Rational structure-based drug design of protein tyrosine kinase inhibitors

基于合理结构的蛋白酪氨酸激酶抑制剂药物设计

• 批准号: LP0454285
• 负责人: Prof Jamie Rossjohn
• 金额: $ 83.56万
• 依托单位: Monash University
• 依托单位国家: 澳大利亚
• 项目类别: Linkage Projects
• 财政年份: 2004
• 资助国家: 澳大利亚
• 起止时间: 2004-06-29 至 2008-12-31
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/LP0454285
• 关键词: Rational; structure; based; drug; design

Protein tyrosine kinases (PTK) are a large, pivotal family of signalling molecules implicated in diseases such as cancer and immune-related disorders, that cause significant morbidity and mortality within the population. This research proposal aims to develop PTK-specific small molecule inhibitors to combat such diseases. Cytopia's drug discovery capability, coupled with the X-ray crystallographic expertise within Monash University, will permit a rational, structure-based drug discovery platform to be established. The ultimate goal of this innovative and mutlidisciplinary approach, namely a portfolio of phase I therapeutics, will be of substantial benefit in the medical health area.

蛋白酪氨酸激酶(PTK)是一个大的、关键的信号分子家族，与癌症和免疫相关疾病等疾病有关，在人群中导致显著的发病率和死亡率。这项研究计划旨在开发PTK特异性小分子抑制剂来对抗此类疾病。Cytopia的药物发现能力，加上莫纳什大学的X射线结晶学专业知识，将使一个合理的、基于结构的药物发现平台得以建立。这一创新和多学科方法的最终目标，即第一阶段疗法的组合，将在医疗卫生领域带来实质性的好处。