ENGINEERING INHIBITORS FOR CANCER ASSOCIATED PROTEASE

癌症相关蛋白酶的工程抑制剂

• 批准号: 6119262
• 负责人: TOSHIHIKO TAKEUCHI
• 金额: $ 0.54万
• 依托单位: UNIVERSITY OF CALIFORNIA, SAN FRANCISCO
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-07-01 至 2000-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6119262
• 关键词: biological products; biomedical resource

We are using macromolecular inhibition of serine protease activity to probe the role of proteases in various biological systems. Our initial protease target is urokinase-type plasminogen activator (uPA), which is thought to play a central role in the invasion and metastasis of cancerous cells. The macromolecular protease inhibitor ecotin is being engineered for specificity and activity against uPA, and these ecotin mutants are further used to identify and isolate other tumor-associated proteases. These mutant ecotins are also useful in dissecting the role of serine proteases in complex biological systems. The Computer Graphics Laboratory facilites have been invaluable in the cloning and characterization of a novel serine protease. The GCG package as well as the blast functions were used frequently. This protease appears to be overexpressed in prostate cancer and will be further characterized.

我们正在使用丝氨酸蛋白酶活性的大分子抑制 探讨蛋白酶在各种生物系统中的作用。 我们的 初始蛋白酶靶点是尿激酶型纤溶酶原激活剂（uPA）， 它被认为在侵袭和转移中发挥核心作用 癌细胞。 大分子蛋白酶抑制剂大肠杆菌素是 被设计用于针对 uPA 的特异性和活性，并且这些 生态素突变体进一步用于鉴定和分离其他 肿瘤相关蛋白酶。 这些突变型大肠杆菌素也可用于 剖析丝氨酸蛋白酶在复杂生物系统中的作用。 计算机图形实验室的设施在 新型丝氨酸蛋白酶的克隆和表征。 GCG 包以及blast函数被频繁使用。 这 蛋白酶似乎在前列腺癌中过度表达，并且将 进一步表征。