Uesugi Yoshiko, Arima Jiro, Iwabuchi Masaki, Hatanaka Tadashi
Research Institute for Biological Sciences-Okayama, 7549-1 Kibichuo-cho, Kaga-gun, Okayama 716-1241, Japan.
Protein Sci. 2007 Feb;16(2):197-207. doi: 10.1110/ps.062537907. Epub 2006 Dec 22.
We have recently shown that two flexible loops of Streptomyces phospholipase D (PLD) affect the catalytic reaction of the enzyme by a comparative study of chimeric PLDs. Gly188 and Asp191 of PLD from Streptomyces septatus TH-2 (TH-2PLD) were identified as the key amino acid residues involved in the recognition of phospholipids. In the present study, we further investigated the relationship between a C-terminal loop of TH-2PLD and PLD activities to elucidate the reaction mechanism and the recognition of the substrate. By analyzing chimeras and mutants in terms of hydrolytic and transphosphatidylation activities, Ala426 and Lys438 of TH-2PLD were identified as the residues associated with the activities. We found that Gly188 and Asp191 recognized substrate forms, whereas residues Ala426 and Lys438 enhanced transphosphatidylation and hydrolysis activities regardless of the substrate form. By substituting Ala426 and Lys438 with Phe and His, respectively, the mutant showed not only higher activities but also higher thermostability and tolerance against organic solvents. Furthermore, the mutant also improved the selectivity of the transphosphatidylation activity. The residues Ala426 and Lys438 were located in the C-terminal flexible loop of Streptomyces PLD separate from the highly conserved catalytic HxKxxxxD motifs. We demonstrated that this C-terminal loop, which formed the entrance of the active well, has multiple functional roles in Streptomyces PLD.
我们最近通过对嵌合磷脂酶D(PLD)的比较研究表明,链霉菌磷脂酶D的两个柔性环影响该酶的催化反应。来自栖土链霉菌TH-2(TH-2PLD)的PLD中的Gly188和Asp191被确定为参与磷脂识别的关键氨基酸残基。在本研究中,我们进一步研究了TH-2PLD的C末端环与PLD活性之间的关系,以阐明反应机制和底物识别。通过分析嵌合体和突变体的水解和转磷脂酰化活性,TH-2PLD的Ala426和Lys438被确定为与活性相关的残基。我们发现Gly188和Asp191识别底物形式,而无论底物形式如何,Ala426和Lys438残基均增强转磷脂酰化和水解活性。通过分别用Phe和His替代Ala426和Lys438,突变体不仅表现出更高的活性,还表现出更高的热稳定性和对有机溶剂的耐受性。此外,该突变体还提高了转磷脂酰化活性的选择性。Ala426和Lys438残基位于链霉菌PLD的C末端柔性环中,与高度保守的催化HxKxxxxD基序分开。我们证明,形成活性阱入口的这个C末端环在链霉菌PLD中具有多种功能作用。