Selected article for: "active site and protease activity"
Author: Sun, Di; Chen, Shun; Cheng, Anchun; Wang, Mingshu
Title: Roles of the Picornaviral 3C Proteinase in the Viral Life Cycle and Host Cells
  • Document date: 2016_3_17
    • ID: 07nfb69o_53
    Snippet: Peptidyl Michael acceptors have been used to develop 3C pro inactivators for inhibiting viral replication [127] [128] [129] . As a potent irreversible inhibitor of HRV 3C pro , AG7088 contains an α,β-unsaturated ester at P1 1 that serves as a Michael acceptor, a lactam ring at P1, a fluoro-phenylalanine at P2, a Val at P3 and a 5-methyl-3-isoxazole. AG7088 binds with the active site Cys residue to influence the functionality of 3C pro [130] . T.....
    Document: Peptidyl Michael acceptors have been used to develop 3C pro inactivators for inhibiting viral replication [127] [128] [129] . As a potent irreversible inhibitor of HRV 3C pro , AG7088 contains an α,β-unsaturated ester at P1 1 that serves as a Michael acceptor, a lactam ring at P1, a fluoro-phenylalanine at P2, a Val at P3 and a 5-methyl-3-isoxazole. AG7088 binds with the active site Cys residue to influence the functionality of 3C pro [130] . Through a series of cell-based protease assays, the activity spectra of the 3C pro inhibitors AG7088 and SG85 have been found to include inhibition of CVB3, EV71, PV, and HRV14 3C pro s. However, these inhibitors have no effect on the 3C pro of EMCV [131, 132] . The inhibition of HAV replication by AG7088 is strain-dependent [133] . As an analogue of AG7088, AG7404 has been demonstrated to inhibit HRV, PV and several EV types [134] .

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