Literature DB >> 19347339

Modelling of the activation of G-protein coupled receptors: drug free constitutive receptor activity.

P J Woodroffe1, L J Bridge, J R King, C Y Chen, S J Hill.   

Abstract

G-protein coupled receptors (GPCRs) form a crucial component of approximately 80% of hormone pathways. In this paper, the most popular mechanism for activation of GPCRs-the shuttling mechanism-is modelled mathematically. An asymptotic analysis of this model clarifies the dynamics of the system in the absence of drug, in particular which reactions dominate during the different timescales. Equilibrium analysis of the model demonstrates the model's ability to predict constitutive receptor activity.

Mesh:

Substances:

Year:  2009        PMID: 19347339     DOI: 10.1007/s00285-009-0268-5

Source DB:  PubMed          Journal:  J Math Biol        ISSN: 0303-6812            Impact factor:   2.259


  19 in total

Review 1.  Inverse, protean, and ligand-selective agonism: matters of receptor conformation.

Authors:  T Kenakin
Journal:  FASEB J       Date:  2001-03       Impact factor: 5.191

Review 2.  Modelling of promiscuous receptor-Gi/Gs-protein coupling and effector response.

Authors:  J P Kukkonen; J Näsman; K E Akerman
Journal:  Trends Pharmacol Sci       Date:  2001-12       Impact factor: 14.819

3.  Modelling of signalling via G-protein coupled receptors: pathway-dependent agonist potency and efficacy.

Authors:  C Y Chen; Y Cordeaux; S J Hill; J R King
Journal:  Bull Math Biol       Date:  2003-09       Impact factor: 1.758

4.  Modelling the activation of G-protein coupled receptors by a single drug.

Authors:  P J Woodroffe; L J Bridge; J R King; S J Hill
Journal:  Math Biosci       Date:  2009-02-26       Impact factor: 2.144

Review 5.  Drug efficacy at G protein-coupled receptors.

Authors:  Terry Kenakin
Journal:  Annu Rev Pharmacol Toxicol       Date:  2002       Impact factor: 13.820

Review 6.  A three-state receptor model of agonist action.

Authors:  P Leff; C Scaramellini; C Law; K McKechnie
Journal:  Trends Pharmacol Sci       Date:  1997-10       Impact factor: 14.819

7.  A theoretical approach to G-protein modulation of cellular responsiveness.

Authors:  J Nauroschat; U an der Heiden
Journal:  J Math Biol       Date:  1997-05       Impact factor: 2.259

Review 8.  Rethinking receptor-G protein-effector interactions.

Authors:  P Chidiac
Journal:  Biochem Pharmacol       Date:  1998-03-01       Impact factor: 5.858

9.  Metabotropic receptor activation, desensitization and sequestration-I: modelling calcium and inositol 1,4,5-trisphosphate dynamics following receptor activation.

Authors:  G Lemon; W G Gibson; M R Bennett
Journal:  J Theor Biol       Date:  2003-07-07       Impact factor: 2.691

10.  A mathematical model for ligand/receptor/G-protein dynamics and actin polymerization in human neutrophils.

Authors:  J A Adams; G M Omann; J J Linderman
Journal:  J Theor Biol       Date:  1998-08-21       Impact factor: 2.691

View more
  3 in total

1.  Pancreatic Beta Cell G-Protein Coupled Receptors and Second Messenger Interactions: A Systems Biology Computational Analysis.

Authors:  Leonid E Fridlyand; Louis H Philipson
Journal:  PLoS One       Date:  2016-05-03       Impact factor: 3.240

2.  Modelling and simulation of biased agonism dynamics at a G protein-coupled receptor.

Authors:  L J Bridge; J Mead; E Frattini; I Winfield; G Ladds
Journal:  J Theor Biol       Date:  2018-01-12       Impact factor: 2.691

3.  Ligand Binding Dynamics for Pre-dimerised G Protein-Coupled Receptor Homodimers: Linear Models and Analytical Solutions.

Authors:  Carla White; Lloyd J Bridge
Journal:  Bull Math Biol       Date:  2018-01-18       Impact factor: 1.758

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.