A5015298498- Protein Degradation and Inhibitors
- Protein Tyrosine Phosphatases
- Bladder and Urothelial Cancer Treatments
- ATP Synthase and ATPases Research
- Cancer-related molecular mechanisms research
- Bioactive Compounds and Antitumor Agents
- Cancer-related gene regulation
- Fibroblast Growth Factor Research
- Ferroptosis and cancer prognosis
- Neutrophil, Myeloperoxidase and Oxidative Mechanisms
- Galectins and Cancer Biology
- Peptidase Inhibition and Analysis
- Ubiquitin and proteasome pathways
Hangzhou Medical College
2023-2024
Peking Union Medical College Hospital
2023
Chinese Academy of Medical Sciences & Peking Union Medical College
2023
Abnormal activation of fibroblast growth factor receptors (FGFRs) results in the development and progression human cancers. FGFR2 is frequently amplified or mutated cancers; therefore, it an attractive target for tumor therapy. Despite several pan-FGFR inhibitors, their long-term therapeutic efficacy hindered by acquired mutations low isoform selectivity. Herein, we report discovery efficient selective proteolysis-targeting chimeric molecule, LC-MB12, that incorporates essential rigid...
RNA Polymerase III Subunit G (POLR3G) promotes tumorigenesis, metastasis, cancer stemness, and chemoresistance of breast lung cancer; however, its biological function in bladder (BLCA) remains unclear. Through bioinformatic analyses, we found that POLR3G expression was significantly elevated BLCA tumor tissues associated with decreased survival. Multivariate Cox analysis indicated could serve as an independent prognostic risk factor. Our functional investigations revealed deficiency resulted...
Interleukin-1 receptor-associated kinase 4 (IRAK4) is a promising therapeutic target in inflammation-related diseases. However, the inhibition of IRAK4 activity may lead to moderate anti-inflammatory efficacy owing dual role as an active and scaffolding protein. Herein, we report design, synthesis, biological evaluation efficient selective proteolysis-targeting chimeric molecule that eliminates functions. The most potent compound, LC-MI-3, effectively degraded cellular IRAK4, with...