Evidence map›Paper›PMID 33247181›Full record

ArticleCommunications biology2020

The PAR2 inhibitor I-287 selectively targets Gα

Charlotte Avet, Claudio Sturino, Sébastien Grastilleur, Christian Le Gouill, Meriem Semache, Florence Gross, Louis Gendron, Youssef Bennani, Joseph A Mancini, Camil E Sayegh and 1 more

Open access · goldAbstract read
In one paragraph

Article in Communications biology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.

0numbers the graph read from it
0cells of the map it votes in
24citing papers in PubMed
2.7field-weighted citation impact, top 8% 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

24 citing papers in PubMed, 33 citations in OpenAlex.

  1. Review
  2. MMP1 and PRSS23 induce PARCommunications biology · 2026
    Article
  3. Review
  4. Review
  5. Article
  6. Article
  7. Review
  8. Article
  9. Review
  10. Article
  11. Article
  12. Article
  13. GRespiratory research · 2024
    Review
  14. New Target(s) for RNF43 Regulation: Implications for Therapeutic Strategies.International journal of molecular sciences · 2024
    Review
  15. Article
  16. Review
  17. Article
  18. Review
  19. Article
  20. PAR2: The Cornerstone of Pancreatic Diseases.Physiological research · 2022
    Review
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

11 authors at 6 institutions in 3 countries.

Charlotte AvetInstitute for Research in Immunology and Cancer, and Department of Biochemistry and Molecular Medicine, Université de Montréal, Montréal, QC, Canada, H3C 1J4.
Claudio SturinoVertex Pharmaceuticals (Canada), Inc., Laval, QC, Canada, H7V 4A7.
Sébastien GrastilleurDépartement de Pharmacologie-Physiologie, Université de Sherbrooke, Centre de Recherche du CHU de Sherbrooke, Centre d'Excellence en Neurosciences de l'Université de Sherbrooke, Institut de Pharmacologie de Sherbrooke, Sherbrooke, QC, Canada, J1H 5N4.
Christian Le GouillInstitute for Research in Immunology and Cancer, and Department of Biochemistry and Molecular Medicine, Université de Montréal, Montréal, QC, Canada, H3C 1J4.ORCID 0000-0002-6455-1800
Meriem SemacheInstitute for Research in Immunology and Cancer, and Department of Biochemistry and Molecular Medicine, Université de Montréal, Montréal, QC, Canada, H3C 1J4.
Florence GrossInstitute for Research in Immunology and Cancer, and Department of Biochemistry and Molecular Medicine, Université de Montréal, Montréal, QC, Canada, H3C 1J4.
Louis GendronDépartement de Pharmacologie-Physiologie, Université de Sherbrooke, Centre de Recherche du CHU de Sherbrooke, Centre d'Excellence en Neurosciences de l'Université de Sherbrooke, Institut de Pharmacologie de Sherbrooke, Sherbrooke, QC, Canada, J1H 5N4.ORCID 0000-0002-2058-8863
Youssef BennaniVertex Pharmaceuticals (Canada), Inc., Laval, QC, Canada, H7V 4A7.
Joseph A ManciniVertex Pharmaceuticals (Canada), Inc., Laval, QC, Canada, H7V 4A7.
Camil E SayeghVertex Pharmaceuticals (Canada), Inc., Laval, QC, Canada, H7V 4A7.
Michel BouvierInstitute for Research in Immunology and Cancer, and Department of Biochemistry and Molecular Medicine, Université de Montréal, Montréal, QC, Canada, H3C 1J4. michel.bouvier@umontreal.ca.ORCID 0000-0003-1128-0100
Institute for Research in Immunology and Cancer · CAUniversité de Sherbrooke · CAAVEO Oncology (United States) · USFPInnovations · CAParaza Pharma (Canada) · CAVertex Pharmaceuticals (Canada) · CA

Funding

CIHR IPCR 136753CIHR MOP-123399
6 · The paper itself

Abstract

Protease-activated receptor-2 (PAR2) is involved in inflammatory responses and pain, therefore representing a promising therapeutic target for the treatment of immune-mediated inflammatory diseases. However, as for other GPCRs, PAR2 can activate multiple signaling pathways and those involved in inflammatory responses remain poorly defined. Here, we describe a new selective and potent PAR2 inhibitor (I-287) that shows functional selectivity by acting as a negative allosteric regulator on Gα

Indexed as

AnimalsAnti-Inflammatory Agentsbeta-ArrestinsBioluminescence Resonance Energy Transfer TechniquesCell Line, TumorGTP-Binding Protein alpha Subunits, G12-G13GTP-Binding Protein alpha Subunits, Gq-G11HumansInflammationInterleukin-8MaleMiceMice, Inbred C57BLReceptor, PAR-2Signal TransductionAnti-Inflammatory Agentsbeta-ArrestinsGTP-Binding Protein alpha Subunits, G12-G13GTP-Binding Protein alpha Subunits, Gq-G11Interleukin-8Receptor, PAR-2

Identifiers

PMID33247181
PMCPMC7695697
OpenAlexW3107576461

What Socratic 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 Socratic graph.