Shao J, Grammatikakis N, Scroggins B T, Uma S, Huang W, Chen J J, Hartson S D, Matts R L
Department of Biochemistry and Molecular Biology, Oklahoma State University, Stillwater, Oklahoma 74078, USA.
J Biol Chem. 2001 Jan 5;276(1):206-14. doi: 10.1074/jbc.M007583200.
Recent studies indicate that p50(cdc37) facilitates Hsp90-mediated biogenesis of certain protein kinases. In this report, we examined whether p50(cdc37) is required for the biogenesis of the heme-regulated eIF2 alpha kinase (HRI) in reticulocyte lysate. p50(cdc37) interacted with nascent HRI co-translationally and this interaction persisted during the maturation and activation of HRI. p50(cdc37) stimulated HRI's activation in response to heme deficiency, but did not activate HRI per se. p50(cdc37) function was specific to immature and inactive forms of the kinase. Analysis of mutant Cdc37 gene products indicated that the N-terminal portion of p50(cdc37) interacted with immature HRI, but not with Hsp90, while the C-terminal portion of p50(cdc37) interacted with Hsp90. The Hsp90-specific inhibitor geldanamycin disrupted the ability of both Hsp90 and p50(cdc37) to bind HRI and promote its activation, but did not disrupt the native association of p50(cdc37) with Hsp90. A C-terminal truncated mutant of p50(cdc37) inhibited HRI's activation, prevented the interaction of Hsp90 with HRI, and bound to HRI irrespective of geldanamycin treatment. Additionally, native complexes of HRI with p50(cdc37) were detected in cultured K562 erythroleukemia cells. These results suggest that p50(cdc37) provides an activity essential to HRI biogenesis via a process regulated by nucleotide-mediated conformational switching of its partner Hsp90.
最近的研究表明,p50(cdc37) 促进热休克蛋白90(Hsp90)介导的某些蛋白激酶的生物合成。在本报告中,我们研究了网织红细胞裂解液中血红素调节的真核起始因子2α激酶(HRI)的生物合成是否需要p50(cdc37)。p50(cdc37) 与新生的HRI在共翻译过程中相互作用,并且这种相互作用在HRI的成熟和激活过程中持续存在。p50(cdc37) 响应血红素缺乏刺激HRI的激活,但本身并不激活HRI。p50(cdc37) 的功能对激酶的未成熟和无活性形式具有特异性。对突变型Cdc37基因产物的分析表明,p50(cdc37) 的N端部分与未成熟的HRI相互作用,但不与Hsp90相互作用,而p50(cdc37) 的C端部分与Hsp90相互作用。Hsp90特异性抑制剂格尔德霉素破坏了Hsp90和p50(cdc37) 结合HRI并促进其激活的能力,但没有破坏p50(cdc37) 与Hsp90的天然结合。p50(cdc37) 的C端截短突变体抑制HRI的激活,阻止Hsp90与HRI的相互作用,并且无论格尔德霉素处理如何都与HRI结合。此外,在培养的K562红白血病细胞中检测到HRI与p50(cdc37) 的天然复合物。这些结果表明,p50(cdc37) 通过其伴侣Hsp90的核苷酸介导的构象转换调节的过程,为HRI生物合成提供了一种必不可少的活性。