Biochemistry. 1973 Nov 6;12(23):4799-801. doi: 10.1021/bi00747a036.
人红细胞中己糖转运系统的不对称性。细胞松弛素B、根皮素和麦芽糖作为竞争性抑制剂的作用比较。
Asymmetry of the hexose transfer system in human erythrocytes. Comparison of the effects of cytochalasin B, phloretin and maltose as competitive inhibitors.
Cytochalasin B inhibits glucose transfer in human red cells. With glucose exit the inhibition is typically non-competitive, but hexose exchange is competitively inhibited. 2. At 16 degrees C the inhibitory constant for inhibition of 3-O-methyl glucose exchange is estimated at 1.1 X 10(-7) M while that for inhibition of glucose exit is 5.0 X 10(-7) M. 3. Uptake of labelled Cytochalasin B includes a saturable component which when correlated with the inhibition of exchange corresponds to a maximal binding of ca. 2.4 X 10(5) molecules per cell. 4. The kinetic parameters are compared with those for maltose (a competitive inhibitor acting on the outside only) and phloretin (an inhibitor acting both inside and out). 5. Kinetic evidence suggests that Cytochalasin B reacts with the inside of the hexose transfer system and that the anomalous inhibitory characteristics are due to the chemical asymmetry of the system. Independent evidence in support of this view is discussed.
摘要
细胞松弛素B抑制人体红细胞中的葡萄糖转运。对于葡萄糖外流,这种抑制通常是非竞争性的,但己糖交换受到竞争性抑制。2. 在16℃时,抑制3 - O - 甲基葡萄糖交换的抑制常数估计为1.1×10⁻⁷M,而抑制葡萄糖外流的抑制常数为5.0×10⁻⁷M。3. 标记的细胞松弛素B的摄取包括一个可饱和成分,当与交换抑制相关时,相当于每个细胞约2.4×10⁵个分子的最大结合量。4. 将动力学参数与麦芽糖(一种仅作用于外部的竞争性抑制剂)和根皮素(一种内外都起作用的抑制剂)的参数进行比较。5. 动力学证据表明细胞松弛素B与己糖转运系统的内部发生反应,并且异常的抑制特性是由于该系统的化学不对称性。讨论了支持这一观点的独立证据。