N-isobutyryl-His-Trp-Ala-Val-D-Ala-His-Leu-NHMe (ICI 216140) a potent in vivo antaconist analogue of bombesin/gastrin releasing peptide (BN/GRP) derived from the C-terminal sequence lacking the final methionine residue.
N-isobutyryl-His-Trp-Ala-Val-D-Ala-His-Leu-NHMe (ICI 216140) a potent in vivo antaconist analogue of bombesin/gastrin releasing peptide (BN/GRP) derived from the C-terminal sequence lacking the final methionine residue.
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N-异丁酰-His-Trp-Ala-Val-D-Ala-His-Leu-NHMe (ICI 216140) 一种有效的体内蟾蜍素/胃泌素释放肽 (BN/GRP) 拮抗剂类似物，源自缺乏 C 端序列
DOI：
10.1016/0024-3205(89)90417-7
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发表时间：
1989
期刊：
影响因子：
6.1
通讯作者：
P. Scholes
中科院分区：
文献类型：
--
作者：
R. Camble;R. Cotton;A. Dutta;A. Garner;C. F. Hayward;V. Moore;P. Scholes
Swiss 3T3 细胞中 GRP 受体介导的生长反应已被用来鉴定 BN/GRP 拮抗剂。对 P 物质类似物和截短的 GRP 类似物的铃蟾肽拮抗作用的分析表明，C 末端甲硫氨酸残基的删除对于拮抗作用很重要。合成了在体外 3T3 系统中显示出有效拮抗剂活性的 Des-Met 类似物 (IC 50∼ 2nM)。这些肽的进一步结构修饰导致鉴定出 (CH 3) 2 CHCOHisTrpAlaValDAlaHisLeuNHCH 3 (ICI 216140)，当以 2.0 mg/kg 皮下给药时，可将铃蟾肽刺激的大鼠胰淀粉酶分泌降低至基础水平。
The GRP receptor mediated growth response in Swiss 3T3 cells has been used to identify BN/GRP antagonists. Analysis of bombesin antagonism by substance P analogues and by truncated GRP analogues revealed that deletion of the C-terminal methionine residue was important for antagonism. Des-Met analogues showing potent antagonist activity in the in vitro 3T3 system (IC 50∼ 2nM) were synthesized. Further structural modification of these peptides led to the identification of (CH 3) 2 CHCO His Trp Ala Val D Ala His Leu NHCH 3 (ICI 216140) which reduced bombesin-stimulated rat pancreatic amylase secretion to basal levels when administered subcutaneously at 2.0 mg per kg.
小细胞肺癌铃蟾肽受体被还原肽键类似物拮抗。
影响因子：
6.1
作者：
Mahmoud,S;Palaszynski,E;Fiskum,G;Coy,DH;Moody,TW
通讯作者：
Moody,TW