Compounds for mutant kras protein degradation and uses thereof

The present disclosure provides a bifunctional compound of formula (I): RB-Linker-ULM (I), which binds more preferentially to mutant KRAS proteins than to wild KRAS protein and promotes degradation of KRAS protein via recruitment of an E3 ubiquitin ligase. Pharmaceutical compositions comprising the...

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Main Authors CHUANG, SHIH-HSIEN, LAI, CHUN-LIANG, LIN, YU-SHIANG, YEN, SHIHIEH, LIU, YEN-HSI, LIN, HER-SHENG, CHEN, PO TING, YANG, YUNG-NING, HSU, HUI-JAN, LI, TSUNG-HUI, LAILEE, YING-SHUAN, LIN, KUAN SHUO
Format Patent
LanguageChinese
English
Published 21.05.2024
Subjects
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present disclosure provides a bifunctional compound of formula (I): RB-Linker-ULM (I), which binds more preferentially to mutant KRAS proteins than to wild KRAS protein and promotes degradation of KRAS protein via recruitment of an E3 ubiquitin ligase. Pharmaceutical compositions comprising the bifunctional compound and uses thereof are also provided.
Bibliography:Application Number: TW202211150700