Evidence map›Paper›PMID 34251810›Full record

ArticleJournal of chemical information and modeling2021

Delineating the Ligand-Receptor Interactions That Lead to Biased Signaling at the μ-Opioid Receptor.

Brendan Kelly, Scott A Hollingsworth, David C Blakemore, Robert M Owen, R Ian Storer, Nigel A Swain, Deniz Aydin, Rubben Torella, Joseph S Warmus, Ron O Dror

Open access · greenAbstract read
In one paragraph

Article in Journal of chemical information and modeling, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
1.4field-weighted citation impact, top 19% 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

20 citing papers in PubMed, 29 citations in OpenAlex.

  1. Article
  2. Article
  3. Structure-Bias Relationship of μ-Opioid Receptor Agonists.Handbook of experimental pharmacology · 2026
    Review
  4. Rational Design Biased Compounds against μ‑Opioid Receptor.ACS pharmacology & translational science · 2025
    Article
  5. Article
  6. Article
  7. Review
  8. Article
  9. Article
  10. Review
  11. Article
  12. The Art and Science of Molecular Docking.Annual review of biochemistry · 2024
    Review
  13. Review
  14. Article
  15. Article
  16. Review
  17. Article
  18. Structure-Based Evolution of G Protein-Biased μ-Opioid Receptor Agonists.Angewandte Chemie (International ed. in English) · 2022
    Article
  19. Article
  20. Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs.International journal of molecular sciences · 2021
    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

10 authors at 3 institutions in 2 countries.

Brendan KellyDepartments of Computer Science, Molecular and Cellular Physiology, and Structural Biology & Institute for Computational and Mathematical Engineering, Stanford University, Stanford, California 94305, United States.
Scott A HollingsworthDepartments of Computer Science, Molecular and Cellular Physiology, and Structural Biology & Institute for Computational and Mathematical Engineering, Stanford University, Stanford, California 94305, United States.ORCID 0000-0003-3294-0083
David C BlakemorePfizer Medicine Design, Eastern Point Road, Groton, Connecticut 06340, United States.
Robert M OwenPfizer Medicine Design, The Portway, Granta Park, Cambridge CB21 6GS, U.K.ORCID 0000-0002-3359-8614
R Ian StorerPfizer Medicine Design, The Portway, Granta Park, Cambridge CB21 6GS, U.K.
Nigel A SwainPfizer Medicine Design, The Portway, Granta Park, Cambridge CB21 6GS, U.K.ORCID 0000-0002-8014-2134
Deniz AydinDepartments of Computer Science, Molecular and Cellular Physiology, and Structural Biology & Institute for Computational and Mathematical Engineering, Stanford University, Stanford, California 94305, United States.
Rubben TorellaPfizer Medicine Design, 610 Main Street, Cambridge, Massachusetts 02139, United States.
Joseph S WarmusPfizer Medicine Design, Eastern Point Road, Groton, Connecticut 06340, United States.
Ron O DrorDepartments of Computer Science, Molecular and Cellular Physiology, and Structural Biology & Institute for Computational and Mathematical Engineering, Stanford University, Stanford, California 94305, United States.ORCID 0000-0002-6418-2793
Stanford University · USGranta Design (United Kingdom) · GBPfizer (United States) · US

Funding

POSTDOCTORAL TRAINING IN MEDICAL INFORMATION SCIENCEST15LM007033 · NLM · STANFORD UNIVERSITY · PI SYLVIA KATINA PLEVRITIS · 1985 to 2026
$25.5M
Discovering the mechanism of GPCR-mediated arrestin stimulation to enable effective drug therapiesR01GM127359 · NIGMS · STANFORD UNIVERSITY · PI DROR, RON · 2018 to 2022
$1.5M
NIGMS NIH HHS R01 GM127359NLM NIH HHS T15 LM007033
6 · The paper itself

Abstract

Biased agonists, which selectively stimulate certain signaling pathways controlled by a G protein-coupled receptor (GPCR), hold great promise as drugs that maximize efficacy while minimizing dangerous side effects. Biased agonists of the μ-opioid receptor (μOR) are of particular interest as a means to achieve analgesia through G protein signaling without dose-limiting side effects such as respiratory depression and constipation. Rational structure-based design of biased agonists remains highly challenging, however, because the ligand-mediated interactions that are key to activation of each signaling pathway remain unclear. We identify several compounds for which the

Indexed as

Receptors, Opioid, muSignal TransductionGTP-Binding ProteinsHumansLigandsPainProtein BindingGTP-Binding ProteinsLigandsReceptors, Opioid, mu

Identifiers

PMID34251810
PMCPMC8317888
OpenAlexW3183113611

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.