Potent and specific immunoproteasome inhibitors
First Claim
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1. A compound having a 10-fold or greater preference for inhibiting an immunoproteasome as compared to a constitutive proteasome, said compound having a structure of Formula (I):
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Abstract
Compounds and methods of selectively inhibiting an immunoproteasome are described. Also described are methods of treating a cancer, an inflammation, and/or an autoimmune disease and methods of suppressing endogenous antigenic peptide generation by administering to a subject in need of treatment thereof a therapeutic amount of an immunoproteasome specific inhibitor.
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Citations
71 Claims
- 1. A compound having a 10-fold or greater preference for inhibiting an immunoproteasome as compared to a constitutive proteasome, said compound having a structure of Formula (I):
- 11. A method of selectively inhibiting an immunoproteasome in a cell where such inhibition is desirable, the method comprising contacting the cell with a proteasome inhibitor having specificity for an immunoproteasome.
- 25. A method for treating a cancer in a subject in need of treatment thereof, the method comprising administering to the subject a therapeutic amount of a proteasome inhibitor having specificity for an immunoproteasome.
- 41. A method for treating inflammation in a subject in need of treatment thereof, the method comprising administering to the subject a therapeutic amount of a proteasome inhibitor having specificity for an immunoproteasome.
- 56. A method for treating an auto-immune disease in a subject in need of treatment thereof, the method comprising administering to the subject a therapeutic amount of a proteasome inhibitor having specificity for an immunoproteasome.
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70. A method of suppressing endogenous antigenic peptide generation in a subject in need thereof, the method comprising administering to the subject a therapeutic amount of a proteasome inhibitor having specificity for an immunoproteasome.
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71. A pharmaceutical formulation comprising:
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(a) a compound having a 10-fold or greater preference for inhibiting an immunoproteasome as compared to a constitutive proteasome; and
(b) a pharmaceutically acceptable carrier.
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Specification