John Tobias, Saffoon Nadia, Walsby-Tickle John, Hester Svenja S, Dingler Felix A, Millington Christopher L, McCullagh James S O, Patel Ketan J, Hopkinson Richard J, Schofield Christopher J
Chemistry Research Laboratory, Department of Chemistry and the Ineos Oxford Institute for Antimicrobial Research, University of Oxford 12 Mansfield Road Oxford OX1 3TA UK
Nuffield Department of Medicine, Target Discovery Institute, University of Oxford Oxford UK.
Chem Sci. 2024 Jan 15;15(7):2509-2517. doi: 10.1039/d3sc06551k. eCollection 2024 Feb 14.
Patients with alcoholism and type 2 diabetes manifest altered metabolism, including elevated aldehyde levels and unusually low asparagine levels. We show that asparagine synthetase B (ASNS), the only human asparagine-forming enzyme, is inhibited by disease-relevant reactive aldehydes, including formaldehyde and acetaldehyde. Cellular studies show non-cytotoxic amounts of reactive aldehydes induce a decrease in asparagine levels. Biochemical analyses reveal inhibition results from reaction of the aldehydes with the catalytically important N-terminal cysteine of ASNS. The combined cellular and biochemical results suggest a possible mechanism underlying the low asparagine levels in alcoholism and diabetes. The results will stimulate research on the biological consequences of the reactions of aldehydes with nucleophilic residues.
酗酒和2型糖尿病患者表现出代谢改变,包括醛水平升高和天冬酰胺水平异常低。我们发现,天冬酰胺合成酶B(ASNS)是人类唯一的天冬酰胺形成酶,它会受到与疾病相关的活性醛类(包括甲醛和乙醛)的抑制。细胞研究表明,非细胞毒性剂量的活性醛会导致天冬酰胺水平下降。生化分析显示,抑制作用源于醛与ASNS催化重要的N端半胱氨酸的反应。细胞和生化研究结果共同提示了酗酒和糖尿病中天冬酰胺水平低的潜在机制。这些结果将激发对醛与亲核残基反应的生物学后果的研究。