Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.
Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases.
Adams
J
J
ProScript, Inc., Cambridge, MA 02139, USA.
Behnke
M
M
Chen
S
S
Cruickshank
A A
AA
Dick
L R
LR
Grenier
L
L
Klunder
J M
JM
Ma
Y T
YT
Plamondon
L
L
Stein
R L
RL
D001897:Boronic Acids / Q000737:chemistry / Q000494:pharmacology*; D003546:Cysteine Endopeptidases / Q000187:drug effects*; D015394:Molecular Structure; D009097:Multienzyme Complexes / Q000187:drug effects*; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D046988:Proteasome Endopeptidase Complex
D001897:Boronic Acids; D009097:Multienzyme Complexes; D011480:Protease Inhibitors; D003546:Cysteine Endopeptidases; D046988:Proteasome Endopeptidase Complex