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Identification of a serotonin/glutamate receptor complex implicated in psychosis
TLDR
It is shown that the mGluR2 interacts through specific transmembrane helix domains with the 2AR, a member of an unrelated G-protein-coupled receptor family, to form functional complexes in brain cortex that may be involved in the altered cortical processes of schizophrenia. Expand
Dopamine D2 receptors form higher order oligomers at physiological expression levels
TLDR
It is combined bioluminescence/fluorescence complementation and energy transfer to demonstrate that at least four dopamine D2 receptors are located in close molecular proximity in living mammalian cells, consistent with their organization as higher order oligomers at the plasma membrane. Expand
Decoding the Signaling of a GPCR Heteromeric Complex Reveals a Unifying Mechanism of Action of Antipsychotic Drugs
TLDR
It is shown that a heteromeric complex between the 2AR and the G(i)-linked GPCR, metabotropic glutamate 2 receptor (mGluR2), integrates ligand input, modulating signaling output and behavioral changes, and provides mechanistic insight into antipsychotic action that may advance therapeutic strategies for disorders including schizophrenia and dementia. Expand
G Protein–Coupled Receptor Oligomerization Revisited: Functional and Pharmacological Perspectives
TLDR
The functional and pharmacological properties of GPCR oligomers are reviewed and some guidelines for the application of discrete direct screening and high-throughput screening approaches to the discovery of receptor-heteromer selective compounds are provided. Expand
Synthetic and Receptor Signaling Explorations of the Mitragyna Alkaloids: Mitragynine as an Atypical Molecular Framework for Opioid Receptor Modulators.
TLDR
The Mitragyna alkaloid scaffold represents a novel framework for the development of functionally biased opioid modulators, which may exhibit improved therapeutic profiles and elucidation of previously unexplored structure-activity relationships within the Mitragynine scaffold. Expand
Crosstalk in G protein-coupled receptors: changes at the transmembrane homodimer interface determine activation.
TLDR
This work has mapped the homodimer interface in the dopamine D2 receptor over the entire length of the fourth transmembrane segment (TM4) by crosslinking of substituted cysteines by identifying a conformational change at the TM4 dimer interface that is part of the receptor activation mechanism. Expand
Inward-facing conformation of the zinc transporter YiiP revealed by cryoelectron microscopy
TLDR
Cryoelectron microscopy and molecular dynamics simulation of YiiP in a lipid environment were used to address the feasibility of a conformational change that involves pivoting of a transmembrane, four-helix bundle relative to the M3-M6 helix pair. Expand
The study of G‐protein coupled receptor oligomerization with computational modeling and bioinformatics
TLDR
The main approaches from bioinformatics, enhanced by computational molecular modeling, that have been used to predict likely interfaces of dimerization/oligomerization of GPCRs are reviewed, and results from their application to rhodopsin‐like GPCrs are compared. Expand
Structural basis of TRPV5 channel inhibition by econazole revealed by cryo-EM
TLDR
The cryo-EM structure of the full-length TRPV5 channel in complex with inhibitor econazole reveals a domain-swapped architecture and provides insights into mechanisms of inhibition, suggesting conserved mechanisms for ligand recognition and lipid binding amongTRPV channels. Expand
International Union of Basic and Clinical Pharmacology. LXVII. Recommendations for the Recognition and Nomenclature of G Protein-Coupled Receptor Heteromultimers
TLDR
The present article illustrates well-documented examples of such native multimeric GPCR complexes, lists a number of recommendations for recognition and acceptance of suchMultimeric receptors, and gives recommendations for their nomenclature. Expand
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