Benzimidazole moiety is a structural isostere of naturally occurring nucleotides and it has been extensively utilized as a drug scaffold in the medicinal chemistry.
目的:G9a(常染色质组蛋白赖氨酸N-甲基转移酶2,euchromatic histone-lysineN-methyltransferase 2,EHMT2)的C-端含有经典的SET(Su(var),Enhancer of zeste,Trithorax)结构域,且毗邻两个富含半胱氨酸的区域,结构类似已知的组蛋白甲基转移酶Suv39h1,与Suv39h1 相比G9a 甲基催化活性高10~20 倍
Histone lysine specific demethylase 1(LSD1)is the first identified histone demethylase,which can demethylate mono-and di-methylated histon3 lysine 4(H3K41/2)and histone 3 lysine 9(H3K9me1/2)when it is
目前,胃癌在我国乃至全球范围内仍然是最常见的恶性肿瘤之一,其每年的死亡人数在各类癌症中排第二位[1]。手术、化疗和放疗是治疗胃癌的三大主要手段。
Lysine specific demethylase 1(LSD1)selectively removes methyl groups from monoand dimethylated histone 3 lysine 4(H3K4),lead to gene silencing[1].
海参硫酸软骨素(sea cucumber chondroitin sulfate)最早由Vieira 和 Mour(a)o[1]小组于1988 年从Ludwigothurea grisea 海参体壁中分离得到。
Various glycoglycerolipids isolated from natural products display notable anti-tumor,anti-viral and anti-inflammatory bioactivities.
1,4-Naphthoquinones(1,4-NQs)are a class of aromatic motifs that are widely present among natural products and synthetic analogues.Numerous 1,4-NQs derivatives with substituent at C-2 and-3 positions h
众所周知,含氟官能团的引入在药物化学中越来越受到重视也极具挑战[1]。化合物在引入含氟基团后,因为氟原子的存在会使化合物的药效和代谢等性质发生明显的变化[2]。相对于较多引入二氟/三氟甲基的方法[3],芳基的直接二氟/三氟乙基化因为原料碘代二氟/三氟乙烷体系中易发生消除反应而鲜有报道[4]。
Adenosine 5-monophosphate activated protein kinase(AMPK)is a master sensor of cellular energy,which regulates the whole-body energy homeostasis.The activation of AMPK can lead to an increase of glucos