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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 | Study on incisional implantation of tumor cells by carbon dioxide pneumoperitoneum in gastric cancer of a murine model显示文摘 | Wang H Zheng MH Zhang HB Zhu J He JR Lu AG Ji YB Zhang MJ Jiang Y Yu BM Li HW | 1999 | World Journal of Gastroenterology1999，5，6： | 2 |
| 4 | Design,synthesis,and anti-inflammatory evaluation of a series of novel amino acid-binding 1,5-diarylpyrazole derivatives显示文摘Aim: To design and synthesize a series of novel amino acid-binding 1,5-diarylpyrazole derivatives, which are intended to act as prodrugs with better aqueous solubility than celecoxib, and which will exert potent anti-inflammatory activi-ties after being converted to their parent compounds in vivo. Methods: To introduce an amino acid, celecoxib analogs containing amino or methylamino group were synthesized first through multi-step chemical reactions. All the synthesized compounds were screened in an intact cell-based assay in vitro and in carrageenan-induced mouse paw edema in vivo. Some active compounds were selected for further evaluation in a carrageenan-induced rat paw edema model. The preliminary pharmacokinetics experiments were conducted using high performance liquid chromatography/mass spectrometry (HPLC/MS). Results: Celecoxib, 6 of the 1,5-diarylpyrazole class of celecoxib analogs, and their amino acid derivatives (hydrochloride salts) were synthesized. In vitro screening, the hydrochloride salts showed decreased inhibitory effects on cyclooxygenase (COX)- 1 and COX-2 compared with their parent compounds, but some exhibited potent anti-inflammatory activity in vivo. Compound 4a was selected for further evaluation, and its anti-inflammatory effect was equivalent to that of celecoxib after oral administration in the carrageenan-induced rat paw edema model. At three doses (25 mg/kg, 50 mg/kg, and 100 mg/kg) the percentage inhibition on edema was 20.7%, 52.6%, and 62.6% (for compound 4a) and 27.8%, 38.4%, and 40.1% (for celecoxib), respectively. Preliminary pharmacokinetic evaluations support the hypothesis that compound 4a was actually converted to its parent compound, compound 4. Conclusion: The compound bound with amino acid acts like prodrug, which can exert anti-inflammatory effect similar to celecoxib after being converted to its parent compound. This finding will be of great benefit in carrying out structural modifications of prodrug-like selective COX-2 inhibitors. | Li MH Yin LL Cai MJ Zhang WY Huang Y Wang X Zhu XZ Shen JK | 2005 | Acta Pharmacologica Sinica2005，26，7： | 2 |
| 5 | Angiographic follow-up of cerebral aneurysms treated with Guglielmi detachable eoils:an analysis of 162 eases with 173 aneurysms显示文摘 | Li MH Gao BL Fang C | 2006 | AJNR2006，27，： | 1 |
| 6 | Excretory-secretory antigen is better than crude antigen for the serodiagnosis of clonorchiasis by ELISA显示文摘 | Choi MH Park IC Li SY | 2003 | Korean J Parasitol2003，41，1： | 1 |
| 7 | Prevention and management of intraprocedural rupture of intracranial aneurysm with detachable coils during embolization显示文摘 | Li MH Gao BL Fang C | 2006 | Neuroradiology2006，48，： | 1 |
| 8 | Stimulatory effect of octopamine on beta 3 adrenoreceports to lower the uptake of -deoxy-D-glucose into rat adipocytes in vitor显示文摘 | Yen ST Li MH Hsu CT | 1998 | Journal of Autonomic Pharmacology1998，18，1： | 1 |
| 9 | A population-based study on the risks of cervical lesion and human papillomavirus infection among women in Beijing,People' s Republic of China显示文摘 | Li CD Wu MH Wang JD | | 0，，10： | 1 |
| 10 | Delayed coil migration from a small wide-necked aneurysm after stent-assisted embolization: case report and literature review显示文摘 | Gao BL Li MH Wang YL | 2006 | Neuroradiology2006，48，5： | 1 |
| 11 | The existence of bronchiectasis predicts worse prognosis in patients with COPD显示文摘 | Mao B Lu HW Li MH | 2015 | Sci Rep2015，5，10： | 1 |
| 12 | Antagonistic activity of Lactobacillus acidophilus LB against intracellular Salmonella enterica serovar typhimurium infecting human enlerocyte-like Caco-2;FC-7 cells显示文摘 | Coconnier MH Li e vin V Lorrot M | 2000 | Appl Environ Microbial2000，66，： | 1 |
| 13 | Fibrosis of collagen I and remodeling of connexin 43 in atrial myocardium of patients with atrial fibrillation显示文摘 | Luo MH Li YS Yang KID | 2007 | Cardiology2007，107，4： | 1 |
| 14 | Tyrosine nitrationof prostacyclin synthase is associated with enhancedretinal cell apoptosis in diabetes显示文摘 | Zou MH Li HL He CY | 2011 | Ame J Pathol2011，179，： | 1 |
| 15 | Laparoscopically assisted biomaterial graft for re- construction in congenital atresia of vagina and cervix显示文摘 | Li MH Zhang ZY | 2013 | Fertil Ster- il2013，100，6： | 1 |
| 16 | Treatment of distal internal carotid artery aneurysm with the willis covered stent: a prospective pilot study显示文摘 | Li MH Li YD Tan HQ | 2009 | Radiology2009，253，2： | 1 |
| 17 | Enhanced production of dihydroxyacetone from glycerol by overexpression of glycerol dehydrogenase in an alcohol dehydrogenase-deficient mutant of Gluconobacter oxydans显示文摘 | Li MH Wu J Liu X | 2010 | Bioresource Technology2010，101，： | 1 |
| 18 | Pseudolarix acid B inhibits angiogenesis by antagonizing the vascular endothelial growth factor- mediated anti-apoptotic effect显示文摘 | Tan WF Zhang X Li MH | 2004 | EurJ Phmacol2004，499，3： | 1 |
| 19 | Enzyme induction and acute endocrine effects in prepubertal female rats receiving environmental PCB/PCDF/PCDD mixtures显示文摘 | Li MH Hansen LG | 1996 | Environ Health Perspect1996，104，7： | 1 |
| 20 | Costimulatory pathways in trans- plantation : challenges and new developments 显示文摘 | Li XC Rothstein DM Sayegh MH | 2009 | Immunol Rev2009，229，1： | 1 |
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