Compounds For Enzyme Inhibition

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United States of America Patent

SERIAL NO

13341022

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Abstract

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Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

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Patent Owner(s)

Patent OwnerAddress
ONYX THERAPEUTICS INC2100 POWELL STREET C/O ONYX PHARMAECUTICALS INC EMERYVILLE CA 94608

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Borchardt, Ronald T Lawrence, US 12 443
Bunin, Barry A San Mateo, US 20 434
Crews, Craig M New Haven, US 73 2174
Laidig, Guy J Menlo Park, US 51 1416
Musser, John H San Carlos, US 110 2903
Radel, Peggy A Berkeley, US 7 218
Shenk, Kevin D Palo Alto, US 26 700
Smyth, Mark S Foster City, US 75 1296

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