烟酰胺酶作为一种新的抗疟靶点。

Nicotinamidase as A Novel Antimalarial Target.

机构信息

Department of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA 23219, USA.

Institute for Structural Biology, Drug Discovery and Development, Virginia Commonwealth University, Richmond, VA 23219, USA.

出版信息

Biomolecules. 2022 Aug 12;12(8):1109. doi: 10.3390/biom12081109.

DOI:10.3390/biom12081109

PMID:36009002

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9405955/

Abstract

Inhibition of nicotinamidase could represent a potential antimalarial since parasites require nicotinic acid to successfully recycle nicotinamide to NAD, and importantly, humans lack this biosynthetic enzyme. Recently, mechanism-based inhibitors of nicotinamidase have been discovered. The most potent compound inhibits both recombinant nicotinamidase and parasites replication in infected human red blood cells (RBCs). These studies provide evidence for the importance of nicotinamide salvage through nicotinamidase as a central master player of NAD homeostasis in .

摘要

烟酰胺酶的抑制作用可能代表一种有潜力的抗疟药物，因为寄生虫需要烟酸来成功地将烟酰胺回收为 NAD，而重要的是，人类缺乏这种生物合成酶。最近，烟酰胺酶的基于机制的抑制剂已经被发现。最有效的化合物抑制重组烟酰胺酶和感染人类红细胞（RBC）中的寄生虫复制。这些研究为烟酰胺通过烟酰胺酶回收在 NAD 动态平衡中的中心主角色的重要性提供了证据。