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US 8,796,229 B2Granted
Feedback prodrug
AssigneeUniversity of Georgia Research Foundation, Inc.
InventorsGeert-Jan Boons, Jun Guo
Life of this patent
Estimating the term…
Abstract
Compounds and methods for use in selectively inhibiting a lytic enzyme based on feedback inhibition are described. The conjugated compound serves as a substrate for a lytic enzyme. Cleavage of the conjugated compound by the lytic enzyme releases an inhibitor of the enzyme.
Claims8
A conjugated compound comprising:
- a first constituent comprising an enzymatic substrate comprising a mannoside;
- and
- a second constituent covalently linked to the first constituent, the second constituent comprising a mannosidase inhibitor selected from the group consisting of mannostatin A, mannostatin B, or a mannostatin A derivative wherein the methyl thioether group (—S—CH3) group of mannostatin A is replaced by a phenyl thioether group (—S—Ph), a methoxy group (—O—CH3) or a phenoxy group (—O—Ph);
- and
- wherein the covalent linkage between the first and second constituents can be enzymatically cleaved by a mannosidase to release the mannosidase inhibitor;
- and wherein the mannosidase inhibitor, when released from the conjugated compound, inhibits the activity of the mannosidase.
3 more elements
Dependencies are inferred from the claim text.