The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jan. 23, 2024

Filed:

Nov. 30, 2021
Applicant:

Ohio State Innovation Foundation, Columbus, OH (US);

Inventors:

Dehua Pei, Columbus, OH (US);

Ziqing Qian, Columbus, OH (US);

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 38/12 (2006.01); C07K 7/06 (2006.01); C07K 7/08 (2006.01); C07K 7/50 (2006.01); A61K 38/00 (2006.01); C07K 5/10 (2006.01); C07K 14/00 (2006.01);
U.S. Cl.
CPC ...
A61K 38/12 (2013.01); C07K 5/10 (2013.01); C07K 7/06 (2013.01); C07K 7/08 (2013.01); C07K 7/50 (2013.01); C07K 14/001 (2013.01); A61K 38/00 (2013.01);
Abstract

Disclosed is a general, reversible bicyclization strategy to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is fused with a short cell-penetrating motif and converted into a conformationally constrained bicyclic structure through the formation of a pair of disulfide bonds. The resulting bicyclic peptide has greatly enhanced proteolytic stability as well as cell-permeability. Once inside the cell, the disulfide bonds are reduced to produce a linear, biologically active peptide. This strategy was applied to generate a cell-permeable bicyclic peptidyl inhibitor against the NEMO-IKK interaction.


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