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沉默钙激活氯通道ANO1促进人前列腺癌PC-3细胞的凋亡
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作者 宋艳 关立照 王克威 《中国药理学通报》 CAS CSCD 北大核心 2015年第B11期9-9,共1页
目的探讨沉默钙激活氯通道(anoctamin1,ANO1)对人前列腺癌PC-3细胞凋亡的影响及其分子机制.方法采用siRNA沉默ANO1在PC-3细胞的表达;采用ELISA、流式细胞仪检测细胞凋亡;采用Apo-ONEHomogeneous Caspase-3/7Assay检测Caspase活性;采... 目的探讨沉默钙激活氯通道(anoctamin1,ANO1)对人前列腺癌PC-3细胞凋亡的影响及其分子机制.方法采用siRNA沉默ANO1在PC-3细胞的表达;采用ELISA、流式细胞仪检测细胞凋亡;采用Apo-ONEHomogeneous Caspase-3/7Assay检测Caspase活性;采用基因表达谱分析检测沉默ANO1表达后PC-3细胞内基因变化,以及Real-timePCR和Westernblot验证.将全长ANO1基因(来源于NCBI)与pIRES2-EGFP融合,构建ANO1-IRES2表达载体,获得稳定表达ANO1的RWPE-1细胞系.结果ANO1在人前列腺癌PC-3细胞中呈高表达,沉默ANO1可诱导PC-3细胞凋亡,并增加肿瘤坏死因子(tumornecrosisfactor,TNF-α)表达和Caspase-3/7活性.TNF-α抑制剂来那度胺(lenalidomide)20nmol·L^-1可逆转沉默ANO1诱导的细胞凋亡.同时,ANO1在人正常前列腺细胞RWPE-1中呈低表达,过表达ANO1可降低RWPE-1细胞凋亡,同时降低TNF-α表达和Caspase-3/7活性.总之,ANO1表达与TNF-α呈负相关.结论沉默ANO1表达可诱导PC-3细胞凋亡,其机制可能与激活TNF-α介导的信号转导通路相关. 展开更多
关键词 钙激活氯通道 ano1-tmem16a 前列腺癌 细胞凋亡 肿瘤坏死因子TNF-Α
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TMEM16A在肿瘤中的研究进展 被引量:3
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作者 谭佳杰 张洪 +2 位作者 范月莹 宋玲 冯豆 《华中科技大学学报(医学版)》 CAS CSCD 北大核心 2022年第6期879-883,共5页
跨膜蛋白16A(transmembrane protein 16A,TMEM16A)是一种钙激活的氯离子通道(calcium-activated chloride channel,CaCC),它在肿瘤中广泛过表达,对肿瘤的发生发展有着重要的影响。在各种肿瘤中,TMEM16A的过表达不仅可以促进癌细胞的增... 跨膜蛋白16A(transmembrane protein 16A,TMEM16A)是一种钙激活的氯离子通道(calcium-activated chloride channel,CaCC),它在肿瘤中广泛过表达,对肿瘤的发生发展有着重要的影响。在各种肿瘤中,TMEM16A的过表达不仅可以促进癌细胞的增殖、转移和侵袭,抑制肿瘤细胞的凋亡,影响肿瘤的生长,还与肿瘤的治疗耐药、复发和预后不良有关。因此,探索TMEM16A的体内表达情况与肿瘤各个方面的关系具有重要的意义,该综述旨在总结近十年来TMEM16A在肿瘤中的研究进展,为以后TMEM16A在肿瘤中的进一步研究提供新的思路。 展开更多
关键词 TMEM16a 钙激活氯离子通道 ano1 抑制剂 肿瘤
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The Ca^(2+)-activated chloride channel ANO1/TMEM16A:An emerging therapeutic target for epithelium-originated diseases? 被引量:13
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作者 Yani Liu Zongtao Liu KeWei Wang 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2021年第6期1412-1433,共22页
Anoctamin 1(ANO1) or TMEM16 A gene encodes a member of Ca^(2+) activated Cl^(-) channels(CaCCs) that are critical for physiological functions,such as epithelial secretion,smooth muscle contraction and sensory signal t... Anoctamin 1(ANO1) or TMEM16 A gene encodes a member of Ca^(2+) activated Cl^(-) channels(CaCCs) that are critical for physiological functions,such as epithelial secretion,smooth muscle contraction and sensory signal transduction.The attraction and interest in ANO1/TMEM16 A arise from a decade long investigations that abnormal expression or dysfunction of ANO1 is involved in many pathological phenotypes and diseases,including asthma,neuropathic pain,hypertension and cancer.However,the lack of specific modulators of ANO1 has impeded the efforts to validate ANO1 as a therapeutic target.This review focuses on the recent progress made in understanding of the pathophysiological functions of CaCC ANO1 and the current modulators used as pharmacological tools,hopefully illustrating a broad spectrum of ANO1 channelopathy and a path forward for this target validation. 展开更多
关键词 Ca^(2+)-activated Cl^(-)channels(CaCCs) ano1 TMEM16a CaCCinh-A01 T16ainh-A01 Drug target Cancer Cystic fibrosis
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Inhibiting calcium-activated chloride channel ANO1/TMEM16A suppresses migration of tumor epithelial cells 被引量:1
