Fauman E B, Cogswell J P, Lovejoy B, Rocque W J, Holmes W, Montana V G, Piwnica-Worms H, Rink M J, Saper M A
Department of Biological Chemistry, The University of Michigan, Ann Arbor 48109-1055, USA.
Cell. 1998 May 15;93(4):617-25. doi: 10.1016/s0092-8674(00)81190-3.
Cdc25 phosphatases activate the cell division kinases throughout the cell cycle. The 2.3 A structure of the human Cdc25A catalytic domain reveals a small alpha/beta domain with a fold unlike previously described phosphatase structures but identical to rhodanese, a sulfur-transfer protein. Only the active-site loop, containing the Cys-(X)5-Arg motif, shows similarity to the tyrosine phosphatases. In some crystals, the catalytic Cys-430 forms a disulfide bond with the invariant Cys-384, suggesting that Cdc25 may be self-inhibited during oxidative stress. Asp-383, previously proposed to be the general acid, instead serves a structural role, forming a conserved buried salt-bridge. We propose that Glu-431 may act as a general acid. Structure-based alignments suggest that the noncatalytic domain of the MAP kinase phosphatases will share this topology, as will ACR2, a eukaryotic arsenical resistance protein.
Cdc25磷酸酶在整个细胞周期中激活细胞分裂激酶。人Cdc25A催化结构域的2.3埃结构揭示了一个小的α/β结构域,其折叠方式不同于先前描述的磷酸酶结构,但与硫转移蛋白硫氰酸酶相同。只有包含半胱氨酸-(X)5-精氨酸基序的活性位点环与酪氨酸磷酸酶相似。在一些晶体中,催化性半胱氨酸-430与不变的半胱氨酸-384形成二硫键,这表明Cdc25在氧化应激期间可能被自身抑制。先前被认为是广义酸的天冬氨酸-383,反而起到结构作用,形成一个保守的埋藏盐桥。我们认为谷氨酸-431可能作为广义酸起作用。基于结构的比对表明,MAP激酶磷酸酶的非催化结构域将共享这种拓扑结构,真核抗砷蛋白ACR2也将如此。