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 识别，以及胃，呼吸和行为过程。 提供 阿片肽的研究用途和最终的药物用途，新的 必须开发用于合成阿片肽的方法 避免了现有技术的问题。 该计划旨在开发一种新的肽段- 偶联工艺克服了化学和 常规的酶促片段偶联方法。 该方法是基于 使用用于偶联肽段的酶方法 一起 当这个过程与一套新的 保护基团，通常与化学和 避免了常规的酶促片段偶联方法（例如， 活性羧基组分外消旋化，侧链的必要性 保护和使用难以处理的极性溶剂）。 在第二阶段，我们建议将该技术扩展到各种 阿片肽的长度增加，并开发信息 在第三阶段将该工艺商业化是必要的。 具体来说，我们将 试图证明这一过程普遍适用于不同的 这种方法在经济上是可行的。

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.