Small cell lung cancer bombesin receptors are antagonized by reduced peptide bond analogues.
Small cell lung cancer bombesin receptors are antagonized by reduced peptide bond analogues.
复制标题
小细胞肺癌铃蟾肽受体被还原肽键类似物拮抗。
DOI：
10.1016/0024-3205(89)90231-2
复制
发表时间：
1989
期刊：
影响因子：
6.1
通讯作者：
Moody,TW
中科院分区：
文献类型：
--
作者：
Mahmoud,S;Palaszynski,E;Fiskum,G;Coy,DH;Moody,TW
用小细胞肺癌（SCLC）细胞株研究了3种还原肽键类似物（BN）的效价。（Psi13, 14, Leu14）BN、（Psi9, 10, Leu14）BN和（Psi12, 13, Leu14）BN抑制125i - grp特异性结合，ic50值分别为15、90和600 nM。（Psi13, 14, Leu14）BN和（Psi9, 10, Leu14）BN不升高细胞质Ca2+水平，但能拮抗BN引起的细胞质Ca2+升高。（psi13,14, Leu14）BN可拮抗BN引起的SCLC细胞克隆生长。这些数据表明，减少肽键类似物可能通过充当BN受体拮抗剂来破坏SCLC细胞的自分泌生长周期。
The potency of 3 reduced peptide bond analogues of bombesin (BN) was investigated using small cell lung cancer (SCLC) cell lines. (Psi13, 14, Leu14)BN, (Psi9, 10, Leu14)BN and (Psi12, 13, Leu14)BN inhibited specific binding of125I-GRP with IC50values of 15, 90, and 600 nM. (Psi13, 14, Leu14)BN and (Psi9, 10, Leu14)BN did not elevate cytosolic Ca2+levels but antagonized the increase in cytosolic Ca2+caused by BN. (Psi13, 14, Leu14)BN antagonized the clonal growth of SCLC cells caused by BN. These data indicate that reduced peptide bond analogues may discrupt the autocrine growth cycle of SCLC cells by functioning as BN receptor antagonists.