BOMBESIN ANTAGONISTS

描述：（改编自申请人的摘要）：最近的铃蟾肽 和胃泌素释放肽受体拮抗剂已经被证明 在抑制蛙皮素在胰腺中的作用方面是相当有效的， 腺泡细胞、脑膜、Swiss 3T3成纤维细胞和人小细胞 肺癌（SCLC）。 然而，这些拮抗剂不显示 在抑制人类小细胞增殖方面具有相当高的效力， 肺癌 某些拮抗剂类似物确实抑制 增殖的克隆生长的SCLC，并已发现抑制SCLC 体内肿瘤生长。 将进行研究， 更稳定的化合物从抑制剂结构通过环化和 降低它们对蛋白水解降解的敏感性。 新的基团 将添加到类似物中，以增加与SCLC的相互作用 受体的 对人SCLC细胞克隆生长的影响将是 作为体内抗肿瘤潜力的指示物测量。

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.