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Videos de Conceptos Relacionados

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...
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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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Video Experimental Relacionado

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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La función de los GPCR en diferentes células óseas

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
Resumen
Este resumen es generado por máquina.

Los receptores acoplados a proteínas G (GPCR) son objetivos clave para los trastornos óseos. Esta revisión detalla los GPCR en las células óseas, ofreciendo información sobre nuevas terapias para enfermedades esqueléticas como la osteoporosis y la artritis.

Palabras clave:
GPCR y sus derivadosEl MSCEl condrocitoel osteoblastoOsteoclasto

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Área de la Ciencia:

  • Biología esquelética y farmacología
  • Medicina celular y molecular

Sus antecedentes:

  • Los receptores acoplados a proteínas G (GPCR) juegan un papel crucial en la regulación de la función de las células óseas y la homeostasis esquelética.
  • La desregulación de la señalización GPCR está implicada en varios trastornos óseos, destacando su potencial terapéutico.

Objetivo del estudio:

  • Revisar y catalogar sistemáticamente la expresión y la función de GPCR en diversos tipos de células óseas.
  • Aclarar los mecanismos moleculares por los cuales los GPCR coordinan la plasticidad celular para la salud esquelética.
  • Proporcionar un marco para el avance de las terapias dirigidas al GPCR para las enfermedades relacionadas con los huesos.

Principales métodos:

  • Revisión sistemática de la expresión de GPCR y de sus funciones en las células madre mesenquimales, los osteoblastos, los osteocitos, los macrófagos, los osteoclastos y los condrocitos.
  • Integración de las vías de señalización canónicas que incluyen cAMP/PKA, PLC-β/IP3 y NF-κB.
  • Análisis de la participación del GPCR en la homeostasis esquelética y la patogénesis de la enfermedad.

Principales resultados:

  • Números específicos catalogados de GPCR y sus funciones en diferentes linajes de células óseas (por ejemplo, 12 en MSC, 21 en osteoblastos/osteoclastos, 23 en macrófagos/osteoclastos, 31 en condrocitos).
  • Se demostró cómo los GPCR regulan dinámicamente la plasticidad celular a través de ejes de señalización integrados.
  • GPCRs identificados como reguladores críticos de la mineralización de la matriz, la mecanotransducción, la reabsorción ósea inflamatoria y la osificación endocondral.

Conclusiones:

  • Los GPCR son reguladores centrales de la homeostasis esquelética, con patrones de expresión y funciones distintos en todos los tipos de células óseas.
  • La comprensión de la señalización GPCR proporciona una base para el desarrollo de nuevas estrategias terapéuticas para los trastornos óseos.
  • Las estrategias de precisión como el agonismo sesgado y la modulación alostérica ofrecen vías prometedoras para la traducción clínica en la osteoporosis, la artritis y la medicina regenerativa.