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US 11,530,235 B2Granted
Compounds and methods used in assessing mono-PARP activity
AssigneeOregon Health & Science University
InventorsMichael Cohen, Ian Carter-O'Connell, Rory Morgan, Haihong Jin
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Abstract
Mutant mono ADP-ribose-polymerases (mono-PARP) proteins and small molecule compound substrates specific for the mutant mono-PARP proteins as well as methods of using these compositions to identify protein targets of the mono-PARPs and to screen for antagonists of the mono-PARPs are described.
Claims10
A method of identifying a protein target of a mono-PARP, the method comprising:
- contacting a small molecule compound (SMC) of formula:
- wherein R is alkyl or aryl, with a protein, said protein comprising a polypeptide comprising a mono-poly-ADP-ribose-polymerases (PARP) catalytic domain comprising SEQ ID NO:
- 15, and wherein the polypeptide catalyzes the addition of the SMC to a PARP protein target, wherein said contacting occurs within a living cell;
- subjecting the cell to conditions that result in the protein catalyzing the reaction by which the SMC is covalently attached to one or more cellular proteins;
- and identifying the one or more cellular proteins to which the SMC is covalently attached as the protein target(s) of the mono-PARP.
2 more elements
Dependencies are inferred from the claim text.