Evidence map›Paper›PMID 32234810›Full record

ArticleMolecular pharmacology2020

A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the

Renee A Bouley, Zara Y Weinberg, Helen V Waldschmidt, Yu-Chen Yen, Scott D Larsen, Manojkumar A Puthenveedu, John J G Tesmer

Open access · bronzeAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecular pharmacology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
1.1field-weighted citation impact, top 24% 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

17 citing papers in PubMed, 24 citations in OpenAlex.

  1. Review
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  13. GRK2 in cardiovascular disease and its potential as a therapeutic target.Journal of molecular and cellular cardiology · 2022
    Review
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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

7 authors at 1 institution in 1 country.

Renee A BouleyLife Sciences Institute (R.A.B., H.V.W.), Departments of Medicinal Chemistry (H.V.W., S.D.L.) and Pharmacology (R.A.B., Z.Y.W., M.A.P.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (H.V.W., S.D.L.), University of Michigan, Ann Arbor, Michigan; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology (Y.-C.Y., J.J.G.T.), Purdue University, West Lafayette, Indiana.ORCID 0000-0002-1358-0994
Zara Y WeinbergLife Sciences Institute (R.A.B., H.V.W.), Departments of Medicinal Chemistry (H.V.W., S.D.L.) and Pharmacology (R.A.B., Z.Y.W., M.A.P.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (H.V.W., S.D.L.), University of Michigan, Ann Arbor, Michigan; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology (Y.-C.Y., J.J.G.T.), Purdue University, West Lafayette, Indiana.ORCID 0000-0001-7176-038X
Helen V WaldschmidtLife Sciences Institute (R.A.B., H.V.W.), Departments of Medicinal Chemistry (H.V.W., S.D.L.) and Pharmacology (R.A.B., Z.Y.W., M.A.P.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (H.V.W., S.D.L.), University of Michigan, Ann Arbor, Michigan; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology (Y.-C.Y., J.J.G.T.), Purdue University, West Lafayette, Indiana.
Yu-Chen YenLife Sciences Institute (R.A.B., H.V.W.), Departments of Medicinal Chemistry (H.V.W., S.D.L.) and Pharmacology (R.A.B., Z.Y.W., M.A.P.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (H.V.W., S.D.L.), University of Michigan, Ann Arbor, Michigan; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology (Y.-C.Y., J.J.G.T.), Purdue University, West Lafayette, Indiana.
Scott D LarsenLife Sciences Institute (R.A.B., H.V.W.), Departments of Medicinal Chemistry (H.V.W., S.D.L.) and Pharmacology (R.A.B., Z.Y.W., M.A.P.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (H.V.W., S.D.L.), University of Michigan, Ann Arbor, Michigan; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology (Y.-C.Y., J.J.G.T.), Purdue University, West Lafayette, Indiana.
Manojkumar A PuthenveeduLife Sciences Institute (R.A.B., H.V.W.), Departments of Medicinal Chemistry (H.V.W., S.D.L.) and Pharmacology (R.A.B., Z.Y.W., M.A.P.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (H.V.W., S.D.L.), University of Michigan, Ann Arbor, Michigan; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology (Y.-C.Y., J.J.G.T.), Purdue University, West Lafayette, Indiana.ORCID 0000-0002-3177-4231
John J G TesmerLife Sciences Institute (R.A.B., H.V.W.), Departments of Medicinal Chemistry (H.V.W., S.D.L.) and Pharmacology (R.A.B., Z.Y.W., M.A.P.), and Vahlteich Medicinal Chemistry Core, College of Pharmacy (H.V.W., S.D.L.), University of Michigan, Ann Arbor, Michigan; and Departments of Biological Sciences and of Medicinal Chemistry and Molecular Pharmacology (Y.-C.Y., J.J.G.T.), Purdue University, West Lafayette, Indiana jtesmer@purdue.edu.ORCID 0000-0003-1125-3727
Purdue University West Lafayette · US

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
MECHANISMS ENSURING SEQUENCE-DEPENDENT GPCR RECYCLINGR01GM117425 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI PUTHENVEEDU, MANOJKUMAR A · 2016 to 2020
$1.5M
NHLBI NIH HHS R01 HL071818NHLBI NIH HHS R01 HL122416NIGMS NIH HHS R01 GM117425
6 · The paper itself

Abstract

G protein-coupled receptor (GPCR) kinases (GRKs) play a key role in terminating signals initiated by agonist-bound GPCRs. However, chronic stimulation of GPCRs, such as that which occurs during heart failure, leads to the overexpression of GRKs and maladaptive downregulation of GPCRs on the cell surface. We previously reported the discovery of potent and selective families of GRK inhibitors based on either the paroxetine or

Indexed as

AnimalsBlotting, WesternCell Membrane PermeabilityCrystallography, X-RayFemaleHEK293 CellsHumansIndazolesMiceMicrosomes, LiverMolecular StructureParoxetinePyrimidinesReceptors, Opioid, muGSK180736AIndazolesOPRM1 protein, humanParoxetinePyrimidinesReceptors, Opioid, mu

Identifiers

PMID32234810
PMCPMC7237867
OpenAlexW3014668246

What Socratic 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 Socratic graph.