Selective inhibition of the insulin-stimulated phosphorylation of the 95,000 dalton subunit of the insulin receptor by TAME or BAEE.
Selective inhibition of the insulin-stimulated phosphorylation of the 95,000 dalton subunit of the insulin receptor by TAME or BAEE.
复制标题
TAME 或 BAEE 选择性抑制胰岛素刺激的胰岛素受体 95,000 道尔顿亚基的磷酸化。
DOI：
10.1016/s0006-291x(84)80272-7
复制
发表时间：
1984
影响因子：
3.1
通讯作者：
Larner,J
中科院分区：
文献类型：
--
作者：
Tamura,S;Schwartz,CF;Whipple,JH;Dubler,RE;Fujita-Yamaguchi,Y;Larner,J
加入Nα-对甲苯磺酰基-L-精氨酸甲酯或Nα-苯甲酰基-L-精氨酸乙酯可抑制胰岛素对大鼠脂肪细胞部分纯化胰岛素受体组分和人胎盘高度纯化胰岛素受体制剂中胰岛素受体95，000道尔顿亚基磷酸化的刺激。N-α-对甲苯磺酰基-L-赖氨酸氯甲基酮、Nα-对甲苯磺酰基-L-赖氨酸甲酯或N-乙酰基-L-苯丙氨酸乙酯的效力要低得多，而N-苯甲酰基-L-丙氨酸甲酯则无作用。精氨酸类似物对磷酸化的抑制不需要在磷酸化之前在胰岛素存在下将胰岛素受体与抑制剂预孵育。Nα-对甲苯磺酰基-L-精氨酸甲酯的抑制作用可通过用冷ATP和MnCl 2预孵育受体组分而降低。这些结果表明，Nα-对甲苯磺酰基-1-精氨酸甲酯抑制胰岛素刺激的磷酸化过程中的初始ATP和Mn ~（2+）依赖性反应。
Added Nα-p-tosyl-l-arginine methyl ester or Nα-benzoyl-l-arginine ethyl ester inhibited the stimulation by insulin of phosphorylation of the 95,000 dalton subunit of the insulin receptor both in a partially purified insulin receptor fraction from rat adipocytes and in a highly purified insulin receptor preparation from human placenta. N-α-p-tosyl-l-lysine chloromethyl ketone, Nα-p-tosyl-l-lysine methyl ester, or N-acetyl-l-phenylalanine ethyl ester were much less potent, while N-benzoyl-l-alanine methyl ester was without effect. Inhibition of the phosphorylation by the arginine analogues did not require preincubation of the insulin receptor with inhibitors in the presence of insulin prior to phosphorylation. Inhibition by Nα-p-tosyl-l-arginine methyl ester was decreased by preincubation of the receptor fraction with cold ATP and MnCl2. These results suggest that Nα-p-tosyl-1-arginine methyl ester inhibits an initial ATP and Mn2+dependent reaction in insulin-stimulated phosphorylation process.