Investigation of the mechanism of phosphoryl group transfer by phosphoryl transfer enzymes using NMR

酶催化磷酰基转移是体现酶高效性的经典范例之一。研究磷酸转移酶的催化机理，最关键的问题是了解磷酰基转移酶如何稳定磷酰基转移反应的过渡态。一种可行的方法是利用三氟化镁（MgF3-）或四氟化铝（AlF4-）模拟过渡态的磷酰基团（PO3-），同磷酸转移酶形成稳定的，可供观测的，酶的金属氟化物过渡态类似物（TSA）。运用19FNMR对金属氟化物过渡态类似物进行观测，可从原子层面了解磷酸转移酶催化位点过渡态的信息。 本博士论文的主要工作是研究p38MAPK信号传导通路中的磷酰基转移机理。利用19FNMR，直接观测到了MEK6DD催化p38MAPK磷酸化位点Tyr182磷酸化反应的金属氟化物过渡态类似物复...Catalysis of phosphoryl transfer reactions involves some of the largest enzymatic rate accelerations in biology. A substantial step forward in understanding the fundamental mechanism of phosphoryl group transfer by enzymes came through the use of MgF3- and AlF4- as transition state analogs (TSAs) of the planar PO3- group. The metal fluoride TSA complexes are particularly informative because 19F NM...学位：理学博士院系专业：化学化工学院化学系_化学生物学学号：1912005140309

丝组二肽——现代蛋白酶分子进化过程中的原始雏形

系统阐述了我们实验室近十五年来对丝组二肽的生物活性的研究.丝组二肽是目前报道的具有多种切割活性的最小活性肽,它不仅能够切割DNA,而且可以切割蛋白质及羧酸酯.丝组二肽是迷你的磷酸酯酶和蛋白水解酶,是现代蛋白酶分子进化过程中的原始雏形

Synthesis and spectral characterization of {phenyl-[(pyridine-4carbonyl)amino]methyl}phosphonic acid dialkyl ester

alpha-Aminophosphonic acids and their derivates, as phosphorous analogs of amino acid, have attracted much attention because they show wide biological activities. In this paper, the title compounds, {phenyl-[(pyridine-4-carbonyl)amino]methyl}phosphonic acid dialkyl esters, were synthesized via Mannich reaction and peptide coupling reaction. Their structures were confirmed by elemental analysis, IR, H-1 NMR, C-13 NMR and MS spectra, and the antibacterial and antitumor activities of these compounds were given in this paper