Evidence map›Paper›PMID 35178172›Full record

ArticleACS medicinal chemistry letters2022

A Comparative Assessment Study of Known Small-molecule GPVI Modulators.

Holly Foster, Clare Wilson, Julia S Gauer, Rui-Gang Xu, Mark J Howard, Iain W Manfield, Robert Ariëns, Khalid Naseem, Lewis R Vidler, Helen Philippou and 1 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
1.1field-weighted citation impact, top 22% 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

2 citing papers in PubMed, 7 citations in OpenAlex.

  1. Article
  2. 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 2 institutions in 1 country.

Holly FosterSchool of Chemistry, University of Leeds, Leeds LS2 9JT, U.K.ORCID https://orcid.org/0000-0002-8440-041X
Clare WilsonLeeds Institute of Cardiovascular and Metabolic Medicine (LICAMM), School of Medicine, University of Leeds, Leeds LS2 9JT, U.K.
Julia S GauerLeeds Institute of Cardiovascular and Metabolic Medicine (LICAMM), School of Medicine, University of Leeds, Leeds LS2 9JT, U.K.
Rui-Gang XuLeeds Institute of Cardiovascular and Metabolic Medicine (LICAMM), School of Medicine, University of Leeds, Leeds LS2 9JT, U.K.
Mark J HowardSchool of Chemistry, University of Leeds, Leeds LS2 9JT, U.K.
Iain W ManfieldFaculty of Biological Sciences and Astbury Centre for Structural Molecular Biology, University of Leeds, Leeds LS2 9JT, U.K.
Robert AriënsLeeds Institute of Cardiovascular and Metabolic Medicine (LICAMM), School of Medicine, University of Leeds, Leeds LS2 9JT, U.K.
Khalid NaseemLeeds Institute of Cardiovascular and Metabolic Medicine (LICAMM), School of Medicine, University of Leeds, Leeds LS2 9JT, U.K.
Lewis R VidlerUCB, Slough, SL1 3WE, U.K.
Helen PhilippouLeeds Institute of Cardiovascular and Metabolic Medicine (LICAMM), School of Medicine, University of Leeds, Leeds LS2 9JT, U.K.
Richard FosterSchool of Chemistry, University of Leeds, Leeds LS2 9JT, U.K.ORCID https://orcid.org/0000-0002-2361-3884
University of Leeds · GBUCB Pharma (United Kingdom) · GB

Funding

British Heart Foundation FS/17/66/33480British Heart Foundation PG/16/6/31941
6 · The paper itself

Abstract

The GPVI platelet receptor was recently validated as a safe antiplatelet target for the treatment of thrombosis using several peptidic modulators. In contrast, few weakly potent small-molecule GPVI antagonists have been reported. Those that have been published often lack evidence for target engagement, and their biological efficacy cannot be compared because of the natural donor variability associated with the assays implemented. Herein, we present the first side-by-side assessment of the reported GPVI small-molecule modulators. We have characterized their functional activities on platelet activation and aggregation using flow cytometry as well as light transmission and electrical impedance aggregometry. We also utilized microscale thermophoresis (MST) and saturation transfer difference (STD) NMR to validate GPVI binding and have used this along with molecular modeling to suggest potential binding interactions. We conclude that of the compounds examined, losartan and compound

Identifiers

PMID35178172
PMCPMC8842102
OpenAlexW4206202688

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.