以类泛素酶NAE为靶点的抗肿瘤药物设计与合成任务书
2020-04-29 19:06:37
1. 毕业设计(论文)的内容和要求
随着越来越多的泛素修饰蛋白被报道,各种类泛素蛋白也不断被发现,如sumo(small ubiquitin-related modifier)、nedd8、atg8(autophagy gene 8)和atg12等。
目前,研究较多的为sumo和nedd8。
nedd8是由81个氨基酸残基组成的蛋白质,与泛素有60%的一致性和80%同源性。
2. 参考文献
[1]Teresa A. Soucy, Peter G. Smith, Michael A. Milhollen etc. (2009) An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature, Vol 458:732-737. [2]Brownell J E, Sintchak M D, Gavin J M, et al. Substrate-Assisted Inhibition of Ubiquitin-like Protein-Activating Enzymes: The NEDD8 E1 Inhibitor MLN4924 Forms a NEDD8-AMP Mimetic In Situ[J]. Molecular Cell, 2010, 37(1):102#8211;111. [3]Tanaka T, Nakatani T, Kamitani T. Inhibition of NEDD8-conjugation pathway by novel molecules: Potential approaches to anticancer therapy[J]. Molecular Oncology, 2012, 6(3):267-275. [6]Yan Z H, Burkhardt A, Loke H K, et al. Quantifiable analysis of cellular pathway inhibition of a Nedd8-activating enzyme inhibitor, MLN4924, using AlphaScreen[J]. Analytical Biochemistry, 2013, 439(2):109-115. [4]Hjerpe R, Thomas Y, Kurz T. NEDD8 overexpression results in neddylation of ubiquitin substrates by the ubiquitin pathway.[J]. Journal of Molecular Biology, 2012, 421(1):27#8211;29.
3. 毕业设计(论文)进程安排
2019.2.25-2019.3.11 文献调研,撰写开题报告和试验方案 2019.3.12-2019.5.15 实验探索,完成化合物合成,获取实验数据 2019.5.16-2019.6.110 撰写毕业设计论文,完成毕业论文答辩