Document Type
Article
Publication Date
September 2025
Patent Number
12415832
CPC
C07K 7/02 , A61K 38/08 , A61K 45/06 , A61K 38/00 , A61P 35/00 , C07D 495/04 , C07D 311/80
Abstract
Disclosed herein is a series of helical sulfono-γ-AApeptides that mimic the binding mode of the α-helical HD2 domain of B-Cell Lymphoma 9 (BCL9). As disclosed herein, sulfono-γ-AApeptides can structurally and functionally mimic the α-helical domain of BCL9, and selectively disrupt β-catenin/BCL9 PPIs with even higher potency. More intriguingly, these sulfono-γ-AApeptides can enter cancer cells, bind with β-catenin and disrupt β-catenin/BCL PPI, and exhibit excellent cellular activity, which is much more potent than the BCL9 peptide. Furthermore, enzymatic stability studies demonstrated the remarkable stability of the helical sulfono-γ-AApeptides, with no degradation in the presence of pronase for 24 h, augmenting their biological potential.
Application Number
17/605219
Recommended Citation
Cai, Jianfeng; Sang, Peng; Shi, Yan; Ji, Haitao; and Zhang, Min, "B-catenin/B-cell Lymphoma 9 protein-protein interaction inhibiting peptidomimetics" (2025). USF Patents. 1528.
https://digitalcommons.usf.edu/usf_patents/1528
Assignees
UNIVERSITY OF SOUTH FLORIDA
Filing Date
04/24/2020
