Zhao Kehao, Chai Xiaomei, Marmorstein Ronen
The Wistar Institute, University of Pennsylvania, Philadelphia, PA 19104, USA.
J Mol Biol. 2004 Mar 26;337(3):731-41. doi: 10.1016/j.jmb.2004.01.060.
Sirtuins are NAD+-dependent protein deacetylase enzymes that are broadly conserved from bacteria to human, and have been implicated to play important roles in gene regulation, metabolism and longevity. cobB is a bacterial sirtuin that deacetylates acetyl-CoA synthetase (Acs) at an active site lysine to stimulate its enzymatic activity. Here, we report the structure of cobB bound to an acetyl-lysine containing non-cognate histone H4 substrate. A comparison with the previously reported archaeal and eukaryotic sirtuin structures reveals the greatest variability in a small zinc-binding domain implicated to play a particularly important role in substrate-specific binding by the sirtuin proteins. Comparison of the cobB/histone H4 complex with other sirtuin proteins in complex with acetyl-lysine containing substrates, further suggests that contacts to the acetyl-lysine side-chain and beta-sheet interactions with residues directly C-terminal to the acetyl-lysine represent conserved features of sirtuin-substrate recognition. Isothermal titration calorimetry studies were used to compare the affinity of cobB for a variety of cognate and non-cognate acetyl-lysine-bearing peptides revealing an exothermic reaction with relatively little discrimination between substrates. In contrast, similar studies employing intact acetylated Acs protein as a substrate reveal a binding reaction that is endothermic, suggesting that cobB recognition of substrate involves a burial of hydrophobic surface and/or structural rearrangement involving substrate regions distal to the acetyl-lysine-binding site. Together, these studies suggest that substrate-specific binding by sirtuin proteins involves contributions from the zinc-binding domain of the enzyme and substrate regions distal to the acetyl-lysine-binding site.
沉默调节蛋白是一类依赖烟酰胺腺嘌呤二核苷酸(NAD+)的蛋白质脱乙酰酶,从细菌到人类广泛保守,并且在基因调控、新陈代谢和寿命方面发挥重要作用。cobB是一种细菌沉默调节蛋白,它在活性位点赖氨酸处使乙酰辅酶A合成酶(Acs)脱乙酰化,以刺激其酶活性。在此,我们报道了cobB与含乙酰赖氨酸的非同源组蛋白H4底物结合的结构。与先前报道的古细菌和真核生物沉默调节蛋白结构进行比较,发现在一个小的锌结合结构域中存在最大的变异性,该结构域被认为在沉默调节蛋白与底物特异性结合中起特别重要的作用。将cobB/组蛋白H4复合物与其他与含乙酰赖氨酸底物结合的沉默调节蛋白进行比较,进一步表明与乙酰赖氨酸侧链的接触以及与乙酰赖氨酸直接C端残基的β折叠相互作用代表了沉默调节蛋白-底物识别的保守特征。等温滴定量热法研究用于比较cobB对多种同源和非同源含乙酰赖氨酸肽的亲和力,结果显示出放热反应,对底物的区分相对较小。相比之下,使用完整的乙酰化Acs蛋白作为底物的类似研究揭示了一个吸热的结合反应,这表明cobB对底物的识别涉及疏水表面的埋藏和/或涉及乙酰赖氨酸结合位点远端底物区域的结构重排。总之,这些研究表明沉默调节蛋白与底物的特异性结合涉及酶的锌结合结构域和乙酰赖氨酸结合位点远端底物区域的作用。