Department of Biochemistry and Biophysics, University of California San Francisco, San Francisco, CA, USA.
Chemistry and Chemical Biology Graduate Program, University of California San Francisco, San Francisco, CA, USA.
Nat Struct Mol Biol. 2023 Mar;30(3):296-308. doi: 10.1038/s41594-022-00918-0. Epub 2023 Feb 13.
The mycolic acid layer of the Mycobacterium tuberculosis cell wall is essential for viability and virulence, and the enzymes responsible for its synthesis are targets for antimycobacterial drug development. Polyketide synthase 13 (Pks13) is a module encoding several enzymatic and transport functions that carries out the condensation of two different long-chain fatty acids to produce mycolic acids. We determined structures by cryogenic-electron microscopy of dimeric multi-enzyme Pks13 purified from mycobacteria under normal growth conditions, captured with native substrates. Structures define the ketosynthase (KS), linker and acyl transferase (AT) domains at 1.8 Å resolution and two alternative locations of the N-terminal acyl carrier protein. These structures suggest intermediate states on the pathway for substrate delivery to the KS domain. Other domains, visible at lower resolution, are flexible relative to the KS-AT core. The chemical structures of three bound endogenous long-chain fatty acid substrates were determined by electrospray ionization mass spectrometry.
结核分枝杆菌细胞壁中的类脂酸层对于其生存力和毒力至关重要,而负责其合成的酶则是抗分枝杆菌药物开发的靶点。聚酮合酶 13(Pks13)是一个编码多种酶和转运功能的模块,它通过两个不同的长链脂肪酸的缩合来产生类脂酸。我们通过低温电子显微镜技术确定了在正常生长条件下从分枝杆菌中纯化的二聚体多酶 Pks13 的结构,该结构与天然底物结合。结构以 1.8Å 的分辨率定义了酮合酶(KS)、连接酶和酰基转移酶(AT)结构域,以及 N 端酰基载体蛋白的两个替代位置。这些结构表明了底物向 KS 结构域传递的途径中的中间状态。其他在较低分辨率下可见的结构域相对于 KS-AT 核心是灵活的。通过电喷雾电离质谱法确定了三个结合的内源性长链脂肪酸底物的化学结构。