Differences in regulatory properties between human and rat glucokinase regulatory protein

Differences in regulatory properties between human and rat glucokinase regulatory protein
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DOI:
10.1042/bj20031414
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发表时间:
2004-03-01
影响因子:
4.1
通讯作者:
Agius, L
Agius, L
中科院分区:
生物学3区
文献类型:
--
作者:
Brocklehurst, KJ;Davies, RA;Agius, L

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大鼠和爪蟾的葡萄糖激酶调节蛋白(GKRPs)对葡萄糖激酶的抑制作用是有充分证据的。我们报告了人类和大鼠GKRPs对葡萄糖激酶活性的影响的比较。在缺乏6-磷酸果糖或6-磷酸山梨醇的情况下,人GKRP是一种比大鼠GKRP更有效的葡萄糖激酶抑制剂,并且对这些配体具有更高的亲和力。然而,人和大鼠GKRPs对果糖1-磷酸和氯化物具有相似的亲和力。在啮齿类动物和人类蛋白质之间不保守的残基会影响果糖6-磷酸和山梨醇6-磷酸的亲和力,以及在没有这些配体的情况下GKRP对葡萄糖激酶的抑制效力。
The inhibition of glucokinase by rat and Xenopus GKRPs (glucokinase regulatory protein) is well documented. We report a comparison of the effects of human and rat GKRPs on glucokinase activity. Human GKRP is a more potent inhibitor of glucokinase than rat GKRP in the absence of fructose 6-phosphate or sorbitol 6-phosphate, and has a higher affinity for these ligands. However, human and rat GKRPs have similar affinities for fructose 1-phosphate and chloride. Residues that are not conserved between the rodent and human proteins affect both the affinity for fructose 6-phosphate and sorbitol 6-phosphate and the inhibitory potency of GKRP on glucokinase in the absence of these ligands.