Non-covalent inhibitors of rhinovirus 3C protease

Andrew Baxter; Mark Chambers; Fredrik Edfeldt; Karl Edman; Adrian Freeman; Cristian Johansson; Sarah King; Andy Morley; Jens Petersen; Phil Rawlins; Loredana Spadola; Bob Thong; Hervé Van de Poël; Nicola Williams

doi:10.1016/j.bmcl.2010.11.110

Non-covalent inhibitors of rhinovirus 3C protease

Bioorg Med Chem Lett. 2011 Jan 15;21(2):777-80. doi: 10.1016/j.bmcl.2010.11.110. Epub 2010 Nov 26.

Authors

Andrew Baxter¹, Mark Chambers, Fredrik Edfeldt, Karl Edman, Adrian Freeman, Cristian Johansson, Sarah King, Andy Morley, Jens Petersen, Phil Rawlins, Loredana Spadola, Bob Thong, Hervé Van de Poël, Nicola Williams

Affiliation

¹ AstraZeneca, R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK.

PMID: 21183345
DOI: 10.1016/j.bmcl.2010.11.110

Abstract

The first known non-covalent inhibitors of rhinovirus 3C protease (3CP) have been identified through fragment based screening and hit identification activities.

MeSH terms

3C Viral Proteases
Antiviral Agents / chemistry
Antiviral Agents / pharmacology
Common Cold / drug therapy
Common Cold / virology
Cysteine Endopeptidases / metabolism*
Cysteine Proteinase Inhibitors / chemistry*
Cysteine Proteinase Inhibitors / pharmacology*
Drug Design
Humans
Models, Molecular
Picornaviridae Infections / drug therapy
Picornaviridae Infections / virology
Rhinovirus / enzymology*
Structure-Activity Relationship
Viral Proteins / antagonists & inhibitors*
Viral Proteins / metabolism*

Substances

Antiviral Agents
Cysteine Proteinase Inhibitors
Viral Proteins
Cysteine Endopeptidases
3C Viral Proteases