BOMBESIN ANTAGONISTS

铃蟾肽拮抗剂

• 批准号: 3492918
• 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: 1992
• 资助国家: 美国
• 起止时间: 1992-04-01 至 1992-09-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3492918
• 关键词: amides; antineoplastics; bombesin; calcium flux; carbonyl group; clone cells; cyclic compound; drug design /synthesis /production; gastrins; inhibitor /antagonist; neoplastic cell; neuropeptide receptor; neuropeptides; nucleic acid sequence; peptide chemical synthesis; protective chemical group; proteolysis; reduction; small cell lung cancer

DESCRIPTION: (Adapted from the Applicant's Abstract): Recent bombesin and gastrin releasing peptide receptor antagonists have been demonstrated to be quite potent in inhibiting the effects of bombesin in pancreatic acinar cells, brainmembranes, Swiss 3T3 fibroblasts, and human small cell lung carcinoma (SCLC). However, these antagonists do not display comparable high potency in inhibiting the proliferation of human small cell lung carcinoma. Certain antagonist analogues do inhibit proliferation of clonal growth of SCLC and have been found to inhibit SCLC tumor growth in vivo. Studies will be conducted to design and synthesize more stable compounds from the inhibitor structures by cyclization and decreasing their susceptibility to proteolytic degradation. Novel groups will be added to the analogues to increase interaction with the SCLC receptor. The effect on clonal growth of human SCLC cells will be measured as an indicator of in vivo anti-tumor potential.

描述：(改编自申请者摘要)：最近的轰炸 和胃泌素释放肽受体拮抗剂已经被证明 对蛙皮素在胰腺中的作用有很强的抑制作用 腺泡细胞、脑膜、瑞士3T3成纤维细胞和人类小细胞 肺癌(SCLC)。然而，这些对手并没有表现出 具有相当高的抑制人小鼠胸腺细胞增殖的效力 细胞性肺癌。某些拮抗剂类似物确实能抑制 小细胞肺癌克隆性生长的增殖和抑制 肿瘤在体内生长。将进行研究以设计和合成 通过环化和环化从抑制剂结构中得到更稳定的化合物 降低它们对蛋白质降解的敏感性。新奇群体 将添加到类似物中，以增加与SCLC的互动 受体。对人小细胞肺癌细胞克隆生长的影响 作为体内抗肿瘤潜力的指标进行测量。

项目成果

Inhibitory cyclic analogues and chlorambucil derivatives of bombesin-like peptides.

铃蟾肽样肽的抑制性环状类似物和苯丁酸氮芥衍生物。

• DOI: 10.1016/0196-9781(95)00074-t
• 发表时间: 1995
• 期刊: Peptides
• 影响因子: 3
• 作者: Knight,M;Takahashi,K;Chandrasekhar,B;Geblaoui,AZ;Jensen,RT;Strader,D;Moody,TW
• 通讯作者: Moody,TW