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US 12,760,298 B2Granted
Technologies useful for assessing permeability
AssigneeParabilis Medicines, Inc.
InventorsAmrita Singh Chandhoke, James Andrew Madsen, Yue-Mei Zhang, John Hanney McGee, Marco Peter Fekkes
Life of this patent
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Abstract
In some embodiments, the invention relates to methods and reagents for the identification of compounds that traverse the cell membrane of an animal cell. In some embodiments, the invention provides additional methods for determining if a candidate compound that traverses an animal cell membrane is able to modulate an intracellular target, as well as reagents and kits for reagents and kits for performing the disclosed methods.
Claims5
A method, comprising:
- contacting an agent with one side of a barrier, wherein the agent has the structure of RB-L-FG2 or a salt thereof, the composition on the other side of the barrier comprises a mutant dehalogenase, and if the agent crosses the barrier, the agent can be covalently bonded to the mutant dehalogenase to form a complex;
- hydrolyzing the composition on the other side of the barrier to provide a hydrolysis composition;
- and
- detecting by mass spectrometry in the hydrolysis composition for a product agent, wherein the product agent has the structure of RP-L-FG3 or a salt thereof;
- wherein:
- RB comprises a stapled peptide moiety;
- RP comprises a stapled peptide moiety;
- -L-FG2 is —C(O)(CH2)2C(O)NH(CH2)2O(CH2)2O(CH2)6Cl;
- and
- -L-FG3 is —C(O)(CH2)2C(O)NH(CH2)2O(CH2)2O(CH2)6OH.
7 more elements
Dependencies are inferred from the claim text.