Research School of Chemistry, Australian National University, Canberra, ACT 2601, Australia.
Research School of Chemistry, Australian National University, Canberra, ACT 2601, Australia.
Bioorg Med Chem Lett. 2020 Mar 1;30(5):126965. doi: 10.1016/j.bmcl.2020.126965. Epub 2020 Jan 11.
In recent years, the Zika virus has emerged from a neglected flavivirus to a health-threatening pathogen that causes epidemic outbreaks associated with neurological disorders and congenital malformations. In addition to vaccine development, the discovery of specific antiviral agents has been pursued intensely. The Zika virus protease NS2B-NS3 catalyses the processing of the viral precursor polyprotein as an essential step during viral replication. Since the epidemic Zika virus outbreak in the Americas, several inhibitors of this protease have been reported. Substrate-derived peptides revealed important structural information about the active site, whilst more drug-like small molecules have been discovered as allosteric inhibitors.
近年来，寨卡病毒已从一种被忽视的黄病毒演变为一种威胁健康的病原体，可引起与神经紊乱和先天畸形相关的流行疫情暴发。除疫苗开发外，人们还在积极探索特异性抗病毒药物。寨卡病毒蛋白酶 NS2B-NS3 作为病毒复制过程中的一个关键步骤，可催化病毒前体多蛋白的加工。自美洲发生寨卡病毒疫情以来，已有多种该蛋白酶抑制剂被报道。底物衍生肽揭示了有关活性位点的重要结构信息，而作为变构抑制剂的更多类药性小分子也被发现。
