Discovery of potent nucleotide-mimicking competitive inhibitors of hepatitis C virus NS3 helicase
作者:Sandra Gemma、Stefania Butini、Giuseppe Campiani、Margherita Brindisi、Samantha Zanoli、Maria Pia Romano、Pierangela Tripaldi、Luisa Savini、Isabella Fiorini、Giuseppe Borrelli、Ettore Novellino、Giovanni Maga
DOI:10.1016/j.bmcl.2010.09.002
日期:2011.5
Among the enzymes involved in the life cycle of HCV, the non-structural protein NS3, with its double function of protease and NTPase/helicase, is essential for the virus replication. Exploiting our previous knowledge in the development of nucleotide-mimicking NS3 helicase (NS3h) inhibitors endowed with key structural and electronic features necessary for an optimal ligand-enzyme interaction, we developed the tetrahydroacridinyl derivative 3a as the most potent NS3h competitive inhibitor reported to date (HCV NS3h K(i) = 20 nM). (C) 2010 Elsevier Ltd. All rights reserved.
Pellerano; Savini; Brizzi, Farmaco, Edizione Scientifica, 1985, vol. 40, # 7, p. 486 - 492
作者:Pellerano、Savini、Brizzi
DOI:——
日期:——
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