Engineering Cyclic Peptides For Oral Bioavailability

工程化环肽以提高口服生物利用度

• 批准号: DP150104609
• 负责人: Prof David Fairlie
• 金额: $ 34.7万
• 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: 2015
• 资助国家: 澳大利亚
• 起止时间: 2015-01-01 至 2017-12-31
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/DP150104609
• 关键词: Engineering; Cyclic; Peptides; Oral; Bioavailability

The 21st century has become the age of injectable peptide therapeutics. To fully realise their benefits , peptide drugs need to become smaller, cheaper and orally deliverable. Proteins often exhibit potent and selective biological actions through small peptide surfaces. These surfaces have been mimicked in cyclic peptides that are similarly potent and selective. However, cyclic peptides do not have the right properties to be oral drugs. This project aims to re-engineer their surfaces to survive potential degradation in the gut, to permeate membranes and to withstand clearance from blood. The projected outcome of this project is new information and technology for downsizing proteins to small orally bioavailable peptides for therapeutic applications.

21世纪世纪已成为注射肽疗法的时代。为了充分实现其益处，肽类药物需要变得更小，更便宜和口服。蛋白质通常通过小肽表面表现出强有力的和选择性的生物学作用。这些表面已经在环肽中被模拟，具有类似的有效性和选择性。然而，环肽不具有作为口服药物的合适性质。该项目旨在重新设计它们的表面，使其在肠道中的潜在降解中存活，渗透膜并承受血液的清除。该项目的预期成果是新的信息和技术，用于将蛋白质缩小为用于治疗应用的小的口服生物可利用肽。