title: Solid phase synthesis of peptide aldehyde protease inhibitors. Probing the proteolytic sites of hepatitis C virus polyprotein.
abstract: The solid phase synthesis of a set of peptide aldehydes derived from the NS5A/NS5B junction of hepatitis C virus (HCV) viral polyprotein is demonstrated using an oxazolidine linker and the Multipin method. Deletion of the P6 and P5 residues results in a dramatic loss of inhibitory activity.
authors.affiliation: Chiron Technologies Pty. Ltd., Clayton, Victoria , Australia. nick_ede@cc.chiron.com
authors.forename: N J
authors.initials: NJ
authors.lastname: Ede
authors.forename: S N
authors.initials: SN
authors.lastname: Eagle
authors.forename: G
authors.initials: G
authors.lastname: Wickham
authors.forename: A M
authors.initials: AM
authors.lastname: Bray
authors.forename: B
authors.initials: B
authors.lastname: Warne
authors.forename: K
authors.initials: K
authors.lastname: Shoemaker
authors.forename: S
authors.initials: S
authors.lastname: Rosenberg
mesh_terms: D000447:Aldehydes / Q000138:chemical synthesis*; D010450:Endopeptidases / Q000378:metabolism; D016174:Hepacivirus / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008956:Models, Chemical; D010455:Peptides / Q000138:chemical synthesis*; D020815:Polyproteins / Q000737:chemistry*; D011480:Protease Inhibitors / Q000138:chemical synthesis*; D013053:Spectrophotometry; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases; D012324:RNA-Dependent RNA Polymerase
chemical_list: D000447:Aldehydes; D010450:Endopeptidases; D010455:Peptides; D020815:Polyproteins; D011480:Protease Inhibitors; D017361:Viral Nonstructural Proteins; C084422:NS3 protein, hepatitis C virus; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases; C087036:NS-5 protein, hepatitis C virus; D012324:RNA-Dependent RNA Polymerase