関連する実験動画

Updated: Jan 8, 2026

Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay

Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay

Published on: October 2, 2017

オレキシンおよび受容体システムのシグナル伝達、二量体化、および治療標的化

Shengnan Zhang¹, Peixiang Wang¹, Bingyuan Ji¹

¹Neurobiology Key Laboratory of Jining Medical University, Jining, China.

Frontiers in pharmacology

|December 12, 2025

Abstract:

Orexin receptors (OXRs), including OX1R (HCRTR1) and OX2R (HCRTR2), are G protein-coupled receptors (GPCRs) that are activated by endogenous orexin peptides (OXA and OXB) and have potential pleiotropic effects in nervous system, which makes them highly valuable therapeutic targets. Emerging evidence indicates that OXRs exhibit a significant propensity to form homodimers and heterodimers with various GPCRs, generating biased signaling that may offer a platform for precision pharmacology and enable the design of pathway-specific drugs with fewer off-target effects. Current and emerging OXR antagonists demonstrate efficacy in sleep disorders, metabolic dysregulation, and psychiatric conditions. Furthermore, transmembrane (TM) peptides targeting specific dimer interfaces represent a novel therapeutic strategy. This review synthesizes current understanding of orexin receptor systems, focusing on the structural composition, signal transduction pathways, dimerization properties, and antagonist compounds of OXRs. We present a comprehensive overview of the current state of research, investigate the molecular pathological mechanisms associated with neurological disorders, and evaluate potential therapeutic targets for pharmaceutical development.

キーワード:

GPCRシグナル伝達 GPCR うつ病神経学神経薬理学

さらに関連する動画

Identification of Orexin and Endocannabinoid Receptors in Adult Zebrafish Using Immunoperoxidase and Immunofluorescence Methods

Identification of Orexin and Endocannabinoid Receptors in Adult Zebrafish Using Immunoperoxidase and Immunofluorescence Methods

Published on: June 25, 2019

HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice

HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice

Published on: July 9, 2016

関連する概念動画

Opioid Receptors: Overview

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2,...

Signal Transduction: Overview

Signal Transduction: Overview

Cells respond to many types of information, often through receptor proteins positioned on the membrane. They respond to chemical signals, such as hormones, neurotransmitters, and other signaling molecules, initiating a series of molecular reactions to produce an appropriate response. This is called signal transduction. Cells also coordinate different responses elicited by the same signaling molecule via mediators, allowing molecular cross-talk.
Typically, signal transduction involves three...

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...

Transducer Mechanism: Enzyme-Linked Receptors

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:

Drug-Receptor Interaction: Agonist

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous...

Interactions Between Signaling Pathways

Interactions Between Signaling Pathways

Signaling cascades usually lack linearity. Multiple pathways interact and regulate one another, allowing cells to integrate and respond to diverse environmental stimuli.
Convergence and divergence, and cross-talk between signaling pathways
Two distinct signaling pathways can converge on a single functional unit, which may either be a single protein or a complex of proteins. The response is either functionally distinct or synergistic between the two pathways but different from the response...