ENZYME REACTORS FOR THE SYNTHESIS OF PEPTIDE INHIBITORS

高血压是中国研究人员面临的主要健康挑战之一。 今天的制药领域。具有抑制作用的合成肽 肾素和血管紧张素转换酶[ACE]已被证明非常成功 在治疗高血压方面，并在治疗其他疾病方面显示出希望 各州。 虽然合成肽的需求很高，但用于治疗高血压和 其他障碍，可用的多肽合成技术有严重的 缺点。缺点包括成分的消旋化 偶联反应，高成本和潜在的环境危害 由偶联剂使用，且价格昂贵，耗时长 在每个耦合步骤之后需要净化步骤。 该项目旨在演示改进后的 多肽合成程序。这一过程基于一种新型的膜-- 基于酶的反应器，克服了传统酶反应器的缺点 合成技术。 此第一阶段计划的目标有三个：1)确定 膜基酶反应器的运行条件 模型多肽的连续合成，2)构建酶 3)测试系统的性能。在第一阶段取得成功 将导致专注于优化和扩展的第二阶段计划 拟议的程序和对更多申请的调查。

Hypertension is one of the major health challenges facing researchers in pharmaceutical field today. Synthetic peptides that are inhibitors of renin and angiotensin-converting enzyme [ACE] have proved very successful in treating hypertension and have shown promise in treating other disease states. While the demand is high for synthetic peptides to treat hypertension and other disorders, available peptide-synthesis techniques have serious drawbacks. The drawbacks include racemization of components during coupling reactions, the high cost and potential environmental hazards posed by the coupling reagents used, and the expensive and time-consuming purification steps required after each coupling step. This project is directed at demonstrating the feasibility of an improved peptide-synthesis procedure. The process is based on a novel membrane- based enzyme reactor that overcome the disadvantages of conventional synthesis techniques. The objectives of this Phase I program are threefold: 1) to determine the operating conditions required for a membrane-based enzyme reactor for the continuous synthesis of a model peptide, 2) to construct the enzyme reactor, and 3) to test the performance of the system. Success in Phase I would lead to a Phase II program focused on the optimization and scale-up of the proposed process and investigation of additional applications.