Silva Rafael G, de Carvalho Luiz Pedro S, Blanchard John S, Santos Diógenes S, Basso Luiz A
Centro de Pesquisas em Biologia Molecular e Funcional, Faculdade de Biociências e Faculdade de Farmacia, Instituto de Pesquisas Biomédicas, PUCRS, 6681/92-A Avenida Ipiranga, 90619-900, Porto Alegre, RS, Brazil.
Biochemistry. 2006 Oct 31;45(43):13064-73. doi: 10.1021/bi0611210.
Beta-ketoacyl-acyl carrier protein (ACP) reductase from Mycobacterium tuberculosis (MabA) is responsible for the second step of the type-II fatty acid elongation system of bacteria, plants, and apicomplexan organisms, catalyzing the NADPH-dependent reduction of beta-ketoacyl-ACP to generate beta-hydroxyacyl-ACP and NADP(+). In the present work, the mabA-encoded MabA has been cloned, expressed, and purified to homogeneity. Initial velocity studies, product inhibition, and primary deuterium kinetic isotope effects suggested a steady-state random bi-bi kinetic mechanism for the MabA-catalyzed reaction. The magnitudes of the primary deuterium kinetic isotope effect indicated that the C(4)-proS hydrogen is transferred from the pyridine nucleotide and that this transfer contributes modestly to the rate-limiting step of the reaction. The pH-rate profiles demonstrated groups with pK values of 6.9 and 8.0, important for binding of NADPH, and with pK values of 8.8 and 9.6, important for binding of AcAcCoA and for catalysis, respectively. Temperature studies were employed to determine the activation energy of the reaction. Solvent kinetic isotope effects and proton inventory analysis established that a single proton is transferred in a partially rate-limiting step and that the mechanism of carbonyl reduction is probably concerted. The observation of an inverse (D)2(O)V/K and an increase in (D)2(O)V when [4S-(2)H]NADPH was the varied substrate obscured the distinction between stepwise and concerted mechanisms; however, the latter was further supported by the pH dependence of the primary deuterium kinetic isotope effect. Kinetic and chemical mechanisms for the MabA-catalyzed reaction are proposed on the basis of the experimental data.
结核分枝杆菌的β-酮脂酰-酰基载体蛋白(ACP)还原酶(MabA)负责细菌、植物和顶复门生物II型脂肪酸延长系统的第二步,催化β-酮脂酰-ACP的NADPH依赖性还原,生成β-羟基脂酰-ACP和NADP(+)。在本研究中,编码MabA的mabA已被克隆、表达并纯化至同质。初始速度研究、产物抑制和初级氘动力学同位素效应表明,MabA催化反应的稳态随机双底物双产物动力学机制。初级氘动力学同位素效应的大小表明,C(4)-proS氢从吡啶核苷酸转移,且这种转移对反应的限速步骤贡献不大。pH速率曲线显示,pK值为6.9和8.0的基团对NADPH的结合很重要,pK值为8.8和9.6的基团分别对乙酰乙酰辅酶A的结合和催化很重要。采用温度研究来确定反应的活化能。溶剂动力学同位素效应和质子存量分析确定,在一个部分限速步骤中转移了一个质子,羰基还原机制可能是协同的。当[4S-(2)H]NADPH为可变底物时,观察到反向的(D)2(O)V/K和(D)2(O)V的增加,这模糊了逐步和协同机制之间的区别;然而,后者得到了初级氘动力学同位素效应的pH依赖性的进一步支持。基于实验数据,提出了MabA催化反应的动力学和化学机制。