Kitabchi A E, Stentz F B
Biochem Biophys Res Commun. 1985 Apr 16;128(1):163-70. doi: 10.1016/0006-291x(85)91659-6.
To assess the role of various modulators of insulin processing on cell-associated A14-125I-insulin intermediates in human fibroblasts, we have studied the effect of N-ethylmaleimide (NEM), chloroquine, bacitracin, dansylcadavarine, and phenylarsine oxide on generation of these intermediate products with the use of HPLC. NEM completely inhibited generation of intermediate peaks or iodotyrosine. Chloroquine inhibited conversion of A14-125I-insulin to iodotyrosine by about 75 percent and the remaining A14-125I-insulin was not susceptible to acid wash. Bacitracin, dansylcadavarine, and phenylarsine oxide, on the other hand, stimulated formation of intermediate products with concomitant inhibition of iodotyrosine formation. We conclude that there are at least three components of insulin degradation in human fibroblasts. These include the sulfhydryl group inhibitor-sensitive, the intracellular chloroquine-sensitive, and membrane site inhibitor-sensitive components.
为了评估胰岛素加工的各种调节剂对人成纤维细胞中与细胞相关的A14 - 125I -胰岛素中间体的作用，我们利用高效液相色谱法研究了N -乙基马来酰亚胺（NEM）、氯喹、杆菌肽、丹磺酰尸胺和苯胂酸氧化物对这些中间产物生成的影响。NEM完全抑制了中间峰或碘酪氨酸的生成。氯喹将A14 - 125I -胰岛素向碘酪氨酸的转化抑制了约75%，剩余的A14 - 125I -胰岛素不易被酸洗脱。另一方面，杆菌肽、丹磺酰尸胺和苯胂酸氧化物刺激了中间产物的形成，同时抑制了碘酪氨酸的形成。我们得出结论，人成纤维细胞中胰岛素降解至少有三个成分。这些成分包括对巯基基团抑制剂敏感的成分、对细胞内氯喹敏感的成分以及对膜位点抑制剂敏感的成分。
