Evidence map›Paper›PMID 24662799›Full record

ReviewCurrent opinion in pharmacology2014

Muscarinic acetylcholine receptor X-ray structures: potential implications for drug development.

Andrew C Kruse, Jianxin Hu, Brian K Kobilka, Jürgen Wess

Open access · greenAbstract readReview
In one paragraph

Review in Current opinion in pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.

0numbers the graph read from it
0cells of the map it votes in
22citing papers in PubMed
2.6field-weighted citation impact, top 10% 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

22 citing papers in PubMed, 45 citations in OpenAlex.

  1. Article
  2. Article
  3. Approaching Pharmacological Space: Events and Components.Methods in molecular biology (Clifton, N.J.) · 2025
    Article
  4. Review
  5. Review
  6. Journal of chemical information and modeling · 2023
    Article
  7. Article
  8. Article
  9. Review
  10. Crystal structure of the MProceedings of the National Academy of Sciences of the United States of America · 2019
    Article
  11. Article
  12. Characterization of methanthelinium binding and function at human MNaunyn-Schmiedeberg's archives of pharmacology · 2018
    Article
  13. Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. Article
  19. Review
  20. Article
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

4 authors at 2 institutions in 1 country.

Andrew C KruseDepartment of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, CA, USA. Electronic address: akruse@stanford.edu.
Jianxin HuMolecular Signaling Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, MD, USA.
Brian K KobilkaDepartment of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, CA, USA.
Jürgen WessMolecular Signaling Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, MD, USA. Electronic address: jurgenw@helix.nih.gov.
National Institute of Diabetes and Digestive and Kidney Diseases · USStanford University · US

Funding

Molecular Biophysics Training Program at StanfordT32GM008294 · NIGMS · STANFORD UNIVERSITY · PI HUANG, KERWYN C. · 1989 to 2019
$7.4M
Molecular basis of G protein-coupled receptor functionZIADK031129 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI WESS, JURGEN · 2009 to 2025
$6.7M
Structure-based discovery of allosteric ligands for G Protein Coupled ReceptorsU19GM106990 · NIGMS · STANFORD UNIVERSITY · PI KOBILKA, BRIAN K · 2013 to 2017
$6.3M
ADENOVIRUS EIA INDUCTION OF CLASS II TRANSCRIPTIONF32GM010699 · NIGMS · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI BRUNET, LISA J · 1985 to 1987
–
Intramural NIH HHS ZIA DK031129NIGMS NIH HHS T32 GM008294NIGMS NIH HHS U19GM10699NIGMS NIH HHS U19 GM106990
6 · The paper itself

Abstract

Muscarinic acetylcholine receptor antagonists are widely used as bronchodilating drugs in pulmonary medicine. The therapeutic efficacy of these agents depends on the blockade of M3 muscarinic receptors expressed on airway smooth muscle cells. All muscarinic antagonists currently used as bronchodilating agents show high affinity for all five muscarinic receptor subtypes, thus increasing the likelihood of unwanted side effects. Recent X-ray crystallographic studies have provided detailed structural information about the nature of the orthosteric muscarinic binding site (the conventional acetylcholine binding site) and an 'outer' receptor cavity that can bind allosteric (non-orthosteric) drugs. These new findings should guide the development of selective M3 receptor blockers that have little or no effect on other muscarinic receptor subtypes.

Indexed as

AnimalsCholinergic AgentsCrystallography, X-RayDrug DiscoveryHumansReceptor, Muscarinic M2Receptor, Muscarinic M3Scopolamine DerivativesTiotropium BromideCholinergic AgentsReceptor, Muscarinic M2Receptor, Muscarinic M3Scopolamine DerivativesTiotropium Bromide

Identifiers

PMID24662799
PMCPMC4065632
OpenAlexW2052064677

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.