Department of Pharmacology and Chemical Biology, State Key Laboratory of Systems Medicine for Cancer, Shanghai Jiao Tong University School of Medicine, Shanghai, 200025, China.
School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou, 310024, China.
Angew Chem Int Ed Engl. 2023 Nov 13;62(46):e202313109. doi: 10.1002/anie.202313109. Epub 2023 Oct 12.
The short-chain dehydrogenase/reductase (SDR) superfamily members acyl-ACP reductases FabG and FabI are indispensable core enzymatic modules and catalytic orientation controllers in type-II fatty acid biosynthesis. Herein, we report their distinct substrate allosteric recognition and enantioselective reduction mechanisms. FabG achieves allosteric regulation of ACP and NADPH through ACP binding across two adjacent FabG monomers, while FabI follows an irreversible compulsory order of substrate binding in that NADH binding must precede that of ACP on a discrete FabI monomer. Moreover, FabG and FabI utilize a backdoor residue Phe187 or a "rheostat" α8 helix for acyl chain length selection, and their corresponding triad residues Ser142 or Tyr145 recognize the keto- or enoyl-acyl substrates, respectively, facilitating initiation of nucleophilic attack by NAD(P)H. The other two triad residues (Tyr and Lys) mediate subsequent proton transfer and (R)-3-hydroxyacyl- or saturated acyl-ACP production.
短链脱氢酶/还原酶 (SDR) 超家族成员酰基辅酶 A 还原酶 FabG 和 FabI 是 II 型脂肪酸生物合成中不可或缺的核心酶模块和催化定向控制器。本文报道了它们独特的底物别构识别和对映选择性还原机制。FabG 通过 ACP 在两个相邻 FabG 单体上的结合来实现 ACP 和 NADPH 的别构调节,而 FabI 遵循不可逆的底物结合强制性顺序,即 NADH 的结合必须先于 ACP 在离散的 FabI 单体上的结合。此外,FabG 和 FabI 利用后门残基 Phe187 或“变阻器”α8 螺旋来选择酰基链长度,其相应的三联体残基 Ser142 或 Tyr145 分别识别酮基或烯酰基酰基底物,从而促进 NAD(P)H 的亲核攻击的起始。另外两个三联体残基(Tyr 和 Lys)介导后续的质子转移和(R)-3-羟基酰基或饱和酰基-ACP 的生成。