Investigating the structure, function and inhibition of the adrenaline-synthesizing enzyme PNMT

研究肾上腺素合成酶 PNMT 的结构、功能和抑制作用

• 批准号: DP0345019
• 负责人: Prof Jennifer Martin
• 金额: $ 18.85万
• 依托单位: The University of Queensland
• 依托单位国家: 澳大利亚
• 项目类别: Discovery Projects
• 财政年份: 2003
• 资助国家: 澳大利亚
• 起止时间: 2003-01-01 至 2006-12-31
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/DP0345019
• 关键词: Investigating; structure; function; inhibition; adrenaline

We determined the structure of the enzyme PNMT and we plan to use this in the design of PNMT inhibitors to enable us to probe the role of adrenaline and PNMT in the central nervous system. As part of this work, we will further characterise the structure of PNMT by crystallography and mutagenesis. The significance is that designed PNMT inhibitors could eventually be used as leads in the development of compounds with novel pharmacological and therapeutic activity. Furthermore, our analysis of PNMT will determine rules that can be applied to the design of new methyltransferase enzymes with novel functions.

我们确定了PNMT酶的结构，并计划将其用于PNMT抑制剂的设计，以使我们能够探索肾上腺素和PNMT在中枢神经系统中的作用。作为这项工作的一部分，我们将进一步通过结晶学和诱变来表征PNMT的结构。其意义在于，设计的PNMT抑制剂最终可能被用作开发具有新的药理和治疗活性的化合物的先导。此外，我们对PNMT的分析将确定可以应用于设计具有新功能的新的甲基转移酶的规则。