MOLECULAR CHARACTERIZATION OF THE GALANIN RECEPTOR

甘丙肽受体的分子表征

• 批准号: 3081128
• 负责人: JOSEPH S DILLON
• 金额: $ 8.69万
• 依托单位: TUFTS MEDICAL CENTER
• 依托单位国家: 美国
• 财政年份: 1993
• 资助国家: 美国
• 起止时间: 1993-08-01 至 1998-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3081128
• 关键词: genetic library; in situ hybridization; laboratory rat; molecular biology; molecular cloning; neuropeptide receptor; neuropeptides; receptor expression; second messengers; tissue /cell culture; transfection

Galanin is a peptide which is widely distributed in the central and peripheral nervous systems. In the pancreas, galanin is present in the sympathetic nerve terminals surrounding the islets of Langerhans and is a major inhibitor of insulin secretion during sympathetic nerve stimulation and certain systemic stresses. Despite these potent effects on insulin secretion, the effect of galanin receptor blockade in type II diabetes has not been investigated because of the lack of suitable galanin receptor blockers. As a prelude to determining the structural requirements of the ligand binding domain of the galanin receptor, the research outlined in this proposal is aimed at elucidating the molecular structure of the galanin receptor, the distribution of galanin receptor subtypes and the determination of the second messenger systems associated with the receptor sub types. The new information gained from achievement of these aims may then be used to determine the molecular requirements for ligand binding and to design galanin receptor antagonists to allow testing of the hypothesis that galanin may play a role in the unfavorable insulin secretion to insulin requirement balance in type II diabetes.

甘丙肽是一种广泛分布于中枢神经系统的肽， 周围神经系统在胰腺中，甘丙肽存在于 交感神经末梢周围的胰岛，是一个 交感神经刺激期间胰岛素分泌的主要抑制剂 和一定的系统压力尽管这些对胰岛素的有效影响 在II型糖尿病中，甘丙肽受体阻断剂的作用 由于缺乏合适的甘丙肽受体， 阻滞剂。作为确定结构要求的前奏， 甘丙肽受体的配体结合域， 该建议旨在阐明 甘丙肽受体、甘丙肽受体亚型的分布和甘丙肽受体的功能 确定与受体相关的第二信使系统 子类型。从实现这些目标中获得的新信息可能 然后用于确定配体结合的分子要求 并设计甘丙肽受体拮抗剂以允许测试 甘丙肽可能在不利的胰岛素分泌中起作用的假设 2型糖尿病的胰岛素分泌与胰岛素需求平衡。