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| 1 | Androgen receptor: structure, role in prostate cancer and drug discovery显示文摘Androgens and androgen receptors (AR) play a pivotal role in expression of the male phenotype. Several diseases, such as androgen insensitivity syndrome (AIS) and prostate cancer, are associated with alterations in AR functions. Indeed, androgen blockade by drugs that prevent the production of androgens and/or block the action of the AR inhibits prostate cancer growth. However, resistance to these drugs often occurs after 2-3 years as the patients develop castration-resistant prostate cancer (CRPC). In CRPC, a functional AR remains a key regulator. Early studies focused on the functional domains of the AR and its crucial role in the pathology. The elucidation of the structures of the AR DNA binding domain (DBD) and ligand binding domain (LBD) provides a new framework for understanding the functions of this receptor and leads to the development of rational drug design for the treatment of prostate cancer. An overview of androgen receptor structure and activity, its actions in prostate cancer, and how structural information and high-throughput screening have been or can be used for drug discovery are provided herein. | MH Eileen TAN Jun LI H Eric XU Karsten MELCHER Eu-leong YONG | 2015 | Acta Pharmacologica Sinica2015,36,1: | 39 |
| 2 | Qingyi decoction protects against myocardial injuries induced by severe acute pancreatitis显示文摘BACKGROUND We studied the protective effects of Qingyi decoction(QYD)(a Traditional Chinese Medicine)against severe acute pancreatitis(SAP)-induced myocardial infarction(MI).AIM To study the function and mechanism of QYD in the treatment of myocardial injuries induced by SAP.METHODS Ultrasonic cardiography,hematoxylin and eosin staining,immunohistochemistry,qRT-PCR,western blot,enzyme-linked immunosorbent assays,and apoptosis staining techniques were used to determine the effects of QYD following SAP-induced MI in Sprague-Dawley rats.RESULTS Our SAP model showed severe myocardial histological abnormalities and marked differences in the symptoms,mortality rate,and ultrasonic cardiography outputs among the different groups compared to the control.The expression of serum cytokines[interleukin(IL)-1?,IL-6,IL-8,IL-12,amyloidβ,and tumor necrosis factor-α]were significantly higher in the SAP versus QYD treated group(P<0.05 for all).STIM1 and Orai1 expression in myocardial tissue extracts were significantly decreased post QYD gavage(P<0.001).There was no significant histological difference between the 2-aminoethyl diphenylborinate inhibitor and QYD groups.The SAP group had a significantly higher apoptosis index score compared to the QYD group(P<0.001).CONCLUSION QYD conferred cardio-protection against SAP-induced MI by regulating myocardial-associated protein expression(STIM1 and Orai1). | Lei Li Yong-Qi Li Zhong-Wei Sun Cai-Ming Xu Jun Wu Ge-Liang Liu Ahmed MH Bakheet Hai-Long Chen | 2020 | World Journal of Gastroenterology2020,26,12: | 17 |
| 3 | Prokaryotical expression of structural and non-structural proteins of hepatitis G virus显示文摘AIM To study the epitope distribution of hepatitis G virus (HGV) and to seek for the potential recombinant antigens for the development of HGV diagnositic reagents.METHODS Fourteen clones encompassing HGV gene fragments from core to NS3 and NS5 were constructed using prokaryotic expression vector pRSET and (or)pGEX. and expressed in E. coli. Western blotting and ELISA were used to detect the immunoreactivity of these recombinant proteins.``RESULTS One clone with HGV fragment from core to El(Gl). one from E2 (G31), three from NS3 (G6, G61, G7),one from NS5B (G821) and one chimeric fragment from NS3and NS5B (G61 821) could be expressed well and showed obvious immunoreactivity by Western blotting.One clone with I-KGV framment from NS5B (G82) was also well expressed, but could not show immunoreactivity by Western blotting. No obvious expression was found in the other six clones. All the expressed recombinant proteins were in inclusion body form, except the protein G61 which could be expressed in soluble form. Further purified recombinant proteins Gl, G,31, G61, G821 and G61 821were detected in indirected ELISA as coating antigen respectively. Only recombinant Gl could still show immunoreactivity, and the other four recombinant proteins failed to react to the HGV antibody positive sera.Western blotting results indicated that the immunoactivity of these four recombinant proteins were lost during purification.