Inside Cover: Induced-Fit Binding of the Macrocyclic Noncovalent Inhibitor TMC435 to its HCV NS3/NS4A Protease Target (Angew. Chem. Int. Ed. 9/2010)

✍ Scribed by Maxwell D. Cummings; Jimmy Lindberg; Tse-I Lin; Herman de Kock; Oliver Lenz; Elisabet Lilja; Sara Felländer; Vera Baraznenok; Susanne Nyström; Magnus Nilsson; Lotta Vrang; Michael Edlund; Åsa Rosenquist; Bertil Samuelsson; Pierre Raboisson; Kenneth Simmen

• Book ID: 102728533
• Publisher: John Wiley and Sons
• Year: 2010
• Tongue: English
• Weight: 614 KB
• Volume: 49
• Category: Article
• ISSN: 0044-8249
• DOI: 10.1002/anie.201000389

✦ Synopsis

The anti-HCV activity … … of TMC435, currently in phase 2b clinical studies as an HCV therapeutic (HCV = hepatitis C virus), is based on inhibition of the NS3/4A protease of the virus. As M. D. Cummings and co-workers describe in their Communication on page 1652 ff., binding of TMC435 to the target enzyme involves an induced fit, leading to occupancy of an extended S2 subsite.