Project 1

项目1

• 批准号: 8380472
• 负责人: RAYMOND C STEVENS
• 金额: $ 66.21万
• 依托单位: SCRIPPS RESEARCH INSTITUTE, THE
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/8380472
• 关键词: Behavior; Binding; Collaborations; Complex; Disease; Docking; Family; Family member; G Protein-Coupled Receptor Genes; Goals; Knowledge; Ligand Binding; Ligands; Pathway interactions; Process; Production; Property; Proteins; Quality Control; Running; Sampling; Screening procedure; Solutions; Structure; Structure-Activity Relationship; computerized data processing; design; drug discovery; experience; gene synthesis; predictive modeling; process optimization; receptor; success; therapeutic development

Project 1 is responsible for achieving the Center‟s Aim 1 goals; the immediate goal of Aim 1 studies is the structure solution of GPCRs and their co-crystals with ligands. The long range goal is to develop a better understanding of the structure-function relationship in GPCRs. Ultimately enough structures will be determined to provide a fine sampling of the various GPCR sequence families and, thus, enable reliable modeling and predictive docking studies of other close family members. Structures of receptors in complex with different ligands will be essential for developing a better understanding of their binding properties. Ultimately, this newly acquired knowledge can then be used to validate and to generate hypothesis regarding GPCRs mechanisms of action (e.g., in signal processing pathways). These new structures will have an enormous impact on furthering our understanding of a number of diseases and most probably will help accelerate success rates in drug discovery and therapeutics development studies.

项目1负责实现中心的目标1目标；目标1研究的直接目标是 GPCR的结构解及其与配体的共结晶。远距离目标是发展更好 了解GPCR中的结构功能关系。最终将确定足够的结构 为各种GPCR序列家族提供精细的采样，从而实现可靠的建模和 对其他亲密家庭成员的预测对接研究。与不同的受体结构不同 配体对于更好地理解其结合特性至关重要。最终，这是新的 然后可以使用获得的知识来验证和产生有关GPCR机制的假设 动作（例如，在信号处理途径中）。这些新结构将对 进一步了解我们对多种疾病的理解，很可能有助于加速成功率 药物发现和治疗学发展研究。