SURAMIN - POTENT ATPASE INHIBITOR WHICH ACTS ON INSIDE SURFACE OF SODIUM PUMP
SURAMIN - POTENT ATPASE INHIBITOR WHICH ACTS ON INSIDE SURFACE OF SODIUM PUMP
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DOI：
10.1016/0005-2736(73)90119-3
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发表时间：
1973-01-01
期刊：
影响因子：
--
通讯作者：
LEW, VL
中科院分区：
文献类型：
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作者：
FORTES, PAG;ELLORY, JC;LEW, VL
(1)不渗透性聚阴离子苏拉明抑制破膜制备物中的（Na+-K+）激活的ATP酶。苏拉明不影响Na+或K+的运输在完整的红细胞或resealed红细胞血影时，存在于孵育介质中，但似乎抑制Na+泵与苏拉明内resealed血影。苏拉明对其他ATP需要酶也有类似的抑制作用（10− 5-10− 4 M时抑制率为50%），表明与酶的底物位点发生了相互作用。2. (2)K+激活的p-硝基苯磷酸酶活性和[3 H]哇巴因结合也被苏拉明抑制。3. (3)苏拉明的抑制作用可通过清洗膜来逆转。4. (4)可以得出结论，苏拉明抑制Na+-K+转运系统通过与泵的细胞内部分的相互作用。5. (5)苏拉明作为泵抑制剂的潜在用途和修改其结构以产生荧光衍生物的可能性进行了讨论。
(1) The impermeant polyanion suramin inhibits the (Na+-K+)-activated ATPase in broken membrane preparations. Suramin does not affect Na+ or K+ transport in intact red cells or resealed red cell ghosts when present in the incubation medium, but appears to inhibit the Na+ pump in ghosts resealed with suramin inside. Other ATP-requiring enzymes are also inhibited by suramin with similar potency (50% inhibition at 10− 5-10− 4 M) suggesting an interaction with the substrate site of the enzyme. 2.(2) K+-activated p-nitrophenylphosphatase activity and [3 H] ouabain binding are also inhibited by suramin. 3.(3) The inhibition by suramin is reversed by washing the membranes. 4.(4) It is concluded that suramin inhibits the Na+-K+ transport system through interactions with the intracellular part of the pump. 5.(5) The potential usefulness of suramin as a pump inhibitor and the possibility of modifying its structure to yield fluorescent derivatives are discussed.