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二肉豆蔻酰磷脂酰肌醇-4-磷酸的硫代磷酸酯类似物是哺乳动物磷酸肌醇特异性磷脂酶C的底物。

A thiophosphate analog of dimyristoylphosphatidyl-inositol-4-phosphate is a substrate for mammalian phosphoinositide-specific phospholipase C.

作者信息

Hendrickson H S, Hendrickson E K

机构信息

Department of Chemistry, University of Washington, Seattle 98195-1700, USA.

出版信息

Bioorg Med Chem Lett. 1998 May 5;8(9):1057-60. doi: 10.1016/s0960-894x(98)00174-7.

DOI:10.1016/s0960-894x(98)00174-7
PMID:9871707
Abstract

1,2-Dimyristoyloxypropane-3-thiophosphate(rac-1-myo-inositol-4- phosphate), a thiophosphate analog of dimyristoyl phosphatidylinositol-4-phosphate was synthesized as a substrate for mammalian phosphoinositide-specific phospholipase C. Its activity with delta(1-132)-PI-PLC-delta 1 (a deletion mutant with the N-terminal pleckstrin homology domain removed) was studied in sonicated dispersions, with and without added Triton X-100. It had an initial activity of about 30 mumol min-1 mg-1, which rapidly decreased due to substrate depletion in the vesicle or micelle. The slower rate of hydrolysis appeared limited by enzyme hopping or exchange of substrate between vesicles or micelles, which was more rapid in the presence of detergent.

摘要

1,2 - 二肉豆蔻酰氧基丙烷 - 3 - 硫代磷酸酯(消旋 - 1 - 肌醇 - 4 - 磷酸),一种二肉豆蔻酰磷脂酰肌醇 - 4 - 磷酸的硫代磷酸酯类似物,被合成为哺乳动物磷酸肌醇特异性磷脂酶C的底物。在添加和不添加Triton X - 100的情况下,研究了其与δ(1 - 132)-PI - PLC - δ1(一种去除了N端普列克底物蛋白同源结构域的缺失突变体)在超声分散体中的活性。它的初始活性约为30 μmol min⁻¹ mg⁻¹,由于囊泡或胶束中底物的消耗,该活性迅速下降。水解速率较慢似乎受到酶跳跃或底物在囊泡或胶束之间交换的限制,在存在去污剂的情况下这种交换更快。

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