Journal ArticleDOI
Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
TLDR
The new findings suggest an expansion of the classical ternary complex model of receptor action to include an explicit isomerization of the receptors from an inactive to an active state which couples to the G protein ('allosteric ternARY complex model').About:
This article is published in Trends in Pharmacological Sciences.The article was published on 1993-08-01. It has received 815 citations till now. The article focuses on the topics: G protein & GTP-binding protein regulators.read more
Citations
More filters
Journal ArticleDOI
Dopamine Receptors: From Structure to Function
TL;DR: Target deletion of several of these dopamine receptor genes in mice should provide valuable information about their physiological functions and provide unequivocal evidence for the involvement of one of these receptors in the etiology of various central nervous system disorders.
Journal ArticleDOI
Uncovering Molecular Mechanisms Involved in Activation of G Protein-Coupled Receptors
TL;DR: The goal of the present review is to specifically address the physical changes linking agonist binding to receptor activation and subsequent transduction of the signal to the associated G protein on the cytoplasmic side of the membrane and to other putative signaling pathways.
Journal ArticleDOI
Binding, gating, affinity and efficacy: The interpretation of structure-activity relationships for agonists and of the effects of mutating receptors
TL;DR: Making this distinction between ecacy has no upper limit in principle, and that when it is large, changes in it are indistinguishable from changes in anity is arguably the fundamental problem of modern molecular studies of receptors.
Journal ArticleDOI
Allosteric mechanisms of signal transduction.
TL;DR: The MWC theory and its applications for the understanding of signal transduction in biology are reviewed, and remaining issues that deserve theoretical and experimental substantiation are identified.
Journal ArticleDOI
Human herpesvirus KSHV encodes a constitutively active G-protein-coupled receptor linked to cell proliferation
Leandros Arvanitakis,Elizabeth Geras-Raaka,Anjali Varma,Marvin C. Gershengorn,Ethel Cesarman +4 more
TL;DR: It is shown that the KSHV G-protein-coupled receptor is a bona fide signalling receptor which has constitutive (agonist-independent) activity in the phosphoinositide–inositoltrisphosphate–protein kinase C pathway, making it a candidate viral oncogene.
References
More filters
Journal ArticleDOI
A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.
TL;DR: In this paper, a ternary complex model was used to fit the data with high accuracy under conditions where the ligand used is either a full or a partial agonist and where the system is altered by the addition of guanine nucleotide or after treatment with group-specific reagents.
Journal ArticleDOI
Model systems for the study of seven-transmembrane-segment receptors.
TL;DR: This paper presents a meta-analyses of the chiral signaling process and its applications in medicine and animal welfare, and investigates the role of chiral reprograming in the development of Alzheimer's disease.
Journal ArticleDOI
A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.
TL;DR: The experimental findings with the mutant receptor cannot be adequately rationalized within the theoretical framework of the Ternary Complex Model, and an extended version of this model that includes an explicit isomerization of the receptor to an active state closely models all the findings for both the mutant and the wild-type receptors.
Journal ArticleDOI
Pigmentation phenotypes of variant extension locus alleles result from point mutations that alter MSH receptor function
Linda S. Robbins,Joseph H. Nadeau,Kenneth R. Johnson,Michele A. Kelly,Linda Roselli-Rehfuss,Eric Baack,Kathleen G. Mountjoy,Roger D. Cone +7 more
TL;DR: It is shown here that the murine extension locus encodes the melanocyte-stimulating hormone (MSH) receptor, and that the Eso-3J receptor is constitutively activated, while the Etob receptor remains hormone responsive and produces a greater activation of its effector than does the wild-type allele.
Journal ArticleDOI
Constitutive activation of the alpha 1B-adrenergic receptor by all amino acid substitutions at a single site. Evidence for a region which constrains receptor activation.
TL;DR: This set of mutated receptors exhibits a graded range of elevated biological activities, apparently representing a spectrum of receptor conformations which mimic the "active" state of the wild type receptor.