Jin Y J, Albers M W, Lane W S, Bierer B E, Schreiber S L, Burakoff S J
Division of Pediatric Oncology, Dana-Farber Cancer Institute, Boston, MA.
Proc Natl Acad Sci U S A. 1991 Aug 1;88(15):6677-81. doi: 10.1073/pnas.88.15.6677.
The 12-kDa FK506-binding protein (FKBP-12) is a cytosolic receptor for the immunosuppressants FK506 and rapamycin. Here we report the molecular cloning and subcellular localization of a 13-kDa FKBP (FKBP-13), which has a 21-amino acid signal peptide and appears to be membrane-associated. Although no internal hydrophobic region, and thus no transmembrane domain, is apparent within the 120 amino acids of mature FKBP-13, a potential endoplasmic reticulum retention sequence (Arg-Thr-Glu-Leu) is found at its C terminus. FKBP-13 has 51% nucleotide sequence identity and 43% amino acid sequence identity to FKBP-12; the N-terminal sequences are divergent, but the 92-amino acid C-terminal sequence of FKBP-13 has 46 identical and 20 related residues when compared with FKBP-12. The conserved residues that comprise the drug binding site and rotamase active site of FKBP-12 are completely conserved in FKBP-13. Therefore, the three-dimensional structures of FKBP-12 and the FKBP-12/FK506 complex are likely to be excellent models of the corresponding FKBP-13 structure.
12千道尔顿的FK506结合蛋白(FKBP - 12)是免疫抑制剂FK506和雷帕霉素的胞质受体。在此我们报道了一种13千道尔顿FKBP(FKBP - 13)的分子克隆及亚细胞定位,它具有一个21个氨基酸的信号肽,且似乎与膜相关。尽管在成熟的FKBP - 13的120个氨基酸内没有明显的内部疏水区域,因此也没有跨膜结构域,但在其C末端发现了一个潜在的内质网滞留序列(精氨酸 - 苏氨酸 - 谷氨酸 - 亮氨酸)。FKBP - 13与FKBP - 12具有51%的核苷酸序列同一性和43%的氨基酸序列同一性;其N末端序列不同,但与FKBP - 12相比,FKBP - 13的92个氨基酸的C末端序列有46个相同和20个相关残基。构成FKBP - 12药物结合位点和肽脯氨酰顺反异构酶活性位点的保守残基在FKBP - 13中完全保守。因此,FKBP - 12及FKBP - 12/FK506复合物的三维结构很可能是相应FKBP - 13结构的出色模型。