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1.
Acta Pharmaceutica Sinica B ; (6): 468-491, 2024.
Article in English | WPRIM | ID: wpr-1011252

ABSTRACT

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.
Chinese Journal of Primary Medicine and Pharmacy ; (12): 1355-1358,后插2, 2015.
Article in Chinese | WPRIM | ID: wpr-601570

ABSTRACT

Objective To investigate the value of 64-slice spiral CT angiography in diagnosis of the origin of abdominal large masses.Methods Twenty patients who were proven by operation and pathology to be abdominal massive tumor were collected in this study,tumor diameter average 17.8cm.All patients accepted plain and enhanced CT scanning,and their data were transferred to Philips IntelliSpace Portal.The tumor vessel were reconstructed with multiplanar reformation(MPR),maximum intensity projection(MIP),and volume rendering(VR).The origin of tumor were judged according to the feeding arteries by 2 attending physician,and the results were compared with pathology.Results Of these 20 cases,15 cases were malignant tumor,5 benign.Blood supply arteries were found in 19 patients,36 vessels.Lateral branch vessels in 6 cases and arteriovenous fistula in 4 cases.MSCTA findings were consistent with operation and pathology,with the accuracy of 90%.One case had no tumor vessel,one was misdiagnosed.Conclusion MSCT could be taken good use in diagnosis of large abdominal masses by tracking down the nourishing artery of masses.

3.
Chinese Journal of Primary Medicine and Pharmacy ; (12): 825-827,828, 2015.
Article in Chinese | WPRIM | ID: wpr-600461

ABSTRACT

Objective To investigate the diagnostic value of multi -modal MRI for prostate cancer .Methods The multi modalitymagnetic resonance data of 43 patients with prostatic diseases were retrospectively analyzed ,selected biopsy or operation pathology results as the control ,analyzed their unenhanced MRI ,DWI,MRS and DCE -MRI. Results (1)In 43 patients,29 cases were diagnosed by biopsy of prostate cancer .37 cancer lesions were found,and 28 cancer lesions showed obviously low signal intensity in T 2WI.(2)The mean ADC value of the cancer lesions and normal areas were (0.69 ±0.09) ×10 -3 mm2/s and (1.31 ±0.18) ×10-3 mm2/s,there was significant difference in ADC value between the two groups (t=21.06,P<0.01);(3) The mean Cho +Cre/Cit value of the cancer lesions and normal areas were (2.67 ±1.58) and (0.74 ±0.28),there was significant difference in ADC value between the two groups (t=7.34,P<0.01);(4)32 rapidly ascending and slowly descending type ROI's,4 flat type ROI's and 1 rising type ROI's were founded in cancer lesions .Conclusion Multi-modal MRI can further provide the blood perfusion of prostate cancer ,water molecule diffusion and microcirculation state ,metabolism and biochemical composi-tion change information .The combination of T2WI,DWI,MRS and DCE-MRI can improve the diagnostic efficiency for the detection of prostate cancer prominently .

4.
Chinese Journal of Rheumatology ; (12): 42-45, 2015.
Article in Chinese | WPRIM | ID: wpr-466181

ABSTRACT

Objective To study the role of RICTOR on rheumatoid arthritis-fibrobast-like synoviocytes (RA-FLS) activation.Methods FLS were isolated from the primary synovial tissues,which were obtained during joint replacement surgery or arthroscopy from three patients with RA.RA-FLS were stimulated with TNF-α at the dose of 10 ng/ml and 20 ng/ml for 48 h.The expression of RICTOR was detected by western blotting.Chemically synthesized RICTOR gene targeted for double-stranded siRNAs were transfected into RA-FLS by cationic liposome.After being transfected with RICTOR siRNA for 48 h,RA-FLS was treated with or without TNF-α for 48 h.The expression of RICTOR was evaluated by western blotting,and the cell viability was analyzed by methylthiazoltetrazolium (MTT) assay.The data were analyzed using analysis of variance (ANOVA) and LDL-t test.Results The expression of RICTOR protein was significantly higher in the TNF-α stimulated group (at the dose of 10 ng/ml and 20 ng/ml for 48 h) than that in the control group (bothP<0.05),while the mean change of RICTOR/GAPDH ratios of band optical density x+s was 0.35±0.06 for the control group,0.60±0.09 for the TNF 10 ng/ml group and 1.10±0.12 for the TNF 20 ng/ml group.Moreover,the expression of RICTOR protein was obviously decreased in RICTOR siRNA transfection groupthan that in control after being trans-fected for 96 h (both P<0.05),and ratios of control group,RICTOR (-)/TNF-α(-) group and RICTOR(-)/TNF-α(+) group was 0.498 4±0.140 1,0.012 8±0.002 0,0.042 5±0.027 3respectively.After the silence of RICTOR,the cell viability decreased in RA-FLS,no matter with or without TNF-α for 48 h later (both P<0.05).Conclusion These results indicat that RICTOR might play an important role in the TNF-α associated activation of RA-FLS.

5.
Microbiology ; (12)1992.
Article in Chinese | WPRIM | ID: wpr-683718

ABSTRACT

The results of experiment showed that B. subtilis BR151 and MI112 containing plasmid pUB110 in LB liquid medium is more stabl than in LB slant. Stable recipient strain BSG for plasmid pUB110 was obtained by mutagenesis with NTG. The strain BSG is more efficient recipient of transformation for shuttle vectors pPTE4 and pBE2 from E.coli than its parent. The chimeric plasmids which contain small inserts are stable in strain BSG after 30 generations.

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