US2015105446A1PendingUtilityA1

Novel Activation and Transfer Cascade for Ubiquitin

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Assignee: HARVARD COLLEGEPriority: Jan 18, 2007Filed: Aug 26, 2014Published: Apr 16, 2015
Est. expiryJan 18, 2027(~0.5 yrs left)· nominal 20-yr term from priority
Inventors:Jeffrey Wade HarperJianping Jin
C12N 9/93C12N 2310/111A61P 35/00A61P 43/00C12N 15/1137A61P 35/02
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Claims

Abstract

A novel activating enzyme for ubiquitin, Uba6, is provided. Compositions and methods for inhibiting ubiquitin via the Uba6 pathway are provided. Methods of identifying novel inhibitors of ubiquitination are also provided. Novel RNAi molecules are also provided.

Claims

exact text as granted — not AI-modified
What is claimed: 
     
         1 . A method for inhibiting a Uba6 activity comprising:
 contacting Uba6 with a compound that inhibits formation of a ubiquitin-adenylate intermediate.   
     
     
         2 . The method of  claim 1 , wherein the compound binds an adenylation domain of Uba6. 
     
     
         3 . The method of  claim 1 , performed in vitro or in vivo. 
     
     
         4 . The method of  claim 1 , performed in tissue culture cells. 
     
     
         5 . A method for inhibiting a Uba6 activity comprising:
 contacting Uba6 with a compound that inhibits thiol esterification of Uba6.   
     
     
         6 . The method of  claim 5 , performed in vitro or in vivo. 
     
     
         7 . The method of  claim 5 , performed in tissue culture cells. 
     
     
         8 . A method for inhibiting a Uba6 activity comprising:
 contacting Uba6 with a compound that inhibits transfer of ubiquitin to a ubiquitin conjugating enzyme.   
     
     
         9 . The method of  claim 8 , wherein the compound binds a Ubl domain of Uba6. 
     
     
         10 . The method of  claim 8 , performed in vitro or in vivo. 
     
     
         11 . The method of  claim 8 , performed in tissue culture cells. 
     
     
         12 . The method of  claim 8 , wherein the ubiquitin conjugating enzyme is selected from the group consisting of: E2C, E2D1, E2D2, E2D3, E2D4, E2E1, E2G, E2S, E2T and E2Z. 
     
     
         13 . The method of  claim 8 , wherein the ubiquitin conjugating enzyme is E2Z. 
     
     
         14 . A method for inhibiting ubiquitin activation comprising:
 contacting Uba6 with a compound that inhibits a catalytic cysteine domain of Uba6.   
     
     
         15 . The method of  claim 14 , performed in vitro or in vivo. 
     
     
         16 . The method of  claim 14 , performed in tissue culture cells.

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