【摘 要】
：
组蛋白去乙酰化酶(HDACs)通过催化各种底物蛋白包括组蛋白、转录因子、α-微管蛋白和核输入蛋白等的ε-赖氨酸残基乙酰化侧链的去乙酰化来影响细胞功能,抑制HDAC活性可以治疗
【机 构】
：
大连理工大学生命科学与技术学院,日本九州工业大学大学院生命体工学研究科,
论文部分内容阅读
组蛋白去乙酰化酶(HDACs)通过催化各种底物蛋白包括组蛋白、转录因子、α-微管蛋白和核输入蛋白等的ε-赖氨酸残基乙酰化侧链的去乙酰化来影响细胞功能,抑制HDAC活性可以治疗表观遗传异常引起的癌症和其他慢性疾病.以HDAC抑制剂(HDACi)Chlamydocin为骨架设计合成一类新型抑制剂,将HDACi的结合区设计为二硫键结构、在环肽中苯丙氨酸的苯环不同位点引入甲基,合成4种不同序列的环肽类HDACi.考察HDACi体外抗肿瘤细胞(MCF-7,Hela和7721)活性,结果表明HDACi对三种肿瘤细胞系均显示良好的生长抑制作用,细胞形态都发生明显变化,其中对Hela细胞的毒性最高,IC50达到0.1μmol/L.
Histone deacetylases (HDACs) catalyze the deacetylation of acetylated side chains of epsilon-lysine residues of various substrate proteins, including histones, transcription factors, alpha-tubulin and nuclear import proteins Affect cell function and inhibit HDAC activity can treat epigenetic abnormalities caused by cancer and other chronic diseases.Using HDACi Chlamydocin as a skeleton design and synthesis of a new class of inhibitors, the HDACi binding region designed as a disulfide bond structure , Four different sequences of cyclopeptide HDACi were synthesized by introducing methyl groups at different positions of the phenylalanine phenyl ring in the cyclic peptide.The activity of HDACi in vitro against the tumor cells (MCF-7, Hela and 7721) was investigated and the results showed that HDACi All the three tumor cell lines showed good growth inhibition, cell morphology had significant changes, of which the highest toxicity Hela cells, IC50 reached 0.1μmol / L.
其他文献
Two silkworm strains viz, B20 A (high cocoon shell ratio) and C.Nichi (low cocoon shell ratio) were sib mated for 10 generations to determine the homozygosis. B
The evolutionary density and the scatter of densities of the short fatigue cracks on the surface of 1Cr18Ni9Ti pipeweld metal were observed by local and overall
Background Echinococcosis, coenurosis and cysticercosis are debilitating diseases which prevail in China.Immunological diagnosis of metacestodosis is important
Background Although the computer tomography (Cr) or magnetic resonance imaging (MRI) findings of alveolar echinococcosis (AE) have been well documented, the con
Background For patients with end-stage hepatic alveolar echinococcosis (AE), in vivo resection of the involved parts of the liver is usually very difficult, the
Low phosphorus (P) availability is one of the most important factors limiting plant growth in red soils across southeastern China. Many non-symbiotic microorgan
Background Cystic echinococcosis (CE) is a zoonosis caused by the cestodes of the Echinococcus species. Its life cycle involves dogs and other canids as defini
通过模拟实际封闭水域的室内水质净化装置,研究了水体生物与多孔混凝土的生态适应性以及形成的综合生态效应对水质的净化效果.多孔混凝土综合生态效应的水质净化效果可通过总
Since the first 2 cases observed in southern Germany and the correct identification of a parasite at the origin of the disease by the famous scientist Rudolf Vi
针对一类新型“浮力-压块”驱动的自治飞艇,研究了该类飞艇的动力学建模和动力学特性。在Kirchhoff方程和Newton-Euler理论基础上,通过对飞艇运动及受力分析,建立了包括独立