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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

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Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high...
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G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

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GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
4.8K
Osteoclasts in Bone Remodeling01:31

Osteoclasts in Bone Remodeling

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Osteoclasts are cells responsible for bone resorption and remodeling. They originate from hematopoietic progenitor cells present in the bone marrow. Numerous progenitor cells fuse to form multinucleated cells, each with 10-20 nuclei. A single osteoclast has a diameter of 150 to 200 µM. These cells have ruffled borders that break down the underlying bone tissue and release minerals such as calcium into the blood in bone resorption. Osteoclasts cling to bones with their ruffled edges during...
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Related Experiment Video

Updated: Sep 10, 2025

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

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The function of GPCRs in different bone cells.

Yan Zhang1,2, Nai-Ning Wang1,3, Zi-Han Qiu1

  • 1Key Laboratory of Biomedical Information Engineering of Ministry of Education, Key Laboratory of Biology Multiomics and Diseases in Shaanxi Province Higher Education Institutions, and Biomedical Informatics & Genomics Center, School of Life Science and Technology, Xi'an Jiaotong University, Xi'an, Shaanxi, 710049, China.

International Journal of Biological Sciences
|August 27, 2025
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) are key targets for bone disorders. This review details GPCRs in bone cells, offering insights into new therapies for skeletal diseases like osteoporosis and arthritis.

Keywords:
GPCRMSCchondrocyteosteoblastosteoclast

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Area of Science:

  • Skeletal Biology and Pharmacology
  • Cellular and Molecular Medicine

Background:

  • G protein-coupled receptors (GPCRs) play crucial roles in regulating bone cell function and skeletal homeostasis.
  • Dysregulation of GPCR signaling is implicated in various bone disorders, highlighting their therapeutic potential.

Purpose of the Study:

  • To systematically review and catalog GPCR expression and function across diverse bone cell types.
  • To elucidate the molecular mechanisms by which GPCRs coordinate cellular plasticity for skeletal health.
  • To provide a framework for advancing GPCR-targeted therapies for bone-related diseases.

Main Methods:

  • Systematic review of GPCR expression and functional roles in mesenchymal stem cells, osteoblasts, osteocytes, macrophages, osteoclasts, and chondrocytes.
  • Integration of canonical signaling pathways including cAMP/PKA, PLC-β/IP3, and NF-κB.
  • Analysis of GPCR involvement in skeletal homeostasis and disease pathogenesis.

Main Results:

  • Cataloged specific numbers of GPCRs and their functions in different bone cell lineages (e.g., 12 in MSCs, 21 in osteoblasts/osteocytes, 23 in macrophages/osteoclasts, 31 in chondrocytes).
  • Demonstrated how GPCRs dynamically regulate cellular plasticity through integrated signaling axes.
  • Identified GPCRs as critical regulators of matrix mineralization, mechanotransduction, inflammatory bone resorption, and endochondral ossification.

Conclusions:

  • GPCRs are central regulators of skeletal homeostasis, with distinct expression patterns and functions across bone cell types.
  • Understanding GPCR signaling provides a foundation for developing novel therapeutic strategies for bone disorders.
  • Precision strategies like biased agonism and allosteric modulation offer promising avenues for clinical translation in osteoporosis, arthritis, and regenerative medicine.