NOVEL PROCESS FOR ENZYMATIC PEPTIDE SEGMENT COUPLING

阿片肽是一类重要的生物调节剂，与疼痛有关 认知，以及胃、呼吸和行为过程。供应，供应 用于研究和最终用于制药的阿片肽，新 必须开发合成阿片肽的方法 避免现有技术的问题。 该计划旨在开发一种新的多肽片段-- 克服了化学和化学的缺点的耦合过程 常规的酶链段偶联方法。该方法的基础是 用于偶联多肽片段的酶过程的使用 在一起。当这一过程与一组新颖的 保护基团，通常与化学和 避免了传统的酶片段偶联方法(例如， 活性羧基的外消旋，侧链的必要性 保护，以及使用难以处理的极性溶剂)。 在第二阶段，我们建议扩展这项技术，将其应用于各种 阿片肽的长度不断增加，并开发信息 有必要在第三阶段将这一过程商业化。具体来说，我们将 力求证明该过程一般适用于不同的 这一工艺在经济上是可行的。

Opioid peptides are an important class of bioregulators, involved in pain recognition, and gastric, respiratory, and behavioral processes. To supply opioid peptides for research use and eventually pharmaceutical use, new methodologies for the synthesis of opioid peptides must be developed that avoid the problems of current techniques. This program is aimed at the development of a novel peptide segment- coupling process that overcomes the disadvantages of chemical and conventional enzymatic segment-coupling methods. the approach is based on the use of an enzyme process that is used to couple peptide segments together. When this process is used in conjunction with a novel set of protecting groups, the drawbacks commonly associated with chemical and conventional enzymatic segment-coupling methods are avoided (e.g., racemization of activated carboxyl components, the necessity of side-chain protection, and the use of polar solvents that are difficult to handle). In Phase II, we propose to expand the technology to apply it to a variety of opioid peptides of increasing lengths and to develop the information necessary to commercialize the process in Phase III. Specifically, we will seek to demonstrate that the process is generally applicable to different peptides and that process is economically feasible.