Identification of a potent and rapidly reversible inhibitor of the 20S-proteasome.
Synthesis and in vitro characterization of novel, lactam boronic acid based, selective, and rapidly reversible inhibitor 14 of the 20S-proteasome is presented.
Purandare
Ashok V
AV
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA. ashok.purandare@bms.com
Wan
Honghe
H
Laing
Naomi
N
Benbatoul
Khalid
K
Vaccaro
Wayne
W
Poss
Michael A
MA
D001897:Boronic Acids / Q000138:chemical synthesis* / Q000737:chemistry; D000069286:Bortezomib; D006801:Humans; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D046988:Proteasome Endopeptidase Complex / Q000737:chemistry; D061988:Proteasome Inhibitors; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D001897:Boronic Acids; D011480:Protease Inhibitors; D061988:Proteasome Inhibitors; D011719:Pyrazines; D000069286:Bortezomib; D046988:Proteasome Endopeptidase Complex