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Acta Pharmaceutica Sinica B ; (6): 468-491, 2024.
Artigo em Inglês | WPRIM | ID: wpr-1011252

RESUMO

G protein-coupled receptors (GPCRs) are a large family of membrane protein receptors, and Takeda G protein-coupled receptor 5 (TGR5) is a member of this family. As a membrane receptor, TGR5 is widely distributed in different parts of the human body and plays a vital role in regulating metabolism, including the processes of energy consumption, weight loss and blood glucose homeostasis. Recent studies have shown that TGR5 plays an important role in glucose and lipid metabolism disorders such as fatty liver, obesity and diabetes. With the global obesity situation becoming more and more serious, a comprehensive explanation of the mechanism of TGR5 and filling the gaps in knowledge concerning clinical ligand drugs are urgently needed. In this review, we mainly explain the anti-obesity mechanism of TGR5 to promote the further study of this target, and show the electron microscope structure of TGR5 and review recent studies on TGR5 ligands to illustrate the specific binding between TGR5 receptor binding sites and ligands, which can effectively provide new ideas for ligand research and promote drug research.

2.
The Journal of Practical Medicine ; (24): 459-461, 2017.
Artigo em Chinês | WPRIM | ID: wpr-513216

RESUMO

Objective To study the effect of tiotropium on urination disorder in benign prostatic hyperplasia (BPH) patients with chronic obstructive pulmonary disease (COPD).Methods In our prospective pilot study,96 BPH patients with COPD patients were enrolled as the treatment group and another 25 similar cases as the control group:In the former group tiotropium was administered and the control group was not.The two groups were compared in terms of the score by the international Prostate Symptom Score(IPSS),the quality of life by QOL,maximum flow rate (Q-max),average flow rate (Q-ave),time to Q-max (TTQ-Max),prostate volume (PVR) and bladder voiding efficiency (BVE) after six months treatment.Results As compared to the control,after six months treatment,such indexes in the treatment group as IPSS (15.1 ± 4.1,16.3 ± 3.4 and 14.7 ± 3.1,P =0.864),QOL(3.9 ± 0.8,4.0± 0.8 and 4.0 ± 0.9,P =0.992),Q-Max(ml/s) (8.5 ± 2.9,10.9 ± 2.2 and 9.0 ± 2.4,P =0.214),Q-ave(ml/s) (3.9 ±1.2,5.0 ± 1.4 and 3.8 ± 0.9,P =0.054),TTQ-Max(s) (11.1 ± 5.6,11.2 ± 4.0 and 10.4 ± 5.1,P =0.424),PVR(mL)(56.8 ± 33.3,62.3 ± 30.5 and 57.4 ± 29.5,P =0.981),BVE(%) (75.6 ± 13.8,72.7 ± 10.5 and 74.3 ± 12.1,P =0.992).showed no significant differences.Conclusion Tiotropium does not adversely affect lower urinary tract functions in BPH patients with COPD.

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