1.Research on clinical effect observation of TACE combined with percutaneous microwave coagulation therapy on treatment of patients with hepatocellular carcinoma
Bin LI ; Chao SUN ; Huiyong DUAN
China Medical Equipment 2015;(12):137-139
Objective:To explore the effect of transcatheter arterial chemoembolization (TACE) combined with percutaneous microwave coagulation therapy(PMCT) on treatment of patients with hepatic carcinoma.Methods: The clinical data of 60 cases of liver cancer patients in our hospital in TACE combined with PMCT were analyzed. Results:The operation was successfully performed, no serious complications and death. Efficacy: 4 CR cases, 38 PR cases, 16 SD cases, 2 PD cases, the total efficiency of treatment was 70.0%; After 1, 2, 3 year, survival cases (ratio) were respectively: 46(76.7%), 35(58.3%), 31(51.7%); The levels of Serum alpha fetoprotein (AFP) after operation was significantly reduced, after treatment, the patient's liver function improved significantly; The diameter of the lesions was significantly reduced.Conclusion: TACE combined with PMCT is an effective therapy for hepatic carcinoma.
2.Genotoxicity produced by radiofrequency electromagnetic radiations:research advances
Linlin DUAN ; Yanyan LIAO ; Hui YU ; Huiyong LIAN ; Peng CAI
Military Medical Sciences 2017;41(3):237-241
Humans are exposed to the ubiquitous radiofrequency (RF, 100 kHz-300 GHz) electromagnetic fields because of the mushroom development of wireless communications,raising concerns over the possible hazards of RF radiations.Epidemiological investigation has showed that chronic use of cellphones increases the risk of brain tumors.Since genetic damage is closely related to tumors, researchers have been trying to find out whether cellphones and other RF devices are genotoxic.However, the investigations have yielded both negative and positive results.This review summarized the recent in vitro and in vivo researches about genotoxicity of RF radiations and proposed a possible mechanism by which of RF radiations cause genetic damage.
3.Discovery of Novel Androgen Receptor Ligands by Structure-based Virtual Screening and Bioassays.
Wenfang ZHOU ; Mojie DUAN ; Weitao FU ; Jinping PANG ; Qin TANG ; Huiyong SUN ; Lei XU ; Shan CHANG ; Dan LI ; Tingjun HOU
Genomics, Proteomics & Bioinformatics 2018;16(6):416-427
Androgen receptor (AR) is a ligand-activated transcription factor that plays a pivotal role in the development and progression of many severe diseases such as prostate cancer, muscle atrophy, and osteoporosis. Binding of ligands to AR triggers the conformational changes in AR that may affect the recruitment of coactivators and downstream response of AR signaling pathway. Therefore, AR ligands have great potential to treat these diseases. In this study, we searched for novel AR ligands by performing a docking-based virtual screening (VS) on the basis of the crystal structure of the AR ligand binding domain (LBD) in complex with its agonist. A total of 58 structurally diverse compounds were selected and subjected to LBD affinity assay, with five of them (HBP1-3, HBP1-17, HBP1-38, HBP1-51, and HBP1-58) exhibiting strong binding to AR-LBD. The IC values of HBP1-51 and HBP1-58 are 3.96 µM and 4.92 µM, respectively, which are even lower than that of enzalutamide (Enz, IC = 13.87 µM), a marketed second-generation AR antagonist. Further bioactivity assays suggest that HBP1-51 is an AR agonist, whereas HBP1-58 is an AR antagonist. In addition, molecular dynamics (MD) simulations and principal components analysis (PCA) were carried out to reveal the binding principle of the newly-identified AR ligands toward AR. Our modeling results indicate that the conformational changes of helix 12 induced by the bindings of antagonist and agonist are visibly different. In summary, the current study provides a highly efficient way to discover novel AR ligands, which could serve as the starting point for development of new therapeutics for AR-related diseases.
Androgen Receptor Antagonists
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pharmacology
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Androgens
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metabolism
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pharmacology
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Biological Assay
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Cell Line, Tumor
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Drug Discovery
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methods
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Humans
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Ligands
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Male
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Molecular Docking Simulation
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Molecular Dynamics Simulation
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Phenylthiohydantoin
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analogs & derivatives
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pharmacology
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Principal Component Analysis
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Prostatic Neoplasms
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drug therapy
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Protein Binding
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physiology
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Protein Conformation
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drug effects
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Receptors, Androgen
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metabolism