Discovery and Modification of in vivo active Nrf2 Activators

来源 :2015年全国药物化学学术会议暨第五届中英药物化学学术会议 | 被引量 : 0次 | 上传用户:pengweimin
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
  Induction of phase Ⅱ antioxidant enzymes by activation of Nrf2/ARE pathway has been recognized as a promising strategy for the regulation of oxidative stress-related diseases.1 Herein we report our effort on the discovery and optimization of Nrf2 activators with 1,2,4-oxadiazole core.
其他文献
吗啡等阿片类镇痛药虽然已被广泛应用于临床,但其耐受、成瘾、便秘和呼吸抑制等副作用限制了其应用范围。近年来发现阿片类的双功能分子可介导低耐受的镇痛活性[1],因此在高效、低副作用的镇痛药物研发中备受关注。
会议
Although cisplatin is a promising anti-cancer agent,multifactorial resistance,serious side effects,and general toxicity have limited the use of cisplatin in cancer chemotherapy [1].Therefore,less toxi
会议
The elevation of oxidative stress preferentially in cancer cells by inhibiting thioredoxin reductase(TrxR)and/or enhancing reactive oxygen species(ROS)has emerged as an effective strategy for selectiv
The increasing multi-drug resistance has become a major threat to the public health [1].Over-expression of multidrug efflux pumps is one of the major mechanisms of drug resistance in bacteria [2].AcrB
通过化合物生物活性的计算预测,来寻找新的活性化合物是药物信息学一个重要的研究内容。我们选取抗艾滋病的HIV-1 整合酶[1-3]、抗丙肝病毒的 HCV 聚合酶[4,5]和蛋白酶[6]、抗流感病毒的神经氨酸酶等生物靶标和抑制剂作为研究对象,采取自组织神经网络和支持向量机等机器学习算法进行化合物生物活性和结构关系的研究,建立配体化合物生物活性的分类模型和定量预测模型。
会议
Currently,chiral non-natural tailor-made amino acids are key structural units in the development of new generation of peptide-based pharmaceuticals of high impact on healthcare industry.Synthesis of c
紫杉醇是靶向肿瘤微管的细胞毒类抗肿瘤药物,临床上广泛应用于各种肿瘤的治疗。紫杉醇在阻断肿瘤细胞有丝分裂的同时,对正常组织细胞也有一定的毒副作用,引起嗜中性白血球减少、呕吐、腹泻等不良反应。
Molecular recognition between biological macromolecules and organic small molecules plays an important role in various life processes.Both structural information and binding data of biomolecular compl