IP Library Granted Patent US 12669508
Granted Patent B2
US 12669508 · App. 17/976,330 · Granted Jun 30, 2026

Methods to prevent disulfide scrambling for MS-based proteomics

Inventors: Andrew Kleinberg (Roslyn Heights, NY); Yuan Mao (Hartsdale, NY); Ning Li (New Canaan, CT)
Assignee: REGENERON PHARMACEUTICALS, INC.
G01N33/6848G01N2560/00
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Quick Facts
Patent No.
US 12669508
App. No.
17/976,330
Granted
Jun 30, 2026
Kind
B2
Abstract

The present invention generally pertains to methods of preventing disulfide scrambling in non-reducing liquid chromatography-mass spectrometry analysis of a protein of interest. In particular, the present invention pertains to the addition of maleimide to a non-reducing liquid chromatography-mass spectrometry analysis of a protein to prevent disulfide scrambling.

Claims (26)

1 . A method for performing a non-reduced peptide mapping of a protein of interest in a sample, said method comprising:

a. contacting said sample to a NEM analog to form an alkylated protein of interest, wherein the NEM analog is maleimide or N-hydroxy maleimide;

b. contacting said alkylated protein of interest to at least one digestive enzyme to form a peptide digest; and

c. analyzing said peptide digest using liquid chromatography-mass spectrometry to obtain said non-reduced peptide mapping of said protein of interest.

2 . The method of claim 1 , wherein the NEM analog is maleimide.

3 . The method of claim 1 , wherein the concentration of NEM analog used to contact said sample is about 1 mM to about 10 mM.

4 . The method of claim 1 , wherein the concentration of NEM analog used to contact said sample is about 2 mM to about 8 mM.

5 . The method of claim 1 , wherein the concentration of NEM analog used to contact said sample is about 4 mM.

6 . The method of claim 1 , wherein said NEM analog is contacted with said sample at 50° C. for 30 minutes.

7 . The method of claim 1 , wherein said protein of interest is an antibody.

8 . The method of claim 1 , further comprising contacting said sample to at least one denaturation agent.

9 . The method of claim 1 , wherein said at least one digestive enzyme is trypsin.

10 . The method of claim 1 , wherein said at least one digestive enzyme is Lys-C.

11 . The method of claim 1 , wherein said at least one digestive enzyme is Lys-C and trypsin.

12 . The method of claim 1 , wherein said digestion is conducted at a pH of about 7 to about 8.

13 . The method of claim 1 , wherein said digestion is conducted at a pH of about 7 to about 7.5.

14 . The method of claim 1 , wherein said digestion is conducted at a pH of about 5 to about 6.

15 . The method of claim 1 , wherein said digestion is conducted at a pH of about 5.3 to about 7.

16 . A method for characterizing a protein of interest in a sample, said method comprising:

a. contacting said sample to a NEM analog to form an alkylated protein of interest, wherein the NEM analog is maleimide or N-hydroxy maleimide;

b. contacting said alkylated protein of interest to at least one digestive enzyme to form a peptide digest; and

c. analyzing said peptide digest using liquid chromatography-mass spectrometry to obtain a non-reduced peptide mapping to characterize said protein of interest.

17 . The method of claim 16 , wherein the NEM analog is maleimide.

18 . The method of claim 17 , wherein the concentration of maleimide used to contact said sample is about 2 mM to about 8 mM.

19 . The method of claim 18 , wherein the concentration of maleimide used to contact said sample is about 4 mM.

20 . The method of claim 16 , further comprising contacting said sample to at least one denaturation agent.