Carrello Amerigo, Allan Rudi K, Morgan Sarah L, Owen Barbara A L, Mok Danny, Ward Bryan K, Minchin Rodney F, Toft David O, Ratajczak Thomas
Laboratory for Molecular Endocrinology, Western Australian Institute for Medical Research, The University of Western Australia, Nedlands, Western Australia 6009, Australia.
Cell Stress Chaperones. 2004 Summer;9(2):167-81. doi: 10.1379/csc-26r.1.
The high-affinity ligand-binding form of unactivated steroid receptors exists as a multicomponent complex that includes heat shock protein (Hsp)90; one of the immunophilins cyclophilin 40 (CyP40), FKBP51, or FKBP52; and an additional p23 protein component. Assembly of this heterocomplex is mediated by Hsp70 in association with accessory chaperones Hsp40, Hip, and Hop. A conserved structural element incorporating a tetratricopeptide repeat (TPR) domain mediates the interaction of the immunophilins with Hsp90 by accommodating the C-terminal EEVD peptide of the chaperone through a network of electrostatic and hydrophobic interactions. TPR cochaperones recognize the EEVD structural motif common to both Hsp90 and Hsp70 through a highly conserved clamp domain. In the present study, we investigated in vitro the molecular interactions between CyP40 and FKBP52 and other stress-related components involved in steroid receptor assembly, namely Hsp70 and Hop. Using a binding protein-retention assay with CyP40 fused to glutathione S-transferase immobilized on glutathione-agarose, we have identified the constitutively expressed form of Hsp70, heat shock cognate (Hsc)70, as an additional target for CyP40. Deletion mapping studies showed the binding determinants to be similar to those for CyP40-Hsp90 interaction. Furthermore, a mutational analysis of CyP40 clamp domain residues confirmed the importance of this motif in CyP40-Hsc70 interaction. Additional residues thought to mediate binding specificity through hydrophobic interactions were also important for Hsc70 recognition. CyP40 was shown to have a preference for Hsp90 over Hsc70. Surprisingly, FKBP52 was unable to compete with CyP40 for Hsc70 binding, suggesting that FKBP52 discriminates between the TPR cochaperone-binding sites in Hsp90 and Hsp70. Hop, which contains multiple units of the TPR motif, was shown to be a direct competitor with CyP40 for Hsc70 binding. Similar to Hop, CyP40 was shown not to influence the adenosine triphosphatase activity of Hsc70. Our results suggest that CyP40 may have a modulating role in Hsc70 as well as Hsp90 cellular function.
未活化的类固醇受体的高亲和力配体结合形式以多组分复合物的形式存在,该复合物包括热休克蛋白(Hsp)90;免疫亲和蛋白亲环蛋白40(CyP40)、FKBP51或FKBP52中的一种;以及另外的p23蛋白组分。这种异源复合物的组装由Hsp70与辅助伴侣蛋白Hsp40、Hip和Hop共同介导。一个包含四肽重复(TPR)结构域的保守结构元件通过静电和疏水相互作用网络容纳伴侣蛋白的C末端EEVD肽,从而介导免疫亲和蛋白与Hsp90的相互作用。TPR共伴侣蛋白通过一个高度保守的钳结构域识别Hsp90和Hsp70共有的EEVD结构基序。在本研究中,我们在体外研究了CyP40与FKBP52以及其他参与类固醇受体组装的应激相关组分(即Hsp70和Hop)之间的分子相互作用。使用固定在谷胱甘肽琼脂糖上的与谷胱甘肽S-转移酶融合的CyP40进行结合蛋白保留测定,我们确定了组成型表达的Hsp70形式,即热休克同源蛋白(Hsc)70,是CyP40的另一个靶点。缺失定位研究表明结合决定簇与CyP40-Hsp90相互作用的决定簇相似。此外,对CyP40钳结构域残基的突变分析证实了该基序在CyP40-Hsc70相互作用中的重要性。其他被认为通过疏水相互作用介导结合特异性的残基对Hsc70识别也很重要。结果表明,CyP40对Hsp90的偏好高于Hsc70。令人惊讶的是,FKBP52不能与CyP40竞争Hsc70的结合,这表明FKBP52区分Hsp90和Hsp70中TPR共伴侣蛋白的结合位点。含有多个TPR基序单元的Hop被证明是与CyP40竞争Hsc70结合的直接竞争者。与Hop类似 CyP40不影响Hsc70的腺苷三磷酸酶活性。我们的结果表明,CyP40可能在Hsc70以及Hsp90的细胞功能中具有调节作用。