Podust Larissa M, Ioanoviciu Alexandra, Ortiz de Montellano Paul R
Department of Pharmaceutical Chemistry, University of California, 600 16th Street, San Francisco, California 94158-2517, USA.
Biochemistry. 2008 Nov 25;47(47):12523-31. doi: 10.1021/bi8012356.
Mycobacterium tuberculosis responds to changes in environmental conditions through a two-component signaling system that detects reduced O(2) tension and NO and CO exposures via the heme-binding GAF domains of two sensory histidine kinases, DosT and DevS, and the transcriptional regulator DosR. We report the first X-ray structure of the DosT heme-bound GAF domain (GAF(DosT)) in both oxy and deoxy forms determined to a resolution of 2.3 A. In GAF(DosT), heme binds in an orientation orthogonal to that in the PAS domains via a highly conserved motif, including invariant H147 as a proximal heme axial ligand. On the distal side, invariant Y169 forms stacking interactions with the heme with its long axis parallel and the plane of the ring orthogonal to the heme plane. In one of the two protein monomers in an asymmetric unit, O(2) binds as a second axial ligand to the heme iron and is stabilized via a H-bond to the OH group of Y169. The structure reveals two small tunnel-connected cavities and a pore on the protein surface that suggest a potential route for the access of O(2) to the sensing pocket. The limited conformational differences observed between differently heme iron-ligated GAF(DosT) monomers in the asymmetric unit may result from crystal lattice limitations since atmospheric oxygen binding likely occurs in the crystal as a result of X-ray-induced Fe(3+) photoreduction during diffraction data collection. Determination of the GAF(DosT) structure sets up a framework in which to address ligand recognition, discrimination, and signal propagation schemes in the heme-based GAF domains of biological sensors.
结核分枝杆菌通过双组分信号系统对环境条件的变化作出反应,该系统通过两个传感组氨酸激酶DosT和DevS以及转录调节因子DosR的血红素结合GAF结构域检测降低的氧张力以及一氧化氮和一氧化碳暴露。我们报告了DosT血红素结合GAF结构域(GAF(DosT))在氧合和脱氧形式下的首个X射线结构,分辨率达到2.3埃。在GAF(DosT)中,血红素通过一个高度保守的基序以与PAS结构域中正交的方向结合,该基序包括不变的H147作为近端血红素轴向配体。在远端,不变的Y169与血红素形成堆积相互作用,其长轴平行且环平面与血红素平面正交。在不对称单元中的两个蛋白质单体之一中,O₂作为第二个轴向配体与血红素铁结合,并通过与Y169的OH基团形成氢键而稳定。该结构揭示了两个由小隧道连接的腔以及蛋白质表面的一个孔,这表明O₂进入传感口袋的潜在途径。在不对称单元中不同血红素铁配位的GAF(DosT)单体之间观察到的有限构象差异可能是由于晶格限制,因为在衍射数据收集期间X射线诱导的Fe(3+)光还原可能导致晶体中大气氧的结合。GAF(DosT)结构的确定建立了一个框架,用于解决生物传感器基于血红素的GAF结构域中的配体识别、区分和信号传播机制。