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75毫克至10克数量的生物活性多肽、新型氨基酸和多肽模拟物，这些都是作为该计划项目资助的广泛生化、药理、生物物理和生物学研究所需的。特别重要的是开发各种研究项目和方案所需的适当的不对称合成方法学、其他合成方法、纯化方法和分析方法。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，以制备计划项目资助中的研究人员所需的任何配体；2)制备0.20克到2克的联苯双酚、新的强啡肽A片段、新的阿片受体激动剂的二价配体和缓激肽和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)通过不对称合成数量(1克到10克)的新氨基酸和多肽模拟物来制备计划项目所需的配体；4)制备生物和/或生物物理研究所需的最多克数量的有效生物活性多肽、糖肽、多肽模拟物和多肽结合物；以及5)制备本计划项目资助中的研究人员进一步进行生物和生物物理研究所需的任何其他多肽、多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.