Screening of antiviral agents that avoid drug resistance by inhibiting virus-specific replication processes

2020 Fiscal Year Final Research Report

• Project/Area Number: 17K08375
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Nihon University
• Principal Investigator: HAKAMATA Wataru 日本大学, 生物資源科学部, 准教授 (10333337)
• Co-Investigator(Kenkyū-buntansha): 氏家 誠 日本獣医生命科学大学, 獣医学部, 准教授 (50415478)
• Project Period (FY): 2017-04-01 – 2021-03-31
• Keywords: 抗ウイルス薬 / ウイルス糖タンパク質 / 糖鎖 / 阻害剤

Outline of Final Research Achievements

The development of antiviral drugs for emerging and re-emerging viral infections has been greatly delayed. In this study, we aim to identify and develop antiviral drugs that target the virus-specific replication process by host enzymes to avoid the emergence of drug-resistant viruses. We focused on the fact that inhibition of glycan synthesis of viral coat proteins significantly reduces viral infectivity and that glycan synthesis inhibits the maturation of viral particles. We synthesized a fluorescent substrate specific for the glycosidase that works in cultured cells, which will enable us to screen for potential inhibitors of antiviral drugs from a compound library.

Free Research Field

創薬化学

Academic Significance and Societal Importance of the Research Achievements

新興・再興ウイルス感染症に対する抗ウイルス薬の開発は大きく遅れている。抗ウイルス薬はウイルス因子を直接標的とする直接作用抗ウイルス薬（Direct-acting antivirals, DAAs）と宿主因子を標的とする抗ウイルス薬（Host-targeting antivirals, HTAs）に大別される。HTAs は薬剤耐性ウイルスおよび将来的に出現が見込まれる未知のウイルスに効果が期待できる。本研究では HTAs をターゲットとして、社会的要請の高い抗ウイルス薬に関する研究を行った。