A5064081580- RNA and protein synthesis mechanisms
- PI3K/AKT/mTOR signaling in cancer
- Ion Channels and Receptors
- Ion channel regulation and function
- Phytochemicals and Antioxidant Activities
- Pain Mechanisms and Treatments
- Neurobiology and Insect Physiology Research
- RNA modifications and cancer
- Neuroscience and Neuropharmacology Research
- Mitochondrial Function and Pathology
- Immunotherapy and Immune Responses
- Heat shock proteins research
- Cancer, Hypoxia, and Metabolism
- Chemical Synthesis and Analysis
- Immune Cell Function and Interaction
- Hypothalamic control of reproductive hormones
- Polyamine Metabolism and Applications
- Estrogen and related hormone effects
- Ovarian function and disorders
- Protein Kinase Regulation and GTPase Signaling
- T-cell and B-cell Immunology
- Microbial Natural Products and Biosynthesis
- Biochemical Analysis and Sensing Techniques
Seoul National University
2002-2019
We developed a compound library for orally available gonadotropin-releasing hormone (GnRH) receptor antagonists that were based on uracil scaffold. On the basis of in vitro activity and CYP inhibition profile, we selected 18a (SKI2496) further vivo studies. Compound exhibited more selective antagonistic toward human GnRH receptors over GnRHRs monkeys rats, this also showed inhibitory effects GnRH-mediated signaling pathways. Pharmacokinetic pharmacodynamic evaluations revealed improved...
Recent studies indicate that LRS may act as a leucine sensor for the mTORC1 pathway, potentially providing an alternative strategy to overcome rapamycin resistance in cancer treatments. In this study, we developed leucyladenylate sulfamate derivatives LRS-targeted inhibitors. Compound 18 selectively inhibited LRS-mediated activation and exerted specific cytotoxicity against colon cells with hyperactive mTORC1, suggesting offer novel treatment option human colorectal cancer.