ENZYMOLOGY

酶学

• 批准号: 6102658
• 负责人: RAYMOND BUDDE
• 金额: $ 14.64万
• 依托单位: UNIVERSITY OF TX MD ANDERSON CAN CTR
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-09-30 至 1999-09-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6102658
• 关键词: antineoplastics; cooperative study; drug design /synthesis /production; enzyme activity; enzyme inhibitors; molecular cloning; protein tyrosine kinase

This Laboratory Program represents the biochemistry section of a multidisciplinary effort to develop specific inhibitors against Src. This Program will be responsible for producing recombinant Src and other PTKs to (1) screen inhibitors, (2) determine the affinity of "hits" identified in the screen, (3) determine the specificity of the "hits" identified in the screen, and (4) perform structural studies of the Src active site. This laboratory program serves as a screen between the two synthetic chemistry laboratories and the two biological testing laboratories which functions to narrow down the thousands of compounds synthesized to those which are worth studying for biological efficacy. In addiction, it aids the synthetic chemistry sections in choosing which analogs to consider for synthesis and testing. The biochemistry lab has developed an infrastructure to produce recombinant PTKs and a high-through put screening of combinatorial libraries.

本实验室计划代表生物化学部分 多学科努力开发针对Src的特定抑制剂。这 项目将负责生产重组Src和其他PTK，以 (1)筛选抑制物，(2)确定在 屏幕，(3)确定在屏幕上识别的“命中”的特定性 筛选，以及(4)进行Src活性部位的结构研究。这 实验室计划是两个合成化学之间的屏障 实验室和两个生物检测实验室，它们的职能是 将数千种合成的化合物缩小到有价值的化合物 研究生物药效。在成瘾方面，它帮助合成 选择要考虑哪些类似物进行合成和处理的化学部分 测试。生化实验室已经开发了一个基础设施来生产 重组PTKs及其组合的高通量筛选 图书馆。