``CONCLUSION Core to El, E2. NS3 and NS5 fragment of HGV contain antigenic epitopes, which could be produced in prokaryotically expressed recombinant proteins. A high. yield recombinant protein (Gl) located in HGV core to E1 could remain its epitope after purification, which showed the potential that G1 could be used as a coating antigen to develop an ELISA kit for HGV specific antibody diagnosis. | Ning-Shao Xia~1 Hai-Jie Yang~1 Jun Zhang~1 Chang-Qing Lin~1 Ying-Bin Wang~1 Juan Wang~1 Mei-Yun Zhan~2 MH Ng~3 1 Key Laboratory of the Ministry of Education for Cell Biology and Tumor Cell Engineering,Xiamen University,Xiamen 361005,Fujian Province,China2 Institute of Virology,Chinese Academy of Preventive Medicine Beijing 100052,China3 Department of Microbiology,Hoog Kong University,Hongkong,China | 2001 | World Journal of Gastroenterology2001,7,5: | 4 |
| 4 | Biomechanical effects of patellar positioning on intraoperative knee joint gap measurement in total knee ar- throplasty显示文摘 | Gejo R Mcgarry MH Jun BJ | 2010 | Clin Biomech(Bristol Avon)2010,25,4: | 1 |
| 5 | Professional Values in Korean Undergraduate Nursing Students 显示文摘 | Bang KS Kang JH Jun MH | 2011 | Nuts Educ Today2011,31,1: | 1 |
| 6 | Anticoccidial effect of green tea-based diets against Eimeria maxima 显示文摘 | Jang S I Jun MH Lillehoj HS | 2007 | Vet Parasitol2007,144,12: | 1 |
| 7 | Fucosterol is a selective liver X receptor modulator that regulates the expression of key genes in cholesterol homeostasis in macrophages,hepatocytes,and intestinal cells显示文摘 | Hoang MH Jia Y Jun HJ Lee JH Lee BY Lee SJ | | 0,,46: | 1 |
| 8 | Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells显示文摘 | Hoang MH Jia Y Jun H J Lee JH Lee DH Hwang BY Kim WJ Lee HJ Lee SJ | | 0,,12: | 1 |
| 9 | Cyanidin,a natural flavonoid,is an agonistic ligand for liver X receptor α and β and reduces cellular lipid accumulation in macrophages and hepatocytes显示文摘 | Jia Y Hoang MH Jun H J Lee JH Lee SJ | | 0,,14: | 1 |
| 10 | Induction of ABCA1 and ABCG1 expression by the liver X receptor modulator cineole in macrophages显示文摘 | Jun H J Hoang MH Yeo SK Jia Y Lee SJ | | 0,,02: | 1 |
| 11 | Autophagy negatively regulates early axon growth in cortical neurons显示文摘 | Ban BK Jun MH Ryu HH | 2013 | Mol Cell Biol2013,33,19: | 1 |
| 12 | Toxoplasma gondii inhibits apoptosis in infected cells by caspase inactivation and NF- kappaB activation显示文摘 | Kim JY Ahn MH Jun HS | 2006 | Yonsei Med J2006,47,6: | 1 |
| 13 | Taurine is a liver X receptor-α ligand and activates transcription of key genes in the reverse cholesterol transport without inducing hepatic lipogenesis显示文摘 | Hoang MH Jia Y Jun HJ Lee JH Hwang KY Choi DW Um S J Lee BY You SG Lee SJ | | 0,,06: | 1 |
| 14 | Catalposide is a natural agonistic ligand of peroxisome proliferator-activated receptor-α 显示文摘 | Lee JH Jun HJ Hoang MH | 2012 | Biochem Biophys Res Commun2012,422,4: | 1 |
| 15 | Hepatic lipid accumu- lation alters global histone h3 lysine 9 and 4 trimethylation in the peroxisome proliferator- activated receptor alpha net- work 显示文摘 | Jun HJ Kim J I-Ioauq MH | 2012 | PLoS ONE2012,7,44: | 1 |
| 16 | Comparative in vitro activities of carbapenem antimicrobial agents against 264 penicillin-resistant Streptococcus pneumoniae isolates from Korea 显示文摘 | Choi SH Park SJ Jun JB Lee SR Jeon MH Kwon HH | 2007 | Diagn Microbiol Infect Dis2007,58,1: | 1 |
| 17 | Toxoplasma gondii apoptosis in infected cells by caspase inactivation and NF-kβactivation 显示文摘 | Kim JY Ahn MH Jun HS | 2006 | Yonsei Med J2006,47,6: | 1 |
| 18 | Mechanical thromboprophylaxis is sufficient to prevent the lower extremity deep vein thrombosis after kidney transplantation显示文摘 | Jun KW Park KM Kim MH | 2014 | Ann Surg Treat Res2014,87,1: | 1 |
| 19 | Professional values in Korean un- dergraduate nursing students 显示文摘 | Bang KS Kang JH Jun MH | 2011 | Nurse Educ Today2011,31,1: | 1 |
| 20 | Rapamycin inhibits ANGⅡ induced proliferation of vascular endothelial cells显示文摘 | Shang MH Fang Y Jun H | 2005 | Chin J Nephrol Dialysis Transp2005,14,2: | 1 |