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免疫抑制剂FK-506与环孢菌素和双鞭甲藻素B一样，在体外可抑制钙调蛋白依赖性的延伸因子2的磷酸化，并在体内抑制佛波酯TPA对小鼠皮肤的生物学效应。

The immunosuppressant FK-506, like cyclosporins and didemnin B, inhibits calmodulin-dependent phosphorylation of the elongation factor 2 in vitro and biological effects of the phorbol ester TPA on mouse skin in vivo.

作者信息

Gschwendt M, Kittstein W, Marks F

机构信息

Department of Biochemistry, German Cancer Research Center, Heidelberg.

出版信息

Immunobiology. 1989 Mar;179(1):1-7. doi: 10.1016/s0171-2985(89)80002-6.

DOI:10.1016/s0171-2985(89)80002-6
PMID:2471685
Abstract

Similar to previous observations with cyclosporins and didemnin B, the novel immunosuppressant FK-506 inhibits the Ca2+/calmodulin-dependent phosphorylation of the eukaryotic elongation factor 2 of protein synthesis in vitro and biological effects of the phorbol ester TPA on mouse skin in vivo. These effects include the induction of the ear edema and the stimulation of alkaline phosphatase activity. FK-506 neither activates nor inhibits protein kinase C in vitro. FK-506 does not compete with cyclosporin A for the high-affinity binding sites in mouse epidermis cytosol.

摘要

与之前使用环孢菌素和苔藓虫素B的观察结果相似，新型免疫抑制剂FK-506在体外可抑制蛋白质合成中真核生物延伸因子2的Ca2+/钙调蛋白依赖性磷酸化，在体内可抑制佛波酯TPA对小鼠皮肤的生物学效应。这些效应包括诱导耳部水肿和刺激碱性磷酸酶活性。FK-506在体外既不激活也不抑制蛋白激酶C。FK-506在小鼠表皮细胞质中不与环孢菌素A竞争高亲和力结合位点。

相似文献

1
The immunosuppressant FK-506, like cyclosporins and didemnin B, inhibits calmodulin-dependent phosphorylation of the elongation factor 2 in vitro and biological effects of the phorbol ester TPA on mouse skin in vivo.免疫抑制剂FK-506与环孢菌素和双鞭甲藻素B一样，在体外可抑制钙调蛋白依赖性的延伸因子2的磷酸化，并在体内抑制佛波酯TPA对小鼠皮肤的生物学效应。
Immunobiology. 1989 Mar;179(1):1-7. doi: 10.1016/s0171-2985(89)80002-6.
2
Didemnin B inhibits biological effects of tumor promoting phorbol esters on mouse skin, as well as phosphorylation of a 100 kD protein in mouse epidermis cytosol.地棘蛙素B可抑制促肿瘤佛波酯对小鼠皮肤的生物学效应，以及小鼠表皮细胞质中一种100 kD蛋白质的磷酸化。
Cancer Lett. 1987 Feb;34(2):187-91. doi: 10.1016/0304-3835(87)90009-7.
3
The weak immunosuppressant cyclosporine D as well as the immunologically inactive cyclosporine H are potent inhibitors in vivo of phorbol ester TPA-induced biological effects in mouse skin and of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro.弱免疫抑制剂环孢素D以及免疫惰性的环孢素H在体内是佛波酯TPA诱导的小鼠皮肤生物学效应的有效抑制剂，在体外是Ca2+/钙调蛋白依赖性EF-2磷酸化的有效抑制剂。
Biochem Biophys Res Commun. 1988 Jan 29;150(2):545-51. doi: 10.1016/0006-291x(88)90428-7.
4
Ciclosporin inhibits phorbol-ester-induced hyperplastic transformation and tumor promotion in mouse skin probably by suppression of Ca2+/calmodulin-dependent processes such as phosphorylation of elongation factor 2.环孢素可能通过抑制钙/钙调蛋白依赖性过程（如延伸因子2的磷酸化）来抑制佛波酯诱导的小鼠皮肤增生性转化和肿瘤促进作用。
Skin Pharmacol. 1988;1(2):84-92. doi: 10.1159/000210753.
5
Effect of tumor promoting phorbol ester TPA on epidermal protein synthesis: stimulation of an elongation factor 2 phosphatase activity by TPA in vivo.促肿瘤佛波酯十四酰佛波醇乙酯（TPA）对表皮蛋白合成的影响：TPA在体内刺激延伸因子2磷酸酶活性
Biochem Biophys Res Commun. 1988 Jun 30;153(3):1129-35. doi: 10.1016/s0006-291x(88)81345-7.
6
Cyclosporin A inhibits phorbol ester-induced cellular proliferation and tumor promotion as well as phosphorylation of a 100-kd protein in mouse epidermis.
Carcinogenesis. 1987 Feb;8(2):203-7. doi: 10.1093/carcin/8.2.203.
7
Cyclosporin A inhibits biological effects of tumor promoting phorbol esters.环孢菌素A抑制促肿瘤佛波酯的生物学效应。
Biochem Biophys Res Commun. 1985 Jan 16;126(1):327-32. doi: 10.1016/0006-291x(85)90609-6.
8
Mechanism of protein synthesis inhibition by didemnin B in vitro.体外海兔毒素B抑制蛋白质合成的机制。
Biochemistry. 1995 Jul 18;34(28):9177-84. doi: 10.1021/bi00028a030.
9
FK-506, a potent novel immunosuppressive agent, binds to a cytosolic protein which is distinct from the cyclosporin A-binding protein, cyclophilin.FK-506是一种强效新型免疫抑制剂，它与一种胞质蛋白结合，这种蛋白不同于环孢素A结合蛋白亲环蛋白。
J Immunol. 1989 Sep 1;143(5):1580-3.
10
Bryostatin 1, an activator of protein kinase C, mimics as well as inhibits biological effects of the phorbol ester TPA in vivo and in vitro.苔藓抑素1是一种蛋白激酶C激活剂，在体内和体外既能模拟又能抑制佛波酯TPA的生物学效应。
Carcinogenesis. 1988 Apr;9(4):555-62. doi: 10.1093/carcin/9.4.555.

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