Opioid Peptide Analogs as Probes of Opioid Receptors

作为阿片受体探针的阿片肽类似物

• 批准号: 6726384
• 负责人: Jane V Aldrich
• 金额: $ 12.98万
• 依托单位: UNIVERSITY OF KANSAS LAWRENCE
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-09-01 至 2009-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6726384
• 关键词: affinity labeling; combinatorial chemistry; computer simulation; conformation; drug abuse; dynorphins; endogenous opioid; ligands; mass spectrometry; molecular probes; nuclear magnetic resonance spectroscopy; opioid receptor; peptide analog; peptide chemical synthesis; peptide library; protein sequence; protein structure function; receptor binding; site directed mutagenesis; stereochemistry

DESCRIPTION (provided by applicant): This application is a competitive renewal of an Independent Scientist Award (K02) to further Dr. Jane Aldrich's research in the area of drug abuse. Dr. Aldrich's long-term goals are to design and use new opioid peptide and peptidomimetic ligands as pharmacological tools to obtain a better understanding of opioid peptide-receptor interactions. The proposed research uses a combination of chemical, pharmacological and computational techniques, with the rationale that the information obtained from these complimentary methodologies will limit the number of possibilities for interactions of the peptides with receptor residues, greatly facilitating the development of models for the peptides bound to opioid receptors. Continuation of the Independent Scientist Award will allow Dr. Aldrich to expand her expertise in several areas related to her research on opioid peptides. These areas include synthesis (including stereoselective synthesis) of novel amino acid analogs for incorporation into opioid peptide analogs, gaining familiarity with molecular biological techniques to study opioid receptors, and obtaining additional experience with protein characterization by mass spectrometry. Experience in these areas will be synergistic with Dr. Aldrich's expertise in peptide chemistry and significantly enhance her contributions to research in the area of drug abuse.

描述（由申请人提供）： 这项申请是独立科学家奖（K 02）的竞争性更新，以促进Jane Aldrich博士在药物滥用领域的研究。奥尔德里奇博士的长期目标是设计和使用新的阿片肽和拟肽配体作为药理学工具，以更好地了解阿片肽-受体相互作用。拟议的研究使用了化学，药理学和计算技术的组合，其基本原理是从这些互补方法中获得的信息将限制肽与受体残基相互作用的可能性，大大促进了与阿片受体结合的肽模型的开发。 独立科学家奖的继续将使奥尔德里奇博士能够扩大她在阿片肽研究相关领域的专业知识。这些领域包括合成（包括立体选择性合成）新的氨基酸类似物纳入阿片肽类似物，熟悉分子生物学技术研究阿片受体，并获得额外的经验与蛋白质表征质谱。在这些领域的经验将与奥尔德里奇博士在肽化学方面的专业知识协同作用，并显着提高她在药物滥用领域的研究贡献。