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作者 Linghan Jia Wen Liu KeWei Wang 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2015年第8期545-551,共7页
Uncontrolled cell migration is a common feature of tumor metastasis and formation. Understanding the molecular targets critically involved in cell migration process can lead to the development of potentially novel the... Uncontrolled cell migration is a common feature of tumor metastasis and formation. Understanding the molecular targets critically involved in cell migration process can lead to the development of potentially novel therapeutic strategies for controlling invasion of tumor cells. In this study, we showed that calcium-activated chloride channel ANO 1/TMEM16A played an important role in cell migration and inhibition of ANO1 channel function suppressed the migration of tumor epithelial cells. Silencing ANO 1 by small hairpin RNA (shRNA) resulted in suppression of cell migration and invasiveness in cancer cell lines. In addition, pharmacological inhibition of ANO1 by the channel specific inhibitor T16Ain-A01 significantly slowed down the migration and invasion of tumor epithelial cells in a dose-dependent manner. Taken together, our findings have demonstrated that calcium-activated chloride channel ANO1 contributes to cell migration, and specific ANO1/TMEM16A inhibitors can be the promising candidate to develop new therapies for cancer metastasis. 展开更多
关键词 Cell migration METASTASIS Cancer Epithelial cells ano1/TMEM16a SHRNA T16ain-A01
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Discovery of 4-arylthiophene-3-carboxylic acid as inhibitor of ANO1 and its effect as analgesic agent 被引量:1
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作者 Yuxi Wang Jian Gao +9 位作者 Song Zhao Yan Song Han Huang Guiwang Zhu Peili Jiao Xiangqing Xu Guisen Zhang Kewei Wang Liangren Zhang Zhenming Liu 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2021年第7期1947-1964,共18页
Anoctamin 1(ANO1)is a kind of calcium-activated chloride channel involved in nerve depolarization.ANO1 inhibitors display significant analgesic activity by the local peripheral and intrathecal administration.In this s... Anoctamin 1(ANO1)is a kind of calcium-activated chloride channel involved in nerve depolarization.ANO1 inhibitors display significant analgesic activity by the local peripheral and intrathecal administration.In this study,several thiophenecarboxylic acid and benzoic acid derivatives were identified as novel ANO1 inhibitors through the shape-based virtual screening,among which the 4-arylthiophene-3-carboxylic acid analogues with the best ANO1 inhibitory activity were designed,synthesized and compound 42(IC;=0.79μmol/L)was finally obtained.Compound 42 selectively inhibited ANO1 without affecting ANO2 and intracellular Ca;concentration.Subsequently,the analgesic effect was investigated by intragastric administration in pain models.Compound 42 significantly attenuated allodynia which was induced by formalin and chronic constriction injury.Through homology modeling and molecular dynamics,the binding site was predicted to be located near the calcium-binding region betweenα6 andα8.Our study validates ANO1 inhibitors having a significant analgesic effect by intragastric administration and also provides selective molecular tools for ANO1-related research. 展开更多
关键词 ano1(anoctamin 1 TMEM16a) INHIBITOR Synthesis Structure-activity relationship ANALGESIA
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