Evidence map›Paper›PMID 28495495›Full record

ReviewCellular signalling2018

Translating in vitro ligand bias into in vivo efficacy.

Louis M Luttrell, Stuart Maudsley, Diane Gesty-Palmer

Abstract readReview
In one paragraph

Review in Cellular signalling, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.

0numbers the graph read from it
0cells of the map it votes in
21citing papers in PubMed
3.0field-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

21 citing papers in PubMed, 45 citations in OpenAlex.

  1. Review
  2. G protein-coupled receptor digital twins for precision and personalized medicine.Computational and structural biotechnology journal · 2025
    Review
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  18. G Protein-Coupled Receptor Systems and Their Role in Cellular Senescence.Computational and structural biotechnology journal · 2019
    Review
  19. Review
  20. 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

3 authors at 3 institutions in 2 countries.

Louis M LuttrellDivision of Endocrinology, Diabetes & Medical Genetics, Medical University of South Carolina, Charleston, SC 29425, USA; Research Service of the Ralph H. Johnson Veterans Affairs Medical Center, Charleston, SC, 29401, USA. Electronic address: luttrell@musc.edu.
Stuart MaudsleyTranslational Neurobiology Group, VIB Department of Molecular Genetics, Laboratory of Neurogenetics-Institute Born-Bunge, University of Antwerp, Belgium.
Diane Gesty-PalmerDivision of Endocrinology, Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA.
Duke Medical Center · USMedical University of South Carolina · USVIB-UAntwerp Center for Molecular Neurology · BE

Funding

TYROSINE KINASES IN G PROTEIN MEDIATED SIGNALINGR01DK055524 · NIDDK · MEDICAL UNIVERSITY OF SOUTH CAROLINA · PI LUTTRELL, LOUIS M · 1998 to 2017
$4.6M
Pharmacodynamics of Biased G protein-Coupled Receptor AgonismR01GM095497 · NIGMS · MEDICAL UNIVERSITY OF SOUTH CAROLINA · PI LUTTRELL, LOUIS M · 2013 to 2016
$1.1M
Parathyroid Hormone and Osteoblast MitogenesisR01DK064353 · NIDDK · MEDICAL UNIVERSITY OF SOUTH CAROLINA · PI LUTTRELL, LOUIS M · 2002 to 2005
$937k
Fluorometric Imaging Plate Reader (FLIPRtetra)S10RR027777 · NCRR · MEDICAL UNIVERSITY OF SOUTH CAROLINA · PI LUTTRELL, LOUIS M · 2010 to 2010
$500k
Functionally-selective parathyroid hormone analogs as therapeutics in metabolic bone diseaseI01BX003188 · VA · RALPH H JOHNSON VA MEDICAL CENTER · PI LUTTRELL, LOUIS M · 2017 to 2020
–
BLRD VA I01 BX003188NCRR NIH HHS S10 RR027777NIDDK NIH HHS R01 DK055524NIDDK NIH HHS R01 DK064353NIGMS NIH HHS R01 GM095497
6 · The paper itself

Abstract

It is increasingly apparent that ligand structure influences both the efficiency with which G protein-coupled receptors (GPCRs) engage their downstream effectors and the manner in which they are activated. Thus, 'biased' agonists, synthetic ligands whose intrinsic efficacy differs from the native ligand, afford a strategy for manipulating GPCR signaling in ways that promote beneficial signals while blocking potentially deleterious ones. Still, there are significant challenges in relating in vitro ligand efficacy, which is typically measured in heterologous expression systems, to the biological response in vivo, where the ligand is acting on natively expressed receptors and in the presence of the endogenous ligand. This is particularly true of arrestin pathway-selective 'biased' agonists. The type 1 parathyroid hormone receptor (PTH

Indexed as

AnimalsArrestinsDrug DesignHumansIn Vitro TechniquesLigandsModels, AnimalOsteogenesisOsteoporosisParathyroid HormoneReceptor, Parathyroid Hormone, Type 1Receptors, G-Protein-CoupledArrestinsLigandsParathyroid HormoneReceptor, Parathyroid Hormone, Type 1Receptors, G-Protein-CoupledArrestinG protein-coupled receptorOsteoblastOsteoporosisParathyroid hormonePharmacology

Identifiers

PMID28495495
PMCPMC5675828
OpenAlexW2610298236

What OpenQuestion holds

Textmetadata
LicenceTDM
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.