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US 2025/0213701 A1Published application
Medicament for treating human tumor based on erf3a-targeting proteolysis mechanism
AssigneeSuzhou Degen Bio-Medical Co., Ltd.
InventorsGuangliang YU, Kai ZHONG, Yao CHEN, Liuquan HAN, Jiahui TIAN, Changzhou ZHANG, Zhenxing HU, Ping XU, Shujun MAO
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Abstract
The present disclosure provides a proteolysis-targeting compound TPB-L-E3B, a method for synthesizing the same, and use thereof. The compound can treat human tumor diseases through the eRF3a-targeting proteolysis mechanism, and exhibits great potential in treating such diseases in in-vitro studies, particularly, in treating diseases such as prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer, and the like.
Claims7
A compound having a structure of:
- TPB-L-E3B,
- wherein TPB is a target protein-binding moiety, L is a linker, and E3B is an E3 ligase-binding moiety,
- TPB is shown in a structure (I),
- L is selected from a structure (IIA) or (IIB),
- X is CH2, O, NH, or CF2, n is an integer of 2-3, Y is NH or O, and Z is NH or O;
- E3B is selected from a structure (IIIA), (IIIB), or (IIIC),
- denotes that C may have R configuration, S configuration, or a mixture of R and S configurations, and R1 denotes that the H at any one of three positions of the benzene ring is substituted by F.
4 more elements
Dependencies are inferred from the claim text.