Molecular Recognition of Potassium Channels

钾通道的分子识别

• 批准号: 7058256
• 负责人: DIRK HARTWIG TRAUNER
• 金额: $ 25.56万
• 依托单位: UNIVERSITY OF CALIFORNIA BERKELEY
• 依托单位国家: 美国
• 财政年份: 2004
• 资助国家: 美国
• 起止时间: 2004-05-01 至 2007-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7058256
• 关键词: Xenopus oocyte; cell line; chemical binding; chemical synthesis; drug discovery /isolation; fluorescence resonance energy transfer; ligands; membrane proteins; molecular probes; peptide library; pharmacokinetics; porphyrins; potassium channel; protein binding; structural biology; voltage gated channel

DESCRIPTION (provided by applicant): The goal of this research proposal is to combine organic synthesis with recent advances in structural biology to make significant contributions both to the fields of molecular recognition and neurobiology. We propose to develop fourfold symmetrical, synthetic ligands that recognize tetrameric ion channels, in particular potassium channels. The primary goal of the proposed research is to provide a large set of molecular probes that discriminate among different types of potassium channels or modulate their functional properties. These compounds could be useful tools in neurobiological studies. It is hoped that these compounds will eventually surpass antibodies and peptide toxins in the selective recognition of potassium channels. Ultimately, the proposed research might lead to novel therapeutic agents against various ailments such as autoimmune disorders, diabetes as well as mental or cardiac diseases. Specifically, the synthesis and biological evaluation of designed ligands for voltage-gated potassium channels such as KvAP, Shaker, and human Kv1.x channels is proposed. Pharmacologically relevant Kv1.x channels such as Kv1.3 or Kv1.5 will receive special attention. The ability of the synthetic ligands to bind to different functional states of a given channel will be evaluated.

描述（由申请人提供）：本研究计划的目标是将有机合成与结构生物学的最新进展结合起来，在分子识别和神经生物学领域做出重大贡献。

项目成果

Introduction: Chemical approaches to neurobiology.

简介：神经生物学的化学方法。

• DOI: 10.1021/cr800273n
• 发表时间: 2008
• 期刊: Chemical reviews
• 影响因子: 62.1
• 作者: Trauner,Dirk