Department of Orthopaedic Surgery, Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou, Henan, People's Republic of China.
Henan Provincial Key Laboratory of Children's Genetics and Metabolic Diseases, Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou, Henan, People's Republic of China.
Drug Des Devel Ther. 2021 Feb 26;15:895-903. doi: 10.2147/DDDT.S289614. eCollection 2021.
Non-gustatory, extraoral bitter taste receptors (T2Rs) are G-protein coupled receptors that are expressed throughout the body and have various functional responses when stimulated by bitter agonists. Presently, T2Rs have been found to be expressed in osteoclasts and osteocytes where osteoclasts were capable of detecting bacterial quorum-sensing molecules through the T2R38 isoform. In the innate immune system, stimulating T2Rs induces anti-inflammatory and anti-pathogenic effects through the phospholipase C/inositol triphosphate pathway, which leads to intracellular calcium release from the endoplasmic reticulum. The immune cells with functional responses to T2R activation also play a role in bone inflammation and orthopaedic disorders. Furthermore, increasing intracellular calcium levels in bone cells through T2R activation can potentially influence bone formation and resorption. With recent studies finding T2R expression in bone cells, we examine the potential of targeting this receptor to treat bone inflammation and to promote bone anabolism.
非味觉性、口腔外苦味受体（T2R）是 G 蛋白偶联受体，在全身表达，当受到苦味激动剂刺激时具有各种功能反应。目前，已经发现 T2R 在破骨细胞和成骨细胞中表达，破骨细胞能够通过 T2R38 同工型检测细菌群体感应分子。在先天免疫系统中，通过磷脂酶 C/三磷酸肌醇途径刺激 T2R 诱导抗炎和抗病原效应，导致内质网中细胞内钙释放。对 T2R 激活有功能反应的免疫细胞也在骨炎症和骨科疾病中发挥作用。此外，通过 T2R 激活增加骨细胞内的细胞内钙水平可能会影响骨形成和吸收。随着最近研究发现 T2R 在骨细胞中的表达，我们研究了靶向该受体治疗骨炎症和促进骨合成代谢的潜力。
