Evidence map›Paper›PMID 31857838›Full record

ArticleACS medicinal chemistry letters2019

Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.

Rachel A Rowlands, M Claire Cato, Helen V Waldschmidt, Renee A Bouley, Qiuyan Chen, Larisa Avramova, Scott D Larsen, John J G Tesmer, Andrew D White

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
–field-weighted citation impact
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

8 citing papers in PubMed.

  1. Article
  2. The roles of G protein-coupled receptor kinase 2 in renal diseases.Journal of cellular and molecular medicine · 2024
    Review
  3. Red light-green light: T-cell trafficking in cardiac and vascular inflammation.American journal of physiology. Cell physiology · 2023
    Review
  4. Article
  5. Targeting GRK5 for Treating Chronic Degenerative Diseases.International journal of molecular sciences · 2021
    Review
  6. Targeting G protein-coupled receptor kinases (GRKs) to G protein-coupled receptors.Current opinion in endocrine and metabolic research · 2021
    Article
  7. Article
  8. 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

9 authors.

Rachel A RowlandsUniversity of Michigan, Vahlteich Medicinal Chemistry Core, College of Pharmacy, 428 Church Street, Ann Arbor, Michigan 48109, United States.
M Claire CatoUniversity of Michigan, Life Sciences Institute, Departments of Pharmacology and Biological Chemistry, 210 Washtenaw Avenue, Ann Arbor, Michigan 48109, United States.
Helen V WaldschmidtUniversity of Michigan, Vahlteich Medicinal Chemistry Core, College of Pharmacy, 428 Church Street, Ann Arbor, Michigan 48109, United States.
Renee A BouleyUniversity of Michigan, Life Sciences Institute, Departments of Pharmacology and Biological Chemistry, 210 Washtenaw Avenue, Ann Arbor, Michigan 48109, United States.
Qiuyan ChenPurdue University, Departments of Biological Sciences and Medicinal Chemistry and Molecular Pharmacology, 915 W State Street, West Lafayette, Indiana 47907, United States.
Larisa AvramovaPurdue University, Departments of Biological Sciences and Medicinal Chemistry and Molecular Pharmacology, 915 W State Street, West Lafayette, Indiana 47907, United States.
Scott D LarsenUniversity of Michigan, Vahlteich Medicinal Chemistry Core, College of Pharmacy, 428 Church Street, Ann Arbor, Michigan 48109, United States.
John J G TesmerPurdue University, Departments of Biological Sciences and Medicinal Chemistry and Molecular Pharmacology, 915 W State Street, West Lafayette, Indiana 47907, United States.
Andrew D WhiteUniversity of Michigan, Vahlteich Medicinal Chemistry Core, College of Pharmacy, 428 Church Street, Ann Arbor, Michigan 48109, United States.

Funding

Structure, function, and inhibition of G protein-coupled receptor kinasesR01HL071818 · NHLBI · UNIVERSITY OF TEXAS AUSTIN · PI TESMER, JOHN · 2004 to 2023
$7.1M
Structure and Function of the LPLA2/LCAT Acyltransferase FamilyR01HL122416 · NHLBI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI TESMER, JOHN · 2015 to 2018
$1.9M
GPCR - Linked RhoGEFs in Tumor Growth and MetastasisR01CA221289 · NCI · PURDUE UNIVERSITY · PI TESMER, JOHN · 2018 to 2022
$1.9M
NCI NIH HHS R01 CA221289NHLBI NIH HHS R01 HL071818NHLBI NIH HHS R01 HL122416
6 · The paper itself

Abstract

The ability of G protein-coupled receptor (GPCR) kinases (GRKs) to regulate desensitization of GPCRs has made GRK2 and GRK5 attractive targets for treating heart failure and other diseases such as cancer. Although advances have been made toward developing inhibitors that are selective for GRK2, there have been far fewer reports of GRK5 selective compounds. Herein, we describe the development of GRK5 subfamily selective inhibitors,

Identifiers

PMID31857838
PMCPMC6912873

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Registered trials

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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.