Kim Joungmok, Beak Dong-Gil, Kim Young-Tae, Choi Jung-Do, Yoon Moon-Young
Department of Chemistry, College of Natural Science, Hanyang University, Seoul 133-791, South Korea.
Biochem J. 2004 Nov 15;384(Pt 1):59-68. doi: 10.1042/BJ20040427.
AHAS (acetohydroxyacid synthase) catalyses the first committed step in the biosynthesis of branched-chain amino acids, such as valine, leucine and isoleucine. Owing to the unique presence of these biosynthetic pathways in plants and micro-organisms, AHAS has been widely investigated as an attractive target of several classes of herbicides. Recently, the crystal structure of the catalytic subunit of yeast AHAS has been resolved at 2.8 A (1 A=0.1 nm), showing that the active site is located at the dimer interface and is near the herbicide-binding site. In this structure, the existence of two disordered regions, a 'mobile loop' and a C-terminal 'lid', is worth notice. Although these regions contain the residues that are known to be important in substrate specificity and in herbicide resistance, they are poorly folded into any distinct secondary structure and are not within contact distance of the cofactors. In the present study, we have tried to demonstrate the role of these regions of tobacco AHAS by constructing variants with serial deletions, based on the structure of yeast AHAS. In contrast with the wild-type AHAS, the truncated mutant which removes the C-terminal lid, Delta630, and the internal deletion mutant without the mobile loop, Delta567-582, impaired the binding affinity for ThDP (thiamine diphosphate), and showed different elution profiles representing a monomeric form in gel-filtration chromatography. Our results suggest that these regions are involved in the binding/stabilization of the active dimer and ThDP binding.
乙酰羟酸合酶(AHAS)催化支链氨基酸(如缬氨酸、亮氨酸和异亮氨酸)生物合成中的首个关键步骤。由于这些生物合成途径在植物和微生物中独特存在,AHAS已被广泛研究,成为几类除草剂的理想作用靶点。最近,酵母AHAS催化亚基的晶体结构已解析到2.8埃(1埃 = 0.1纳米),结果表明活性位点位于二聚体界面附近且靠近除草剂结合位点。在此结构中,有两个无序区域值得关注,一个是“移动环”,另一个是C端“盖子”。尽管这些区域包含已知对底物特异性和除草剂抗性很重要的残基,但它们难以折叠成任何明显的二级结构,且与辅因子没有接触距离。在本研究中,我们基于酵母AHAS的结构,通过构建一系列缺失变体,试图阐明烟草AHAS这些区域的作用。与野生型AHAS不同,去除C端盖子的截短突变体Delta630和没有移动环的内部缺失突变体Delta567 - 582,削弱了对硫胺二磷酸(ThDP)的结合亲和力,并且在凝胶过滤色谱中显示出代表单体形式的不同洗脱图谱。我们的结果表明,这些区域参与活性二聚体的结合/稳定以及ThDP的结合。