ArticleJournal of theoretical biology2018
Modelling and simulation of biased agonism dynamics at a G protein-coupled receptor.
Article in Journal of theoretical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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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.
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Who cites it
16 citing papers in PubMed, 34 citations in OpenAlex.
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- Loss-of-function GαScience signaling · 2025Article
- Predicting oxytocin binding dynamics in receptor genetic variants through computational modeling.npj women's health · 2025Article
- Agonist efficacy at the βFrontiers in pharmacology · 2025Article
- The affinity-efficacy problem: an essential part of pharmacology education.Royal Society open science · 2024Review
- Modelling altered signalling of G-protein coupled receptors in inflamed environment to advance drug design.Scientific reports · 2023Article
- Quantifying the Kinetics of Signaling and Arrestin Recruitment by Nervous System G-Protein Coupled Receptors.Frontiers in cellular neuroscience · 2021Article
- Mechanobiology predicts raft formations triggered by ligand-receptor activity across the cell membrane.Journal of the mechanics and physics of solids · 2020Article
- Evaluation of the profiles of CBBritish journal of pharmacology · 2020Article
- Analyzing kinetic signaling data for G-protein-coupled receptors.Scientific reports · 2020Article
- 100 years of modelling ligand-receptor binding and response: A focus on GPCRs.British journal of pharmacology · 2020Review
- Engineering G protein-coupled receptor signalling in yeast for biotechnological and medical purposes.FEMS yeast research · 2020Review
- Utilization of Biased G Protein-Coupled ReceptorSignaling towards Development of Safer andPersonalized Therapeutics.Molecules (Basel, Switzerland) · 2019Review
- Article
- Biased Signaling and Allosteric Modulation at the FSHR.Frontiers in endocrinology · 2019Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Theoretical models of G protein-coupled receptor (GPCR) concentration-response relationships often assume an agonist producing a single functional response via a single active state of the receptor. These models have largely been analysed assuming steady-state conditions. There is now much experimental evidence to suggest that many GPCRs can exist in multiple receptor conformations and elicit numerous functional responses, with ligands having the potential to activate different signalling pathways to varying extents-a concept referred to as biased agonism, functional selectivity or pluri-dimensional efficacy. Moreover, recent experimental results indicate a clear possibility for time-dependent bias, whereby an agonist's bias with respect to different pathways may vary dynamically. Efforts towards understanding the implications of temporal bias by characterising and quantifying ligand effects on multiple pathways will clearly be aided by extending current equilibrium binding and biased activation models to include G protein activation dynamics. Here, we present a new model of time-dependent biased agonism, based on ordinary differential equations for multiple cubic ternary complex activation models with G protein cycle dynamics. This model allows simulation and analysis of multi-pathway activation bias dynamics at a single receptor for the first time, at the level of active G protein (α
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Registered trials
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.