IP Library Granted Patent US 7,741,432
Granted Patent B2
US 7,741,432 · App. 11/443,819 · Granted Jun 22, 2010

Substrate for Rpn11 enzymatic activity

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Quick Facts
Patent No.
US 7,741,432
App. No.
11/443,819
Granted
Jun 22, 2010
Kind
B2
Abstract

The present application provides peptides that serve as substrates for proteasome enzymatic activity, e.g., the enzymatic activity of Rpn11, a metalloprotease of the 19S regulatory particle. The present application also provides methods and compositions employing the peptide substrates.

Claims (28)

1. An isolated peptide comprising an amino acid sequence at least 80% identical to SEQ ID NO:1 and at least one ubiquitin moiety that is at least 90% identical to the first 76-amino acid sequence of SEQ ID NO:2, wherein a deubiquitinating protease deubiquitinates the peptide.

2. The peptide of claim 1 , wherein the protease is a deubiquitinating metalloprotease.

3. The peptide of claim 1 , wherein the protease is a deubiquitinating non-metalloprotease.

4. The peptide of claim 1 , wherein the protease is Rpn11.

5. The peptide of claim 1 , further comprising at least 3 additional amino acids at the C-terminus of the peptide.

6. The peptide of claim 1 , wherein the amino acid sequence has the amino acid sequence of SEQ ID NO:1 wherein at least one non-Ala amino acid is replaced by Ala.

7. The peptide of claim 1 , wherein the amino acid sequence has the amino acid sequence of SEQ ID NO:4 wherein at least one non-Ala amino acid is replaced by Ala.

8. The peptide of claim 1 , further comprising one or more ubiquitin moieties at the N-terminus of the peptide.

9. The peptide of claim 8 , wherein the ubiquitin moiety consists of two or more repeats of an amino acid sequence that is at least 90% identical to the first 76-amino acid sequence of SEQ ID NO:2.

10. The peptide of claim 1 , wherein the ubiquitin moiety comprises the first 76-amino acid sequence of SEQ ID NO:2 modified such that the 75th amino acid is an Ala.

11. The peptide of claim 1 , wherein the ubiquitin moiety comprises the first 76-amino acid sequence of SEQ ID NO:2 modified such that the 76th amino acid is an Ala.

12. The peptide of claim 1 , further comprising a detectable agent linked to the peptide.

13. The peptide of claim 12 , wherein the detectable agent is a fluorescent label.

14. The peptide of claim 13 , wherein the fluorescent label is a fluorescent peptide linked to the C-terminus of the peptide by a peptide bond.

15. The peptide of claim 12 , wherein the detectable agent is a radioactive label.

16. The peptide of claim 1 further comprising an N-terminal target portion or C-terminal target portion that specifically binds to a selection agent.

17. The peptide of claim 16 , wherein the selection agent is an antibody.

18. The peptide of claim 16 , wherein the selection agent is a divalent metal ion.

19. The peptide of claim 1 , wherein the peptide comprises SEQ ID NO: 1 and at least one ubiquitin moiety that is at least 90% identical to the first 76-amino acid sequence of SEQ ID NO:2.

20. The peptide of claim 19 , wherein the peptide comprises SEQ ID NO: 1 and at least one ubiquitin moiety that is identical to the first 76-amino acid sequence of SEQ ID NO:2.

21. The peptide of claim 1 , wherein the peptide comprises at least one of the amino acid sequences as set forth in SEQ ID NOs: 3-15 and at least one ubiquitin moiety that is at least 90% identical to the first 76-amino acid sequence of SEQ ID NO:2.

22. The peptide of claim 21 , wherein the peptide comprises at least one of the amino acid sequences as set forth in SEQ ID NOs: 3-15 and at least one ubiquitin moiety that is identical to the first 76-amino acid sequence of SEQ ID NO:2.

23. The peptide of claim 10 , wherein the peptide comprises SEQ ID NO: 1.

24. The peptide of claim 11 , wherein the peptide comprises SEQ ID NO: 1.

25. The peptide of claim 10 , wherein the peptide comprises at least one of the amino acid sequences as set forth in SEQ ID NOs: 3-15.

26. The peptide of claim 11 , wherein the peptide comprises at least one of the amino acid sequences as set forth in SEQ ID NOs: 3-15.

27. The peptide of claim 1 , wherein the deubiquitinating protease comprises a JAMM motif.

28. The peptide of claim 27 , wherein the JAMM motif comprises the amino acid sequence of SEQ ID NO: 17 or SEQ ID NO:18.

Assignments (3)
MERGER Recorded May 14, 2010
From: PROTEOLIX, INC.
To: ONYX THERAPEUTICS, INC.
Reel/Frame 024380/0824 →
ASSIGNEE ADDRESS CHANGE Recorded Apr 30, 2009
From: PROTEOLIX, INC.
To: PROTEOLIX, INC.
Reel/Frame 022868/0325 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 15, 2006
From: PARLATI, FRANCESCO; AUJAY, MONETTE; BENNETT, MARK K.
To: PROTEOLIX, INC.
Reel/Frame 018270/0768 →