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US 2021/0255193 A1Published application
Lysine reactive probes and uses thereof
AssigneeThe Scripps Research Institute
InventorsBenjamin F. CRAVATT, Stephan M. HACKER, Keriann M. BACKUS
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Abstract
Disclosed herein are methods and compounds for profiling a lysine reactive protein. Also described herein are methods, compounds, and compositions for identifying a small molecule fragment ligand that interacts with a reactive lysine residue.
Claims27
A method of identifying a reactive lysine of a protein, comprising:
- a) providing a protein sample comprising isolated proteins, living cells, or a cell lysate;
- b) contacting the protein sample with a probe compound of Formula (I) at a first concentration for a time sufficient for the probe compound to react with the reactive lysine of the protein sample;
- and
- c) analyzing the proteins of the protein sample to identify the reactive lysine that bound with the probe compound at the first concentration;
- wherein the probe compound has a structure represented by Formula (I):
- wherein,
- F1 is a small molecule fragment moiety comprising an alkyne moiety, a fluorophore moiety, a labeling group, or a combination thereof, and
- LG is a leaving group moiety.
5 more elements
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-41. (canceled)
A modified lysine-containing protein comprising:
- a small molecule fragment moiety, covalently bonded to a lysine residue of a lysine-containing protein,
- wherein a covalent bond is formed by reaction with a non-naturally occurring small molecule probe having a structure of Formula (I):
- wherein,
- F1 is a small molecule fragment moiety comprising an alkyne moiety, a fluorophore moiety, a labeling group, or a combination thereof, and
- LG is a leaving group moiety.
2 more elements
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-53. (canceled)
A modified lysine-containing protein comprising:
- a small molecule fragment moiety, covalently bonded to a lysine residue of a lysine-containing protein,
- wherein a covalent bond is formed by reaction with a non-naturally occurring ligand-electrophile having a structure of Formula (II):
- wherein,
- F2 is a small molecule fragment moiety;
- and
- LG is a leaving group moiety.
3 more elements
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Dependencies are inferred from the claim text.