Selected article for: "cell culture and human rhinovirus"
Author: Linlin Zhang; Daizong Lin; Yuri Kusov; Yong Nian; Qingjun Ma; Jiang Wang; Albrecht von Brunn; Pieter Leyssen; Kristina Lanko; Johan Neyts; Adriaan de Wilde; Eric J. Snijder; Hong Liu; Rolf Hilgenfeld
Title: Alpha-ketoamides as broad-spectrum inhibitors of coronavirus and enterovirus replication
  • Document date: 2020_2_10
    • ID: 7n8p9okf_41
    Snippet: Occasionally, individual a-ketoamides have been reported in the literature as inhibitors of both the enterovirus 3C protease and the coronavirus main protease. A single capped dipeptidyl a-ketoamide, Cbz-Leu-GlnLactam-CO-CO-NH-iPr, was described that inhibited the recombinant transmissible gastroenteritis virus (TGEV) and SARS-CoV M pro s as well as human rhinovirus and poliovirus 3C pro s in the one-digit micromolar range. 44 Coded GC-375, this .....
    Document: Occasionally, individual a-ketoamides have been reported in the literature as inhibitors of both the enterovirus 3C protease and the coronavirus main protease. A single capped dipeptidyl a-ketoamide, Cbz-Leu-GlnLactam-CO-CO-NH-iPr, was described that inhibited the recombinant transmissible gastroenteritis virus (TGEV) and SARS-CoV M pro s as well as human rhinovirus and poliovirus 3C pro s in the one-digit micromolar range. 44 Coded GC-375, this compound showed poor activity in cell culture against EV-A71 though (EC50 = 15.2 µM), probably because P2 was isobutyl. As we have shown here, an isobutyl side-chain in the P2 position of the inhibitors is too small to completely fill the S2 pocket of the EV-A71 3C pro and the CVB3 3C pro .

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