SYNTHESIS CORE

合成核心设施由亚利桑那大学专门为该计划项目资助而翻新，其主要目标是合成、纯化并对75毫克至10克的生物活性肽、新型氨基酸和肽模拟物进行必要的分析工作，这些生物活性肽、新型氨基酸和肽模拟物是该计划项目资助中广泛的生化、药理学、生物物理和生物学研究所需要的。特别重要的是发展适当的不对称合成方法、其他合成方法、净化方法和各种研究项目和协议所需的分析方法。具体目标是：1)开发和建立所有必要的合成方法、纯化方案和分析程序，这些方法、纯化方案和分析程序用于制备计划项目资助中研究人员所需的任何配体；2)制备0.20 g - 2g双脑啡肽、新型动力啡肽A片段、新型二价配体，作为阿片受体的激动剂和缓激肽及其他中枢神经系统受体的拮抗剂，用于广泛的体外和体内生物活性研究和生物物理研究；3)通过不对称合成（1 g - 10 g）制备本项目配体所需的新型氨基酸和肽模拟物；4)制备生物和/或生物物理研究所需的可达克量的有效生物活性肽、糖肽、拟肽和肽偶联物；5)制备本计划项目资助研究人员为进一步的生物和生物物理研究所需的任何其他肽、肽模拟物或其他配体。

The major goals of the Synthetic Core Facility, which was renovated by the University of Arizona specifically for this Program Project Grant are to synthesize, purify and perform necessary analytical work on 75 mg to 10 g quantities of bioactive peptides, novel amino acids and peptide mimetics that are needed for the extensive biochemical, pharmacological, biophysical and biological studies which are part of this Program Project Grant. Of specific importance will be the development of proper asymmetric synthetic methodology, other synthetic methods, purification methods and analytical methods that are needed for the various research projects and protocols. The Specific Aims are: 1) To develop and establish all necessary synthetic methodologies, purification protocols, and analytical procedures that are needed for preparing any ligands that are needed by investigators in the Program Project Grant; 2) To prepare 0.20 g to 2 g of biphalin, novel dynorphin A fragments, novel bivalent ligands that are agonists at opioid receptors and antagonists at bradykinin and other CNS receptors for extensive in vitro and in vivo biological activity studies and for biophysical studies; 3) To prepare by asymmetric synthesis quantities (1 g to 10 g) of novel amino acids and peptide mimetics that are needed for the preparation of ligands for the Program Project; 4) To prepare up to gram quantities of potent bioactive peptides, glycopeptides, peptidomimetics, and peptide conjugates that will be needed for biological and/or biophysical studies; and 5) To prepare any other peptides, peptide mimetics or other ligands that are needed by investigators in this Program Project Grant for further biological and biophysical studies.