Evidence mapPaperPMID 39584635Full record

ArticleProteins2025

Unraveling GPCRs Allosteric Modulation. Cannabinoid 1 Receptor as a Case Study.

Alejandro Cruz, Arieh Warshel

Abstract read
In one paragraph

Article in Proteins, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

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

1 citing paper in PubMed.

  1. 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

2 authors.

Alejandro CruzDepartment of Chemistry, University of Southern California, Los Angeles, California, USA.ORCID 0000-0003-0928-0718
Arieh WarshelDepartment of Chemistry, University of Southern California, Los Angeles, California, USA.ORCID 0000-0001-7971-5401

Funding

Multiscale Simulations of Biological Systems and ProcessesR35GM122472 · UNIVERSITY OF SOUTHERN CALIFORNIA · 2025 to 2025
$620k
National Science Foundation MCB 1707167NIGMS NIH HHS R35 GM122472NIH HHS R35 GM122472
6 · The paper itself

Abstract

G-protein-coupled receptors (GPCRs) constitute one of the most prominent families of integral membrane receptor proteins that mediate most transmembrane signaling processes. Malfunction of these signal transduction processes is one of the underlying causes of many human pathologies (Parkinson's, Huntington's, heart diseases, etc), provoking that GPCRs are the largest family of druggable proteins. However, these receptors have been targeted traditionally by orthosteric ligands, which usually causes side effects due to the simultaneous targeting of homologous receptor subtypes. Allosteric modulation offers a promising alternative approach to circumvent this problematic and, thus, comprehending its details is a most important task. Here we use the Cannabinoid type-1 receptor (CB1R) in trying to shed light on this issue, focusing on positive allosteric modulation. This is done by using the protein-dipole Langevin-dipole (PDLD) within the linear response approximation (LRA) framework (PDLD/S-2000) along with our coarse-grained (CG) model of membrane proteins to evaluate the dissociation constants (K

Indexed as

Receptor, Cannabinoid, CB1Allosteric RegulationAllosteric SiteBinding SitesHumansLigandsMolecular Dynamics SimulationProtein BindingLigandsReceptor, Cannabinoid, CB1binding free energy calculationscannabinoid type‐1 receptorcannabinoid type‐1 receptor positive allosteric modulationcooperativity factordissociation constantfolding free energy calculationsGPCRs allosteric modulation

Identifiers

PMID39584635
PMCPMC11879764

What Socratic holds

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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 Socratic graph.