【摘 要】
：
Brutions tyrosine kinase(BTK)is a key component of the B-cell receptor signaling pathway which plays a critical role in B-cell development.Ample evidence indicates that the dysregulation of BTK is ass
【机 构】
：
State Key Laboratory of Natural Medicines,Jiangsu Key Laboratory of Drug Discovery for Metabolic Dis
【出 处】
：
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
论文部分内容阅读
Brutions tyrosine kinase(BTK)is a key component of the B-cell receptor signaling pathway which plays a critical role in B-cell development.Ample evidence indicates that the dysregulation of BTK is associated with the pathogenesis and development of B-cell malignancies.1,2 Nowadays,some of BTK inhibitors have advanced into clinical trials,and one of them,ibrutinib,is approved by the US FDA for the treatment of mantle cell lymphoma(MCL)and chronic lymphocytic leukemia(CLL).
其他文献
2005年，拥有自主知识产权的丁苯酞软胶囊被国家药监局批准上市，成为国际上首个作用于急性缺血性脑卒中多个病理环节的创新药物。丁苯酞能重建脑缺血区微循环，显著缩小脑梗塞面积，并能保护线粒体功能，改善脑代谢。
Directly disrupting the Keap1-Nrf2 protein-protein interaction(PPI)has been proven an effective way to activate Nrf2.On the basis of the potent Keap1-Nrf2 PPI inhibitor reported by our group previousl
Rosiglitazone is clinically used to treat insulin resistance.However,its long-term administration will increase the incidence of cardiovascular side effects.[1] Given the beneficial effects of nitric
α,β-不饱和酮化合物CDDO-Me具有显著的抗炎和抗肿瘤活性[1],但在进行2型糖尿病慢性肾病Ⅲ期临床研究时,发现它有严重的心血管不良反应[2]。我们推测,CDDO-MeA环上的α-氰基烯酮反应性极强,除与靶标作用外,也可能与非靶标蛋白的巯基发生了迈克尔加成,产生了副作用。
The epidermal growth factor receptor(EGFR)is one important member of protein tyrosine kinases.Aberrant activation of EGFR has been linked to tumor proliferation,invasion and metastasis.1,2 Several rev
The synthesis of 4-isochromanones via Parham-type cyclization with Weinreb amide as the internal electrophilic group,t-BuLi as the lithium reagent was described.The reaction was very efficient and cou
酸性神经鞘磷脂酶(ASM)水解鞘磷脂生成神经酰胺和磷酰胆碱，调节体内神经鞘磷脂的动态平衡及神经酰胺参与的信号转导，在动脉粥样硬化，抑郁症，肺泡组织损伤，肝损伤等多种疾病的发生发展过程中起着重要的作用[1]。
Heat shock protein 90(Hsp90)is highly expressed in many tumor cells and is associated with the maintenance of malignant phenotypes.Targeting Hsp90 has shown some therapeutic success in solid and hemat