Methods and compositions for irreversible enzyme inhibition
AssigneeTriterpenoid Therapeutics, Inc.
InventorsMichael B. SPORN, Xiaoli MENG
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Abstract
The present invention relates to compounds, methods, and compositions for irreversibly inhibiting protein targets, including Keap1 and/or LONP1 protease. In certain aspects, the present invention relates to conjugates and/or cross-linked conjugates comprising a protein or a protein complex and a bifunctional triterpenoid, such as 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-2-yl)-1H-imidazole (“CDDO-2P-Im”), 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-3-yl)-1H-imidazole (“CDDO-3P-Im”), or derivatives thereof.
Claims20
A method for irreversibly inhibiting the activity of a protein in a patient or in a biological sample comprising the step of administering to said patient or contacting said biological sample with 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-2-yl)-1H-imidazole (CDDO-2P-Im) or a pharmaceutically acceptable salt thereof or 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-3-yl)-1H-imidazole (CDDO-3P-Im) or a pharmaceutically acceptable salt thereof, wherein the activity of the protein is irreversibly inhibited by covalently modifying a nucleophilic amino acid residue contained therein.
Dependencies are inferred from the claim text.