title: Selective inhibition of the chymotrypsin-like activity of the 20S proteasome by 5-methoxy-1-indanone dipeptide benzamides.
abstract: Potent inhibitors of the 20S proteasome that contain a novel indanone head group coupled to di and tripeptides are described. These compounds are the first proteasome inhibitors have demonstrated high selectivity for the chymotrypsin-like activity of the 20S proteasome.
authors.affiliation: CV Therapeutics Inc. Palo Alto, CA 94304, USA.
authors.forename: R T
authors.initials: RT
authors.lastname: Lum
authors.forename: M G
authors.initials: MG
authors.lastname: Nelson
authors.forename: A
authors.initials: A
authors.lastname: Joly
authors.forename: A G
authors.initials: AG
authors.lastname: Horsma
authors.forename: G
authors.initials: G
authors.lastname: Lee
authors.forename: S M
authors.initials: SM
authors.lastname: Meyer
authors.forename: M M
authors.initials: MM
authors.lastname: Wick
authors.forename: S R
authors.initials: SR
authors.lastname: Schow
mesh_terms: D001549:Benzamides / Q000737:chemistry / Q000494:pharmacology*; D002918:Chymotrypsin / Q000037:antagonists & inhibitors*; D003546:Cysteine Endopeptidases / Q000187:drug effects*; D015394:Molecular Structure; D009097:Multienzyme Complexes / Q000187:drug effects*; D046988:Proteasome Endopeptidase Complex; D013237:Stereoisomerism; D014361:Trypsin Inhibitors / Q000494:pharmacology*
chemical_list: D001549:Benzamides; D009097:Multienzyme Complexes; D014361:Trypsin Inhibitors; D002918:Chymotrypsin; D003546:Cysteine Endopeptidases; D046988:Proteasome Endopeptidase Complex