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US 12,618,847 B2Granted
Activity-based probes with unnatural amino acids to monitor proteasome activity
AssigneePurdue Research Foundation
InventorsDarci J. Trader, Andres Salazar-Chaparro, Breanna Zerfas
Life of this patent
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Abstract
The disclosure relates to a compound of the formula (I) and the use of such compounds.
Claims13
A compound of formula (I):
- wherein:
- R is A1-A2-A3-A4* (SEQ ID NO:
- 2) or A1-A2-A3-A4-A5* (SEQ ID NO:
- 2);
- R2 is:
- each R3 is independently —N(CH3)2 or —OCH3;
- A1 is Leu or Ac;
- A2 is Leu, Gly, or Arg;
- A3 is Val, Pro, or Leu;
- A4 is Tyr, Leu, or Arg;
- A5 is Asp;
- each instance of n is independently 1, 2, or 3;
- and
- m is 1, 2, or 3.
11 more elements
A method of monitoring a real time increase in proteasome activity in cells, the method comprising contacting the cells with a compound of formula (I)
- wherein:
- R1 is A1-A2-A3-A4* (SEQ ID NO:
- 2) or A1-A2-A3-A4-A5-* (SEQ ID NO:
- 2);
- R2 is:
- each R3 is independently —N(CH3)2 or —OCH3;
- A1 is Leu or Ac;
- A2 is Leu, Gly, or Arg;
- A3 is Val, Pro, or Leu;
- A4 is Tyr, Leu, or Arg;
- A5 is Asp;
- each instance of n is independently 1 2, 3;
- and
- m is 1, 2, 3,
- and measuring proteasome activity by the accumulation of a fluorescent signal.
12 more elements
A method of determining the threshold of proteasome activity required for a cancer cell type to be highly susceptible to proteasome inhibitors, the method comprising contacting the cells with a compound of formula (I)
- wherein:
- R1 is A1-A2-A3-A4* (SEQ ID NO:
- 2) or A1-A2-A3-A4-A5-* (SEQ ID NO:
- 2);
- R2 is:
- each R3 is independently —N(CH3)2 or —OCH3;
- A1 is Leu or Ac;
- A2 is Leu, Gly, or Arg;
- A3 is Val, Pro, or Leu;
- A4 is Tyr, Leu, or Arg;
- A5 is Asp;
- each instance of n is independently 1 2, 3;
- and
- m is 1, 2, 3,
- and measuring proteasome activity by the accumulation of a fluorescent signal.
12 more elements
Dependencies are inferred from the claim text.