Granted Patent
B2
US 12,570,698 · App. 18/306,724 · Granted Mar 10, 2026
Stabilized peptides for covalent binding to target protein
Assignee:
Dana-Farber Cancer Institute, Inc.
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Abstract
Provided herein is a platform technology for designing stabilized peptides that covalently bind their target protein and thereby inhibit the activity of the target protein. Also provided are exemplary stabilized peptides that can be used for covalent modification of their target proteins.
Claims (15)
1 . A stapled peptide comprising:
(i) LKXJLRXHRFLWQR (SEQ ID NO: 13), wherein the first X is cross-linked to the second X;
(ii) LKXALRXJRFLWQR (SEQ ID NO:14), wherein the first X is cross-linked to the second X;
(iii) LKXALRXHRFLJQR (SEQ ID NO:15), wherein the first X is cross-linked to the second X;
(iv) LKKJLRRHXFLWXR (SEQ ID NO:16), wherein the first X is cross-linked to the second X;
(v) LKKALRRJXFLWXR (SEQ ID NO:17), wherein the first X is cross-linked to the second X;
(vi) LKKALRRHXFLJXR (SEQ ID NO:18), wherein the first X is cross-linked to the second X;
(vii) L8KJLRRHXFLWQR (SEQ ID NO:19), wherein 8 is cross-linked to X;
(viii) L8KALRRJXFLWQR (SEQ ID NO:20), wherein 8 is cross-linked to X; or
(ix) L8KALRRHXFLJQR (SEQ ID NO:21), wherein 8 is cross-linked to X; and
wherein X is S-pentenyl alanine, 8 is R-octenyl alanine, and J is a non-natural electrophile containing amino acid.
2 . The stapled peptide of claim 1 , wherein the non-natural electrophile containing amino acid comprises acrylamide.
3 . The stapled peptide of claim 1 , which is no more than 30 amino acids in length.
4 . A pharmaceutical composition comprising the stapled peptide of claim 1 and a pharmaceutically acceptable carrier.
5 . A pharmaceutical composition comprising the stapled peptide of claim 3 and a pharmaceutically acceptable carrier.
Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Apr 25, 2023
From: WALENSKY, LOREN D.; BIRD, GREGORY H.
To: DANA-FARBER CANCER INSTITUTE, INC.
Reel/Frame 063436/0110 →
Continuity (4)
Continuation
15752372
Provisional Application
62211681
· Aug 28, 2015
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