Peptide derivatives useful as antagonists of bombesin and gastrin-releasing peptide
申请人:MERRELL DOW PHARMACEUTICALS INC.
公开号:EP0434979A1
公开(公告)日:1991-07-03
A method for controlling the growth of tumor tissues, especially small cell lung and prostatic carcinomas, and gastric acid secretion, causative and symptomatic of, peptic (esophageal, gastric, and duodenal) ulcers. Treatment comprises administering to a patient in need thereof, an effective amount of a bombesin/GRP type inhibitor.
Antagonists of bombesin/GRP which are derivatives of naturally occurring bombesin/GRP possessing a thiomethylene or methylene sulfoxide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which bombesin/GRP is implicated is also described.
一种控制肿瘤组织(特别是小细胞肺癌和前列腺癌)生长和胃酸分泌的方法,胃酸分泌是消化性(食管、胃和十二指肠)溃疡的致病因素和症状。治疗方法包括向有需要的患者施用有效量的蚕豆蛋白/GRP 型抑制剂。
本文描述了蚕豆蛋白/GRP的拮抗剂,它们是天然蚕豆蛋白/GRP的衍生物,具有连接羧基末端两个氨基酸的硫亚甲基或亚甲基亚砜键。使用传统的竞争性结合和生化测定法以及传统的生理测试证实了这种拮抗作用,还介绍了这些衍生物在涉及γ-胰高血糖素的各种情况下的应用。