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G Protein-Coupled Receptors in Osteoarthritis: A Novel Perspective on Pathogenesis and Treatment

期刊

出版社

FRONTIERS MEDIA SA
DOI: 10.3389/fcell.2021.758220

关键词

G protein-coupled receptor; osteoarthritis; cartilage matrix degradation; synovitis; pathogenesis; treatment

资金

  1. National Key R&D Program of China [2019YFA0111900]
  2. National Natural Science Foundation of China [81874030, 82072506, 82102581]
  3. National Postdoctoral Science Foundation of China [2021M693562]
  4. Hunan Young Talents of Science and Technology [2021RC3025]
  5. Provincial Outstanding Postdoctoral Innovative Talents Program [2021RC2020]
  6. Provincial Natural Science Foundation of Hunan [2020JJ3060]
  7. Provincial Clinical Medical Technology Innovation Project of Hunan [2020SK53709]
  8. Administration of Traditional Chinese Medicine of Hunan Province [2021075]
  9. Innovation-Driven Project of Central South University [2020CX045]
  10. Wu Jieping Medical Foundation [320.6750.2020-03-14]
  11. CMA Young and Middle-Aged Doctors Outstanding Development Program-Osteoporosis Specialized Scientific Research Fund Project [G-X-2019-1107-12]
  12. Young Investigator Grant of Xiangya Hospital, Central South University [2020Q14]
  13. Independent Exploration and Innovation Project for Postgraduate Students of Central South University [2021zzts1030, 2021zzts1037]

向作者/读者索取更多资源

G protein-coupled receptors (GPCRs) are important transmembrane receptor proteins that play crucial roles in the pathogenesis of osteoarthritis (OA). Current research indicates that targeting GPCRs could provide a novel therapeutic strategy for OA treatment.
G protein-coupled receptors (GPCRs) are transmembrane receptor proteins that trigger numerous intracellular signaling pathways in response to the extracellular stimuli. The GPCRs superfamily contains enormous structural and functional diversity and mediates extensive biological processes. Until now, critical roles have been established in many diseases, including osteoarthritis (OA). Existing studies have shown that GPCRs play an important role in some OA-related pathogenesis, such as cartilage matrix degradation, synovitis, subchondral bone remodeling, and osteophyte formation. However, current pharmacological treatments are mostly symptomatic and there is a paucity of disease-modifying OA drugs so far. Targeting GPCRs is capable of inhibiting cartilage matrix degradation and synovitis and up-regulating cartilage matrix synthesis, providing a new therapeutic strategy for OA. In this review, we have comprehensively summarized the structures, biofunctions, and the novel roles of GPCRs in the pathogenesis and treatment of OA, which is expected to lay the foundation for the development of novel therapeutics against OA. Even though targeting GPCRs may ameliorate OA progression, many GPCRs-related therapeutic strategies are still in the pre-clinical stage and require further investigation.

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