SYNTHESIS CORE

综合核心

基本信息

批准号：
8025973
负责人：
Victor J Hruby
金额：
$ 16.56万
依托单位：
UNIVERSITY OF ARIZONA
依托单位国家：
美国
项目类别：
财政年份：
2010
资助国家：
美国
起止时间：
2010-04-01 至 2014-03-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/8025973
关键词：
Address Adverse effects Agonist Amino Acids Analgesics Animals Arizona Biochemical Biological Biology Bradykinin Bradykinin Receptor Chemicals Chimera organism Complex Core Facility Custom Cyclization Development Disease Drug abuse Dynorphin A Enkephalin, D-Penicillamine (2,5)-Ensure Evaluation GTP-Binding Proteins Glycopeptides Goals In Vitro Ion Channel Laboratories Lead Life Ligands Mediator of activation protein Methodology Methods Mind Molecular Neurotransmitters Opioid Opioid Receptor Pain Pain management Peptides Pharmacology Phosphotransferases Physiological Physiology Preparation Price Problem Solving Procedures Program Research Project Grants Property Protocols documentation Public Health Research Research Personnel Research Project Grants Resources Role Second Messenger Systems Services Societies Source Spectrum Analysis Structure System Time Universities Work addiction allodynia analytical method arrestin3 biphalin cost design drug seeking behavior experience in vivo mimetics novel painful neuropathy peptide hormone peptidomimetics pre-clinical programs receptor second messenger stereochemistry success

Address Adverse effects Agonist Amino Acids Analgesics Animals Arizona Biochemical Biological Biology Bradykinin Bradykinin Receptor Chemicals Chimera organism Complex Core Facility Custom Cyclization Development Disease Drug abuse Dynorphin A Enkephalin, D-Penicillamine (2,5)-Ensure Evaluation GTP-Binding Proteins Glycopeptides Goals In Vitro Ion Channel Laboratories Lead Life Ligands Mediator of activation protein Methodology Methods Mind Molecular Neurotransmitters Opioid Opioid Receptor Pain Pain management Peptides Pharmacology Phosphotransferases Physiological Physiology Preparation Price Problem Solving Procedures Program Research Project Grants Property Protocols documentation Public Health Research Research Personnel Research Project Grants Resources Role Second Messenger Systems Services Societies Source Spectrum Analysis Structure System Time Universities Work addiction allodynia analytical method arrestin3 biphalin cost design drug seeking behavior experience in vivo mimetics novel painful neuropathy peptide hormone peptidomimetics pre-clinical programs receptor second messenger stereochemistry success

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项目摘要

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.

由亚利桑那大学（Arizona of Arizona）对该计划项目赠款进行了翻新的合成核心设施的主要目标是合成，净化和执行必要的分析工作，对75 mg至10 g量的生物活性肽，新型氨基酸和肽模拟物进行了广泛的生物学，生物学研究所需的生物学和肽模拟物需要，该计划需要该计划。具有特定重要性的是开发适当的不对称合成方法，其他合成方法，纯化方法和分析方法是各种研究项目和协议所需的分析方法。具体目的是：1）开发和建立所有必要的合成方法，纯化协议和分析程序，这些方法是准备计划项目赠款中研究人员所需的任何配体所需的； 2）准备0.20 g至2 g的双峰，新型的dynorphin a片段，新型的二价配体，它们是阿片类受体的激动剂，在Bradykinin和其他中枢神经系统受体上，用于广泛的体外和体内生物学活性研究，用于生物物理研究； 3）通过为程序项目制备配体所需的新型氨基酸和肽模拟物的不对称合成量（1 g至10 g）的制备； 4）准备大量有效的生物活性肽，糖肽，肽肽和肽结合物，这些肽需要用于生物学和/或生物物理研究； 5）准备任何其他肽，肽模拟物或该计划项目赠款中需要的其他配体，以进行进一步的生物学和生物物理研究。