Selective inhibition of the chymotrypsin-like activity of the 20S proteasome by 5-methoxy-1-indanone dipeptide benzamides.
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.
Lum
R T
RT
CV Therapeutics Inc. Palo Alto, CA 94304, USA.
Nelson
M G
MG
Joly
A
A
Horsma
A G
AG
Lee
G
G
Meyer
S M
SM
Wick
M M
MM
Schow
S R
SR
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*
D001549:Benzamides; D009097:Multienzyme Complexes; D014361:Trypsin Inhibitors; D002918:Chymotrypsin; D003546:Cysteine Endopeptidases; D046988:Proteasome Endopeptidase Complex