BOMBESIN ANALOGUES

蟾蜍素类似物

• 批准号: 3491714
• 负责人: MARTHA KNIGHT
• 金额: $ 5万
• 依托单位: PEPTIDE TECHNOLOGIES CORPORATION
• 依托单位国家: 美国
• 财政年份: 1986
• 资助国家: 美国
• 起止时间: 1986-09-15 至 1987-03-14
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3491714
• 关键词: anorexic agent; chemotaxis; macrophage; neoplasm /cancer chemotherapy; neoplastic cell; peptide chemical synthesis; small cell lung cancer

Bombesin is a gastrointestinal hormone and neurally active peptide. It stimulates gastric acid secretion via gastrin release. The peptide is behaviorally active in suppressing food intake and lowers body temperature. The mammalian endogenous form of the peptide is ectopically produced in small cell carcinoma of the lung. These tumor cells also have bombesin receptors. Therefore, a possible means of chemotherapy could consist of drugs derived from this peptide. The synthesis of a series of analogues is proposed. One group is composed of agonist peptides designed for enhanced potency and efficacy. The peptides contain a minimum active sequence with changes to stabilize the conformation. Included in this group is a cyclic analogue. In the other group are possible specific antagonists. The peptides will be screened for activity and antagonism in chemotaxis to macrophages and tumor cells and in food intake behavior.

蛙皮素是一种胃肠激素和神经活性肽。 它 通过释放胃泌素刺激胃酸分泌。 所述肽是 行为活跃，抑制食物摄入，降低身体 温度 哺乳动物内源形式的肽是异位的 产生于肺小细胞癌。 这些肿瘤细胞还具有 蛙皮素受体 因此，一种可能的化疗方法可以 由这种肽衍生的药物组成。 合成了一系列 提出了类似物。 一组由激动剂肽组成， 以增强效力和功效。 所述肽含有最小活性 改变序列以稳定构象。 纳入本 基团是环状类似物。 在另一组中可能有特定的 对手。 将筛选肽的活性和拮抗作用， 对巨噬细胞和肿瘤细胞的趋化性以及食物摄取行为。

项目成果

Countercurrent chromatography for the purification of peptides.

用于纯化肽的逆流色谱法。

• 发表时间: 1992
• 期刊: Advances in chromatography
• 作者: Knight,M