Composition and method for HIP1-targeting inhibitor compounds
AssigneeUtah Valley University
InventorsNathan E. Goldfarb, Andrew Abell, Nicholas Schumann, Borja Lopez Perez
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Abstract
Provided herein is an inhibitor compound targeting Hip1, with the inhibitor compound comprising a tripeptide targeting sequence that directs the compound to the active site of Hip1 and a C-terminal electrophilic warhead conjugated to the targeting sequence, the warhead configured to inactive the enzyme.
Claims20
A compound for the inhibition of a Hydrolase important for pathogenesis (Hip1) enzyme, the compound comprising:
- a tripeptide targeting sequence, that directs the compound to the active site of Hip1, the tripeptide targeting sequence comprising the sequence Phe-Lys-Leu in the N-terminal to C-terminal direction;
- and
- a C-terminal group conjugated to the Leu of the targeting sequence, the C-terminal group comprising
- (i) an alpha-keto methyl ester electrophilic warhead configured to inactivate the Hip1 enzyme, or
- (ii) a chromophore or fluorophore reporter group.
A compound for the inhibition of a Hydrolase important for pathogenesis (Hip1) enzyme, the compound comprising:
- a tripeptide comprising the sequence Phe-Lys-Leu in the N-terminal to C-terminal direction;
- and
- a C-terminal group conjugated to the Leu of the tripeptide, the C-terminal group comprising
- (i) an alpha-keto methyl ester, or
- (ii) a reporter group.
A compound for the inhibition of a Hydrolase important for pathogenesis (Hip1) enzyme, the compound comprising:
- a tripeptide comprising the sequence Phe-Lys-Leu in the N-terminal to C-terminal direction;
- and
- a C-terminal group conjugated to the Leu of the tripeptide, the C-terminal group comprising
- (i) an alpha-keto methyl ester, and the compound comprising the structure:
- or
- (ii) a paranitroanilide (pNa) reporter group, and the compound comprising the structure:
Dependencies are inferred from the claim text.