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- W2364155957 abstract "Objective It has been reported that several kinds of tumors express increased insulin receptors and the molecule of insulin can be internalized in cells and enter the nuclei through the mediation of the insulin receptor.In this study,we investigated the receptor binding characteristics of insulin-IUdR for the possibility of using insulin as carriers for carcinoma targeted therapy by receptor mediation. Methods IUdR (idoxuridine) was covalently linked to insulin using the bifunctional reagent succinic acid. The insulin-IUdR conjugate was purified by polyacrylamide agarose gel electrophoresis and analysed by high performance liquid chromatography and SDS-polyacrylamide agarose gel electrophoresis. The human hepatocellular carcinoma specimens confirmed histologically were obtained from patients at surgery and immediately frozen under -80 ℃. Cell membrane fractions were isolated by sucrose density gradient centrifugation.Competitive displacement of 125I-insulin with insulin and insulin-IUdR binding to the insulin receptor were carried out. Values of IC 50 and KI were calculated to observe the characteristics of insulin-IUdR binding to the insulin receptor. Results Insulin-IUdR competed as effectively as insulin with 125I-insulin for binding to insulin receptors. The values of IC 501 and IC 502 for insulin-IUdR were (11.50±2.83) nmol/L and (19.35±5.11) nmol/L, respectively; the values of KI1 and KI2 for insulin-IUdR were (11.26±2.65) nmol/L and (19.30±5.02) nmol/L, respectively, while values of IC 501 and IC 502 for insulin were (5.01±1.24) nmol/L and (17.75±4.86) nmol/L, respectively. The values of KI1 and KI2 for insulin were (4.85±1.12) nmol/L and (17.69±4.81) nmol/L, respectively. Conclusions Insulin-IUdR could bind with the insulin receptor with high affinity.The result shows that there is a possibility of using insulin as carriers for carcinoma targeted therapy through receptor mediation." @default.
- W2364155957 created "2016-06-24" @default.
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- W2364155957 date "2002-01-01" @default.
- W2364155957 modified "2023-09-24" @default.
- W2364155957 title "Study on insulin receptor binding characteristics of insulin-IUdR" @default.
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