Staley J, Coy D, Taylor J E, Kim S, Moody T W
Department of Biochemistry & Molecular Biology, George Washinton University School of Medicine and Health Sciences, Washington, DC 20037.
Peptides. 1991 Jan-Feb;12(1):145-9. doi: 10.1016/0196-9781(91)90181-n.
A series of bombesin (BN) analogues lacking the C-terminal methionine at the 14 position were evaluated as BN receptor antagonists. [D-Phe6]BN(6-13)amide inhibited specific 125I-GRP binding to lung cancer cell line NCI-H720 with an IC50 value of 12 nM. In contrast, [D-Phe6]BN(6-13)propylamide, butylamide and methylester were more potent with IC50 values of 3, 5 and 5 nM whereas [D-Phe6,Sta13]BN(6-13)amide was less potent with an IC50 value of 180 nM. [D-Phe6]BN(6-13)propylamide antagonized the ability of BN to elevate cytosolic Ca2+, whereas [D-Phe6]BN(6-13)butylamide was a partial agonist. In a small cell lung cancer (SCLC) growth assay, [D-Phe6]BN(6-13)propylamide inhibited colony formation. In summary, BN analogues which lack a C-terminal methionine may function as useful SCLC BN receptor antagonists.
一系列在14位缺少C末端甲硫氨酸的蛙皮素（BN）类似物被评估为BN受体拮抗剂。[D-Phe6]BN(6-13)酰胺抑制125I-GRP与肺癌细胞系NCI-H720的特异性结合，IC50值为12 nM。相比之下，[D-Phe6]BN(6-13)丙酰胺、丁酰胺和甲酯的活性更强，IC50值分别为3、5和5 nM，而[D-Phe6,Sta13]BN(6-13)酰胺的活性较弱，IC50值为180 nM。[D-Phe6]BN(6-13)丙酰胺拮抗BN升高胞质Ca2+的能力，而[D-Phe6]BN(6-13)丁酰胺是一种部分激动剂。在小细胞肺癌（SCLC）生长试验中，[D-Phe6]BN(6-13)丙酰胺抑制集落形成。总之，缺少C末端甲硫氨酸的BN类似物可能作为有用的SCLC BN受体拮抗剂发挥作用。
