Novel selective anti-platelet and clot-specific anticoagulant strategies targeting conformational states of GPIIb/IIIa

针对 GPIIb/IIIa 构象状态的新型选择性抗血小板和凝块特异性抗凝策略

• 批准号: nhmrc : 367645
• 负责人: Prof Karlheinz Peter
• 金额: $ 33.11万
• 依托单位: Baker IDI Heart and Diabetes Institute
• 依托单位国家: 澳大利亚
• 项目类别: NHMRC Project Grants
• 财政年份: 2006
• 资助国家: 澳大利亚
• 起止时间: 2006-01-01 至 2008-12-31
• 项目状态: 已结题
• 来源: https://researchdata.edu.au/novel-selective-anti-states-gpiibiiia/77557
• 关键词: Novel; selective; anti; platelet; clot

The inhibition of platelets and the inhibition of coagulation factors are among the most widely used drugs in medicine and provide major benefits for numerous patients. Prevention and treatment of thrombosis, emboli, stroke and heart attack are examples of the many diseases where anti-platelet and anticoagulant drugs are administered. However, the downsides of these drugs are bleeding complications, which can result in death or disability. The consequences of these drug-associated bleeding complications are also a major financal burden for our health care system. Thus, progress towards therapeutic strategies with less bleeding complications is highly sought-after. The proposed project aims to generate new antibody-based agents for platelet inhibition. One group of these agents do only block platelets when they are activated. Furthermore, these agents allow an enrichment of potent inhibitors of coagulation factors at the site of the clot. Thus, these inhibitors should predominatly act at the site where they are needed. At the same time the overall concentration of inhibitors of coagulation factors can be kept low and the functions of non-activated platelet can be left intact. Overall, the proposed project aims for the development of novel anti-platelet and anticoagulant strategies with high anti-thrombotic efficacy and low bleeding risks.

血小板的抑制和凝血因子的抑制是医学中最广泛使用的药物之一，并且为许多患者提供了主要益处。预防和治疗血栓形成、栓塞、中风和心脏病发作是施用抗血小板和抗凝药物的许多疾病的例子。然而，这些药物的缺点是出血并发症，可能导致死亡或残疾。这些药物相关出血并发症的后果也是我们卫生保健系统的主要财政负担。因此，出血并发症较少的治疗策略的进展是非常受欢迎的。拟议项目旨在产生新的基于抗体的血小板抑制剂。这些药物中的一组仅在血小板被激活时才能阻断血小板。此外，这些试剂允许在凝块部位富集凝血因子的强效抑制剂。因此，这些抑制剂应主要作用于需要它们的部位。同时，凝血因子抑制剂的总浓度可以保持较低，未活化血小板的功能可以保持完整。总体而言，拟议项目旨在开发具有高抗血栓疗效和低出血风险的新型抗血小板和抗凝策略。