Van Laer Koen, Oliveira Margarida, Wahni Khadija, Messens Joris
VIB Department of Structural Biology, Brussels, Belgium; Structural Biology Brussels, Vrije Universiteit Brussel, Brussels, Belgium; Brussels Center for Redox Biology, Brussels, Belgium.
Protein Sci. 2014 Feb;23(2):238-42. doi: 10.1002/pro.2397. Epub 2013 Dec 13.
NrdH-redoxins shuffle electrons from the NADPH pool in the cell to Class Ib ribonucleotide reductases, which in turn provide the precursors for DNA replication and repair. NrdH-redoxins have a CVQC active site motif and belong to the thioredoxin-fold protein family. As for other thioredoxin-fold proteins, the pK(a) of the nucleophilic cysteine of NrdH-redoxins is of particular interest since it affects the catalytic reaction rate of the enzymes. Recently, the pK(a) value of this cysteine in Corynebacterium glutamicum and Mycobacterium tuberculosis NrdH-redoxins were determined, but structural insights explaining the relatively low pK(a) remained elusive. We subjected C. glutamicum NrdH-redoxin to an extensive molecular dynamics simulation to expose the factors regulating the pK(a) of the nucleophilic cysteine. We found that the nucleophilic cysteine receives three hydrogen bonds from residues within the CVQC active site motif. Additionally, a fourth hydrogen bond with a lysine located N-terminal of the active site further lowers the cysteine pK(a). However, site-directed mutagenesis data show that the major contribution to the lowering of the cysteine pK(a) comes from the positive charge of the lysine and not from the additional Lys-Cys hydrogen bond. In 12% of the NrdH-redoxin family, this lysine is replaced by an arginine that also lowers the cysteine pK(a). All together, the four hydrogen bonds and the electrostatic effect of a lysine or an arginine located N-terminally of the active site dynamically regulate the pK(a) of the nucleophilic cysteine in NrdH-redoxins.
NrdH-氧化还原蛋白将细胞中烟酰胺腺嘌呤二核苷酸磷酸(NADPH)池中的电子转移至Ib类核糖核苷酸还原酶,而后者又为DNA复制和修复提供前体。NrdH-氧化还原蛋白具有CVQC活性位点基序,属于硫氧还蛋白折叠蛋白家族。与其他硫氧还蛋白折叠蛋白一样,NrdH-氧化还原蛋白亲核半胱氨酸的pK(a)特别受关注,因为它会影响酶的催化反应速率。最近,已测定了谷氨酸棒杆菌和结核分枝杆菌NrdH-氧化还原蛋白中该半胱氨酸的pK(a)值,但解释该pK(a)相对较低的结构见解仍不明确。我们对谷氨酸棒杆菌NrdH-氧化还原蛋白进行了广泛的分子动力学模拟,以揭示调节亲核半胱氨酸pK(a)的因素。我们发现亲核半胱氨酸从CVQC活性位点基序内的残基接受三个氢键。此外,与活性位点N端的赖氨酸形成的第四个氢键进一步降低了半胱氨酸的pK(a)。然而,定点诱变数据表明,半胱氨酸pK(a)降低的主要贡献来自赖氨酸的正电荷,而非额外的赖氨酸-半胱氨酸氢键。在12%的NrdH-氧化还原蛋白家族中,该赖氨酸被精氨酸取代,后者也会降低半胱氨酸的pK(a)。总之,四个氢键以及活性位点N端赖氨酸或精氨酸的静电效应动态调节NrdH-氧化还原蛋白中亲核半胱氨酸的pK(a)。