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酪氨酸磷酸化抑制剂对利用GTP的酶的抑制作用。

Inhibition of GTP-utilizing enzymes by tyrphostins.

作者信息

Wolbring G, Hollenberg M D, Schnetkamp P P

机构信息

Department of Medical Biochemistry, University of Calgary, Alberta, Canada.

出版信息

J Biol Chem. 1994 Sep 9;269(36):22470-2.

PMID:7915715
Abstract

Tyrphostins are a group of organic compounds which are widely used as a tool to specifically inhibit protein tyrosine kinases (Yaish, P., Gazit, A., Gilon, C., and levitzki A. (1988) Science 242, 933-935; Gazit, A., Yaish, P., Gilon, C., and Levitzki A. (1989) J. Med. Chem. 32, 2344-2352; Lyall, R. M., Zilberstein, A., Gazit, A., Gilon, C., Levitzki, A., and Schlessinger J. (1989) J. Biol. Chem. 264, 14503-14509; Osherov, N., Gazit, A., Gilon, C., and Levitzki, A. (1993) J. Biol. Chem. 268, 11134-11142). We report here that members of the tyrphostin family inhibit the GTPase activity of transducin and the enzymatic activities of other GTP-utilizing proteins in retinal rod outer segments, such as guanylyl cyclase or fructose-6-phosphate kinase. In contrast, ATP-utilizing enzymes such as hexokinase or rhodopsin kinase were not effected.

摘要

tyrphostins是一类有机化合物,被广泛用作特异性抑制蛋白酪氨酸激酶的工具(Yaish, P., Gazit, A., Gilon, C., 和levitzki A. (1988) 《科学》242, 933 - 935;Gazit, A., Yaish, P., Gilon, C., 和Levitzki A. (1989) 《药物化学杂志》32, 2344 - 2352;Lyall, R. M., Zilberstein, A., Gazit, A., Gilon, C., Levitzki, A., 和Schlessinger J. (1989) 《生物化学杂志》264, 14503 - 14509;Osherov, N., Gazit, A., Gilon, C., 和Levitzki, A. (1993) 《生物化学杂志》268, 11134 - 11142)。我们在此报告,tyrphostin家族成员抑制转导素的GTP酶活性以及视网膜视杆细胞外段中其他利用GTP的蛋白质的酶活性,如鸟苷酸环化酶或6 - 磷酸果糖激酶。相比之下,利用ATP的酶,如己糖激酶或视紫红质激酶则不受影响。

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