxoamide inhibitors of cytosolic group IVA phospholipase A2 with reduced lipophilicity.

Georgia Antonopoulou, Victoria Magrioti, Maroula G Kokotou, Aikaterini Nikolaou, Efrosini Barbayianni, Varnavas D Mouchlis, Edward A Dennis, George Kokotos

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2016. 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
1.3field-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

4 citing papers in PubMed, 5 citations in OpenAlex.

  1. Article
  2. Review
  3. Small-molecule inhibitors as potential therapeutics and as tools to understand the role of phospholipases ABiochimica et biophysica acta. Molecular and cell biology of lipids · 2019
    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

8 authors at 2 institutions in 2 countries.

Georgia AntonopoulouDepartment of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece; Institute of Biology, Medicinal Chemistry and Biotechnology, National Hellenic Research Foundation, Athens, Greece.
Victoria MagriotiDepartment of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece.
Maroula G KokotouDepartment of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece.
Aikaterini NikolaouDepartment of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece.
Efrosini BarbayianniDepartment of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece.
Varnavas D MouchlisDepartment of Chemistry and Biochemistry, School of Medicine, MC 0601, University of California, San Diego, La Jolla, CA 92093-0601, USA; Department of Pharmacology, School of Medicine, MC 0601, University of California, San Diego, La Jolla, CA 92093-0601, USA.
Edward A DennisDepartment of Chemistry and Biochemistry, School of Medicine, MC 0601, University of California, San Diego, La Jolla, CA 92093-0601, USA; Department of Pharmacology, School of Medicine, MC 0601, University of California, San Diego, La Jolla, CA 92093-0601, USA. Electronic address: edennis@ucsd.edu.
George KokotosDepartment of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece. Electronic address: gkokotos@chem.uoa.gr.
National and Kapodistrian University of Athens · GRUniversity of California San Diego · US

Funding

ACTION OF LIPOLYTIC ENZYMESR01GM020501 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI DENNIS, EDWARD A · 1985 to 2020
$7.3M
NIGMS NIH HHS R01 GM020501
6 · The paper itself

Abstract

Cytosolic GIVA phospholipase A2 (GIVA cPLA2) initiates the eicosanoid pathway of inflammation and thus inhibitors of this enzyme constitute novel potential agents for the treatment of inflammatory diseases. Traditionally, GIVA cPLA2 inhibitors have suffered systemically from high lipophilicity. We have developed a variety of long chain 2-oxoamides as inhibitors of GIVA PLA2. Among them, AX048 was found to produce a potent analgesic effect. We have now reduced the lipophilicity of AX048 by replacing the long aliphatic chain with a chain containing an ether linked aromatic ring with in vitro inhibitory activities similar to AX048.

Indexed as

AnimalsCytosolDrug DesignEnzyme InhibitorsGroup IV Phospholipases A2HumansPyridinesStructure-Activity RelationshipEnzyme InhibitorsGroup IV Phospholipases A2oxoamidePyridines2-OxoamidesGIVA cPLA(2)InhibitorsLipophilicityPhospholipase A(2)

Identifiers

PMID27522578
PMCPMC5014611
OpenAlexW2482598500

What OpenQuestion holds

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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.