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二酰基甘油激酶抑制剂R59949可增强人血小板中47千道尔顿蛋白的分泌,但不会增加其磷酸化水平。

The diacylglycerol kinase inhibitor, R59949, potentiates secretion but not increased phosphorylation of a 47 kDalton protein in human platelets.

作者信息

Rodríguez-Liñares B, Walker T, Watson S

机构信息

Department of Pharmacology, Oxford, U.K.

出版信息

Biochem Pharmacol. 1991 Mar 1;41(5):835-8. doi: 10.1016/0006-2952(91)90089-n.

DOI:10.1016/0006-2952(91)90089-n
PMID:1847818
Abstract

We have investigated the action of a novel inhibitor of DG-kinase, R59949. This agent was found to produce partial inhibition of formation of phosphatidic acid in human platelets challenged with thrombin, DC8 or OAG. However, this effect was not associated with enhanced phosphorylation of a 47 kDa protein, a known substrate for protein kinase C. We therefore believe that this compound does not represent a major advance on its earlier prototype, R59022.

摘要

我们研究了新型二酰甘油激酶抑制剂R59949的作用。发现该药物对用凝血酶、DC8或1-油酰基-2-乙酰基-sn-甘油(OAG)刺激的人血小板中磷脂酸的形成产生部分抑制作用。然而,这种作用与蛋白激酶C的已知底物——一种47 kDa蛋白的磷酸化增强无关。因此,我们认为该化合物在其早期原型R59022的基础上并没有取得重大进展。

相似文献

1
The diacylglycerol kinase inhibitor, R59949, potentiates secretion but not increased phosphorylation of a 47 kDalton protein in human platelets.二酰基甘油激酶抑制剂R59949可增强人血小板中47千道尔顿蛋白的分泌,但不会增加其磷酸化水平。
Biochem Pharmacol. 1991 Mar 1;41(5):835-8. doi: 10.1016/0006-2952(91)90089-n.
2
A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets.二酰基甘油激酶抑制剂R59022可增强凝血酶刺激的人血小板的分泌及聚集。
Biochem J. 1987 May 1;243(3):809-13. doi: 10.1042/bj2430809.
3
Inhibition of thrombin-induced Ca²⁺ influx in platelets by R59949, an inhibitor of diacylglycerol kinase.二酰基甘油激酶抑制剂 R59949 抑制凝血酶诱导的血小板内钙离子内流。
J Pharm Pharmacol. 2012 Jun;64(6):855-61. doi: 10.1111/j.2042-7158.2012.01485.x. Epub 2012 Mar 12.
4
The use of diacylglycerol kinase inhibitors for elucidating the roles of protein kinase C.
Adv Second Messenger Phosphoprotein Res. 1990;24:491-6.
5
Differential effects of the diacylglycerol kinase inhibitor R59022 on thrombin versus collagen-induced human platelet secretion.二酰基甘油激酶抑制剂R59022对凝血酶与胶原诱导的人血小板分泌的不同作用。
Biochim Biophys Acta. 1988 Apr 2;969(1):9-17. doi: 10.1016/0167-4889(88)90082-1.
6
Activation of phospholipase C and protein kinase C has little involvement in ADP-induced primary aggregation of human platelets: effects of diacylglycerols, the diacylglycerols, the diacylglycerol kinase inhibitor R59022, staurosporine and okadaic acid.磷脂酶C和蛋白激酶C的激活在二磷酸腺苷诱导的人血小板初级聚集中几乎不起作用:二酰基甘油、二酰基甘油激酶抑制剂R59022、星形孢菌素和冈田酸的作用
Biochem J. 1993 Mar 15;290 ( Pt 3)(Pt 3):849-56. doi: 10.1042/bj2900849.
7
The role of endogenously formed diacylglycerol in the propagation and termination of platelet activation. A biochemical and functional analysis using the novel diacylglycerol kinase inhibitor, R 59 949.内源性生成的二酰基甘油在血小板激活的传播与终止中的作用。使用新型二酰基甘油激酶抑制剂R 59 949进行的生化与功能分析。
J Biol Chem. 1989 Feb 25;264(6):3274-85.
8
R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet.R 59 022,一种二酰基甘油激酶抑制剂。它对完整血小板中由二酰基甘油和凝血酶诱导的C激酶激活的影响。
J Biol Chem. 1985 Dec 15;260(29):15762-70.
9
The diacylglycerol kinase inhibitor, R59022, potentiates cholecystokinin-induced enzyme secretion from rabbit pancreatic acini.二酰基甘油激酶抑制剂R59022可增强胆囊收缩素诱导的兔胰腺腺泡酶分泌。
Eur J Biochem. 1990 Mar 10;188(2):333-8. doi: 10.1111/j.1432-1033.1990.tb15408.x.
10
A role of diacylglycerol kinase in stimulus-secretion coupling of human platelets. Dissociation of serotonin secretion from Ca2+ mobilization.二酰基甘油激酶在人血小板刺激-分泌偶联中的作用。5-羟色胺分泌与Ca2+动员的解离。
Thromb Res. 1987 Jul 1;47(1):25-35. doi: 10.1016/0049-3848(87)90237-4.

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