A5016925161- Protein Kinase Regulation and GTPase Signaling
- Ubiquitin and proteasome pathways
- Synthesis and biological activity
- PI3K/AKT/mTOR signaling in cancer
- Cytokine Signaling Pathways and Interactions
- HER2/EGFR in Cancer Research
- Peptidase Inhibition and Analysis
- Glycosylation and Glycoproteins Research
- Hearing, Cochlea, Tinnitus, Genetics
- Adenosine and Purinergic Signaling
- Enzyme function and inhibition
- Cancer, Stress, Anesthesia, and Immune Response
- Click Chemistry and Applications
- Melanoma and MAPK Pathways
- Platelet Disorders and Treatments
- Protein Degradation and Inhibitors
- Lung Cancer Treatments and Mutations
- Cancer-related gene regulation
- Respiratory and Cough-Related Research
- Rheumatoid Arthritis Research and Therapies
- Synthetic Organic Chemistry Methods
- Synthesis and Characterization of Heterocyclic Compounds
- Quinazolinone synthesis and applications
- Phagocytosis and Immune Regulation
- Cancer Immunotherapy and Biomarkers
Yonsei University
2011-2024
Abstract PRMT5 participates in various cellular processes, including transcription regulation, signal transduction, mRNA splicing, and DNA repair; however, its mechanism of regulation is poorly understood. Here, we demonstrate that phosphorylated at residue Y324 by Src kinase, a negative regulator activity. Either phosphorylation or substitution the suppresses activity preventing binding with methyl donor S-adenosyl-L-methionine. Additionally, show associated non-homologous end joining...
Rationale: Pendrin is encoded by SLC26A4 and its mutation leads to congenital hearing loss. Additionally, pendrin up-regulated in inflammatory airway diseases such as chronic obstructive pulmonary disease, allergic rhinitis, asthma. In this study, the effects of a novel inhibitor, YS-01, were investigated an LPS-induced acute lung injury (ALI) mice model, mechanism underlying effect YS-01 was examined. Methods: Lipopolysaccharide (LPS, 10 mg/kg) intranasally instilled wild type (WT)...
Abstract Phospholipase D (PLD) is a potential therapeutic target against cancer. However, the contribution of PLD inhibition to antitumor response remains unknown. We developed potent and selective PLD1 inhibitor based on computer-aided drug design. The enhanced apoptosis in colorectal cancer (CRC) cells but not normal colonic cells, vitro cardiotoxicity was observed. downregulated Wnt/β-catenin signaling pathway reduced migration, invasion, self-renewal capacity CRC cells. In cancer,...
The epidermal growth factor receptor (EGFR), also known as ErbB1 and HER1, belongs to the tyrosine kinase family. EGFR serves primary driver in non-small-cell lung cancer (NSCLC) is a promising therapeutic target for NSCLC. In this study, we synthesized novel chemical library based on benzofuran–indole hybrid scaffold identified 8aa potent selective inhibitor. Interestingly, not only showed anticancer effects against NSCLC cell lines, PC9, A549, but it significant inhibitory double mutant...
Although natural products are an important source of drugs and drug leads, identification validation their target proteins have proven difficult. Here, we report the development a systematic strategy for employing affinity responsive stability (DARTS) mass spectrometry imaging (MSI) without modifying or labeling compounds. Through step using curcumin, which targets aminopeptidase N (APN), successfully standardized strategy. Using label-free voacangine, antiangiogenic alkaloid molecule as...
In this study we showed that 2-(trimethylammonium)ethyl (R)-3-methoxy-3-oxo-2-stearamidopropyl phosphate [(R)-TEMOSPho], a derivative of an organic chemical identified from natural product library, promotes highly efficient differentiation megakaryocytes. Specifically, (R)-TEMOSPho induces cell cycle arrest, size increase and polyploidization K562 HEL cells, which are used extensively to model megakaryocytic differentiation. addition, megakaryocyte-specific surface markers dramatic in...
This study explored novel immunomodulatory approaches for cancer treatment, with a specific focus on lung cancer, the leading cause of cancer-related deaths worldwide. We synthesized indole-based phospholipase D (PLD) inhibitors various substituents to improve anticancer efficacy. Through structure–activity relationship studies, key compound was identified that significantly inhibiting PLD, suppressing cell growth, viability, and migration in vitro, while inducing apoptosis cells. In silico...
Although natural products are an important source of drugs and drug leads, identification validation their target proteins have proven difficult. Here, we report the development a systematic strategy for employing affinity responsive stability (DARTS) mass spectrometry imaging (MSI) without modifying or labeling compounds. Through step using curcumin, which targets aminopeptidase N (APN), successfully standardized strategy. Using label-free voacangine, antiangiogenic alkaloid molecule as...
Ras protein has been considered a fascinating target for anticancer therapy because its malfunction is closely related to cancer. However, undruggable of the failure regulate by controlling activation mechanism. Recently, Lumakras targeting G12C mutation was approved, and therapeutic interest in rejuvenated. Here, we present series compounds that inhibit via unique mechanism action exploits relationship between Wnt/β-catenin pathway Ras. KYA1797K (1) binds axin stabilize β-catenin...
Variants in SLC26A4 (pendrin) are the most common reasons for genetic hearing loss and vestibular dysfunction East Asians. In patients with Pendred syndrome DFNB4 (autosomal recessive type of 4), caused by variants SLC26A4, function is residual at birth deteriorates over several years, no curative treatment these disorders. present study, we revealed that a novel small molecule restores expression mutant pendrin. High-throughput screening 54,000 molecules was performed. We observed pendrin...