Evidence map›Paper›PMID 20431569›Full record

ReviewNature reviews. Drug discovery2010

Teaching old receptors new tricks: biasing seven-transmembrane receptors.

Sudarshan Rajagopal, Keshava Rajagopal, Robert J Lefkowitz

Abstract readReview
In one paragraph

Review in Nature reviews. Drug discovery, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 431 papers.

0numbers the graph read from it
0cells of the map it votes in
431citing papers in PubMed
39.2field-weighted citation impact, top 1% 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

431 citing papers in PubMed, 808 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Article
  6. Review
  7. Article
  8. Article
  9. Article
  10. Biased Allosteric Modulation in GPCR Drug Discovery.Handbook of experimental pharmacology · 2026
    Review
  11. Article
  12. KCTD Family: Emerging Regulators of GPCR Biased Signaling.Handbook of experimental pharmacology · 2026
    Review
  13. Review
  14. CXCR1 and CXCR2 display receptor bias for shared chemokine agonists.bioRxiv : the preprint server for biology · 2025
    Article
  15. Review
  16. Rewiring βSignal transduction and targeted therapy · 2025
    Article
  17. Review
  18. Article
  19. Article
  20. Article

371 more citing papers are in PubMed but not listed here.

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 2 institutions in 1 country.

Sudarshan RajagopalDepartment of Medicine, Duke University Medical Center, 2301 Erwin Road, Durham, North Carolina 27710, USA.
Keshava Rajagopal
Robert J Lefkowitz
Duke Medical Center · USDuke University Hospital · US

Funding

Molecular Regulation of Cardiovascular 7 TM ReceptorsR01HL016037 · NHLBI · DUKE UNIVERSITY · PI ROBERT J LEFKOWITZ · 1985 to 2026
$14.5M
MULTIDISCIPLINARY HEART &VASCULAR DISEASEST32HL007101 · NHLBI · DUKE UNIVERSITY · PI FREEDMAN, NEIL J. · 1985 to 2020
$9.8M
B-Arrestins and G Protein-Coupled Receptor Kinases in Cardiovascular FunctionR01HL070631 · NHLBI · DUKE UNIVERSITY · PI LEFKOWITZ, ROBERT J · 2002 to 2011
$3.5M
MOLECULAR PROPERTIES OF CARDIAC ADRENERGIC RECEPTORSR37HL016037 · NHLBI · DUKE UNIVERSITY · PI LEFKOWITZ, ROBERT J · 1986 to 1995
–
NHLBI NIH HHS HL07101-34NHLBI NIH HHS HL16037NHLBI NIH HHS HL70631NHLBI NIH HHS R01 HL016037NHLBI NIH HHS R01 HL070631NHLBI NIH HHS T32 HL007101
6 · The paper itself

Abstract

Seven-transmembrane receptors (7TMRs; also known as G protein-coupled receptors) are the largest class of receptors in the human genome and are common targets for therapeutics. Originally identified as mediators of 7TMR desensitization, beta-arrestins (arrestin 2 and arrestin 3) are now recognized as true adaptor proteins that transduce signals to multiple effector pathways. Signalling that is mediated by beta-arrestins has distinct biochemical and functional consequences from those mediated by G proteins, and several biased ligands and receptors have been identified that preferentially signal through either G protein- or beta-arrestin-mediated pathways. These ligands are not only useful tools for investigating the biochemistry of 7TMR signalling, they also have the potential to be developed into new classes of therapeutics.

Indexed as

Drug Delivery SystemsAnimalsArrestinsbeta-ArrestinsDrug DesignGenome, HumanHumansLigandsReceptors, G-Protein-CoupledSignal Transductionarrestin3Arrestinsbeta-ArrestinsLigandsReceptors, G-Protein-Coupledseven-transmembrane G-protein-coupled receptor

Identifiers

PMID20431569
PMCPMC2902265
OpenAlexW2147196684

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.