Maier Timm, Strater Norbert, Schuette Christina G, Klingenstein Ralf, Sandhoff Konrad, Saenger Wolfram
Institut für Chemie Kristallographie, Freie Universität Berlin, Takustrasse 6, 14195 Berlin, Germany.
J Mol Biol. 2003 May 2;328(3):669-81. doi: 10.1016/s0022-2836(03)00311-5.
Human lysosomal beta-hexosaminidases are dimeric enzymes composed of alpha and beta-chains, encoded by the genes HEXA and HEXB. They occur in three isoforms, the homodimeric hexosaminidases B (betabeta) and S (alphaalpha), and the heterodimeric hexosaminidase A (alphabeta), where dimerization is required for catalytic activity. Allelic variations in the HEXA and HEXB genes cause the fatal inborn errors of metabolism Tay-Sachs disease and Sandhoff disease, respectively. Here, we present the crystal structure of a complex of human beta-hexosaminidase B with a transition state analogue inhibitor at 2.3A resolution (pdb 1o7a). On the basis of this structure and previous studies on related enzymes, a retaining double-displacement mechanism for glycosyl hydrolysis by beta-hexosaminidase B is proposed. In the dimer structure, which is derived from an analysis of crystal packing, most of the mutations causing late-onset Sandhoff disease reside near the dimer interface and are proposed to interfere with correct dimer formation. The structure reported here is a valid template also for the dimeric structures of beta-hexosaminidase A and S.
人溶酶体β-己糖胺酶是由α链和β链组成的二聚体酶,分别由HEXA和HEXB基因编码。它们以三种同工型存在,即同二聚体己糖胺酶B(ββ)和S(αα),以及异二聚体己糖胺酶A(αβ),其中二聚化是催化活性所必需的。HEXA和HEXB基因的等位基因变异分别导致致命的代谢性先天性疾病泰-萨克斯病和桑德霍夫病。在此,我们展示了人β-己糖胺酶B与过渡态类似物抑制剂复合物在2.3埃分辨率下的晶体结构(pdb 1o7a)。基于该结构以及之前对相关酶的研究,提出了β-己糖胺酶B进行糖基水解的保留双置换机制。在通过晶体堆积分析得出的二聚体结构中,大多数导致迟发性桑德霍夫病的突变位于二聚体界面附近,并被认为会干扰正确的二聚体形成。此处报道的结构也是β-己糖胺酶A和S二聚体结构的有效模板。