Evidence map›Paper›PMID 25737495›Full record

ReviewMolecular pharmacology2015

G Protein-Coupled Receptor (GPCR) Expression in Native Cells: "Novel" endoGPCRs as Physiologic Regulators and Therapeutic Targets.

Paul A Insel, Andrea Wilderman, Alexander C Zambon, Aaron N Snead, Fiona Murray, Nakon Aroonsakool, Daniel S McDonald, Shu Zhou, Thalia McCann, Lingzhi Zhang and 6 more

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

Review in Molecular pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.

0numbers the graph read from it
0cells of the map it votes in
36citing papers in PubMed
2.9field-weighted citation impact, top 9% 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

36 citing papers in PubMed, 63 citations in OpenAlex.

  1. Local GPCR density tips the balance of μ-opioid receptor trafficking.bioRxiv : the preprint server for biology · 2026
    Article
  2. Article
  3. Article
  4. Shifting our perspective on orphan G protein-coupled receptors.Nature structural & molecular biology · 2024
    Article
  5. Article
  6. Expanding the GPCR-RAMP interactome.bioRxiv : the preprint server for biology · 2023
    Article
  7. Article
  8. Article
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  11. Article
  12. 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

16 authors at 1 institution in 1 country.

Paul A InselDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California pinsel@ucsd.edu.
Andrea WildermanDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Alexander C ZambonDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Aaron N SneadDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Fiona MurrayDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Nakon AroonsakoolDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Daniel S McDonaldDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Shu ZhouDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Thalia McCannDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Lingzhi ZhangDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Krishna SriramDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Amy M ChinnDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Alexander V MichkovDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Rebecca M LynchDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Aaron C OverlandDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
Ross CorridenDepartments of Pharmacology (P.A.I., A.W., A.C.Z., A.N.S., N.A., D.S.M., S.Z., T.M., L.Z., K.S., A.M.C., A.V.M., R.M.L., A.C.O., R.C.) and Medicine (P.A.I., F.M.), University of California, San Diego, La Jolla, California.
University of California, San Diego · US

Funding

Vector Production CoreP01HL066941 · NHLBI · VETERANS MEDICAL RESEARCH FDN/SAN DIEGO · PI MIYANOHARA, ATSUSHI · 2001 to 2017
$34.8M
UCSD/SDSU IRACDAK12GM068524 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI TREJO, JOANN · 2003 to 2025
$24.4M
GRADUATE TRAINING IN CELLULAR &MOLECULAR PHARMACOLOGYT32GM007752 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI BROWN, JOAN HELLER, HANDEL, TRACY M · 1985 to 2023
$13.5M
Training In Cardiovascular Physiology & PharmacologyT32HL007444 · NHLBI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI Ju Chen, Robert Scott Ross · 1985 to 2026
$11.1M
UCSD Cancer Center Training Program in Drug DevelopmentT32CA121938 · NCI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI Michael Bouvet, Dwayne G. Stupack · 2006 to 2026
$10.3M
Training Grant in GastroenterologyT32DK007202 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI GHOSH, PRADIPTA · 1985 to 2022
$7.7M
Phosphodiesterase-1 in Pulmonary Hypertension: Expression, Regulation, and TargetR00HL091061 · NHLBI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI MURRAY, FIONA · 2010 to 2012
$743k
GPCRs: novel targets in cancer-associated fibroblastsR21CA189477 · NCI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI INSEL, PAUL A, LOWY, ANDREW M · 2014 to 2015
$371k
Phosphodiesterase-1 in Pulmonary Hypertension: Expression, Regulation, and TargetK99HL091061 · NHLBI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI MURRAY, FIONA · 2008 to 2009
$167k
NCI NIH HHS CA121938NCI NIH HHS CA189477NCI NIH HHS R21 CA189477NCI NIH HHS T32 CA121938NHLBI NIH HHS HL007444NHLBI NIH HHS HL066941NHLBI NIH HHS HL091061NHLBI NIH HHS K99 HL091061NHLBI NIH HHS P01 HL066941NHLBI NIH HHS R00 HL091061NHLBI NIH HHS T32 HL007444NIDDK NIH HHS T32 DK007202NIGMS NIH HHS GM-68524NIGMS NIH HHS GM68524NIGMS NIH HHS K12 GM068524NIGMS NIH HHS T32 GM007752
6 · The paper itself

Abstract

G protein-coupled receptors (GPCRs), the largest family of signaling receptors in the human genome, are also the largest class of targets of approved drugs. Are the optimal GPCRs (in terms of efficacy and safety) currently targeted therapeutically? Especially given the large number (∼ 120) of orphan GPCRs (which lack known physiologic agonists), it is likely that previously unrecognized GPCRs, especially orphan receptors, regulate cell function and can be therapeutic targets. Knowledge is limited regarding the diversity and identity of GPCRs that are activated by endogenous ligands and that native cells express. Here, we review approaches to define GPCR expression in tissues and cells and results from studies using these approaches. We identify problems with the available data and suggest future ways to identify and validate the physiologic and therapeutic roles of previously unrecognized GPCRs. We propose that a particularly useful approach to identify functionally important GPCRs with therapeutic potential will be to focus on receptors that show selective increases in expression in diseased cells from patients and experimental animals.

Indexed as

AnimalsGene Expression ProfilingGene Expression RegulationHumansMolecular Targeted TherapyReceptors, G-Protein-CoupledTissue DistributionReceptors, G-Protein-Coupled

Identifiers

PMID25737495
PMCPMC4468643
OpenAlexW2240242048

What OpenQuestion holds

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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.