Mahmoud S, Palaszynski E, Fiskum G, Coy D H, Moody T W
Dept. of Biochemistry, George Washington University School of Medicine & Health Sciences, Washington, DC 20037.
Life Sci. 1989;44(5):367-73. doi: 10.1016/0024-3205(89)90231-2.
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 of 125I-GRP with IC50 values 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 disrupt the autocrine growth cycle of SCLC cells by functioning as BN receptor antagonists.
利用小细胞肺癌（SCLC）细胞系研究了3种蛙皮素（BN）的还原肽键类似物的效力。（Ψ13,14，Leu14）BN、（Ψ9,10，Leu14）BN和（Ψ12,13，Leu14）BN抑制125I-GRP的特异性结合，IC50值分别为15、90和600 nM。（Ψ13,14，Leu14）BN和（Ψ9,10，Leu14）BN不会提高胞质Ca2+水平，但能拮抗BN引起的胞质Ca2+增加。（Ψ13,14，Leu14）BN拮抗BN引起的SCLC细胞的克隆生长。这些数据表明，还原肽键类似物可能通过作为BN受体拮抗剂发挥作用来破坏SCLC细胞的自分泌生长周期。
