A5079473826- Lipid metabolism and disorders
- Renal Diseases and Glomerulopathies
- Crystallization and Solubility Studies
- Chronic Lymphocytic Leukemia Research
- X-ray Diffraction in Crystallography
- Synthesis and Catalytic Reactions
- Catalytic C–H Functionalization Methods
- Protein Degradation and Inhibitors
- Metal complexes synthesis and properties
- Ubiquitin and proteasome pathways
- Histone Deacetylase Inhibitors Research
- Peptidase Inhibition and Analysis
- Lung Cancer Research Studies
- Cancer, Lipids, and Metabolism
- Bioactive Compounds and Antitumor Agents
- Crystallography and molecular interactions
- Effects and risks of endocrine disrupting chemicals
- Multiple Myeloma Research and Treatments
- Medicinal Plant Extracts Effects
- Sulfur-Based Synthesis Techniques
- Cancer-related Molecular Pathways
- Click Chemistry and Applications
- Magnetism in coordination complexes
- Cancer Research and Treatments
- Immune Cell Function and Interaction
University of Florida
2021-2024
Florida College
2023-2024
University of Florida Health
2021-2024
UF Health Cancer Center
2024
Sungkyunkwan University
2014-2018
Government of the Republic of Korea
2016-2018
Kwangshin University
2015
Suwon Research Institute
2014
Pusan National University
2011-2013
The rhodium(III)-catalyzed redox-neutral coupling reaction of N-acyl ketimines generated in situ from 3-hydroxyisoindolinones with various activated olefins is described. This approach leads to the synthesis bioactive spiroisoindolinone derivatives moderate high yields. In case internal such as maleimides, maleates, fumarates, and cinnamates, spiroindanes were obtained by [3 + 2] annulations reaction. sharp contrast, acrylates quinones displayed β-H elimination followed Prins-type...
The weakly coordinating ketone group directed C–H functionalizations of chromones, 1,4-naphthoquinones, and xanthones with various maleimides under rhodium(III) catalysis are described. These protocols efficiently provide a range succinimide-containing naphthoquinones, excellent site selectivity functional compatibility. All synthetic compounds were screened for in vitro anticancer activity against human breast adenocarcinoma cell lines (MCF-7). In particular, 7aa 7ca naphthoquinone scaffold...
The rhodium(III)-catalyzed direct C-H functionalization of various indolines with 1,4,2-dioxazol-5-ones as new amidating agents is described. This transformation provides efficient preparation C7-amidated known to display potent anticancer activity. synthetic compounds were evaluated for in vitro activity against human prostate adenocarcinoma cells (LNCaP), endometrial (Ishikawa), and ovarian carcinoma (SKOV3). Compound 4f was found be highly cytotoxic, competitive that agent doxorubicin.
Regulatory T (Treg) cells are one of the major immunosuppressive cell types in cancer and a potential target for immunotherapy, but targeting tumor-infiltrating (TI) Treg has been challenging. Here, using single-cell RNA sequencing immune from renal clear carcinoma (ccRCC) patients, we identify two distinct transcriptional fates TI cells, Fate-1 Fate-2. The signature is associated with poorer prognosis ccRCC several other solid cancers. CD177, surface protein normally expressed on...
Small-cell lung cancer (SCLC) is an aggressive malignancy with limited therapeutic options. The dismal prognosis in SCLC part associated upregulation of BCL-2 family anti-apoptotic proteins, including BCL-XL and MCL-1. Unfortunately, the currently available inhibitors except inhibitors, are not clinically relevant because various on-target toxicities. We, therefore, aimed to develop effective safe strategy targeting these proteins DT2216 (our platelet-sparing degrader) AZD8055 (an mTOR...
Abstract Regulatory T cells (Tregs) play an important role in maintaining immune homeostasis and, within tumors, their upregulation is common and promotes immunosuppressive microenvironment. Therapeutic strategies that can eliminate Tregs the tumor (i.e., therapies do not run risk of affecting normal tissues), are urgently needed for development cancer immunotherapies. Here we report our discovery B-cell lymphoma extra-large (BCL-X L ) as a potential molecular target tumor-infiltrating (TI)...
A ketone-assisted ruthenium-catalyzed selective amination of xanthones and chromones C–H bonds with sulfonyl azides is described. The reactions proceed efficiently a broad range substrates excellent functional group compatibility. This protocol provides direct access to 1-aminoxanthones, 5-aminochromones, 5-aminoflavonoid derivatives known exhibit potent anticancer activity.
The sirtuins (SIRTs), a family of NAD + -dependent class III histone deacetylase, are involved in various biological processes including cell survival, division, senescence, and metabolism via activation the stress-response pathway.Recently, inhibition SIRTs has been considered promising anticancer strategy, but their precise mechanisms action not well understood.In particular, relevance p53 to SIRT-induced effects fully elucidated.We investigated novel SIRT inhibitor, MHY2256, its efficacy...
We previously discovered a novel sirtuin (SIRT) inhibitor, MHY2256, that exerts anticancer activity through p53 acetylation in MCF-7 human breast cancer cells. investigated the of MHY2256 against hormone-related cancer, an endometrial with poor prognosis. The IC50 values were shown to be much lower than those salermide, well-known SIRT inhibitor. Furthermore, significantly reduced protein expression and activities SIRT1, 2, 3, similar effects salermide. Particularly, markedly inhibited tumor...
Six mononuclear Ir complexes (1-6) using polypyridyl-pyrazine based ligands (L1 and L2) {[cp*IrCl(μ-Cl)]2 [(ppy)2Ir(μ-Cl)]2} precursors have been synthesised characterised. Complexes 1-5 shown potent anticancer activity against various human cancer cell lines (MCF-7, LNCap, Ishikawa, DU145, PC3 SKOV3) while complex 6 is found to be inactive. Flow cytometry studies established that cellular accumulation of the lies in order 2 > 1 5 4 3 which accordance with their observed cytotoxicity. No...
An effective cancer therapy requires killing cells and targeting the tumor microenvironment (TME). Searching for molecules critical multiple cell types in TME, we identified NR4A1 as one such molecule that can maintain immune suppressive TME. Here, establish a valid target immunotherapy describe first-of-its-kind proteolysis-targeting chimera (PROTAC, named NR-V04) against NR4A1. NR-V04 degrades within hours vitro exhibits long-lasting degradation tumors with an excellent safety profile....
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Heterodinuclear Ir–Ru (<bold>2</bold>) with polypyridyl based phpy ligand shows autophagy induced cell death, whereas homodinuclear Ru–Ru (<bold>1</bold>) is inactive.
Abstract The rhodium(III)‐catalyzed C−H amidation and subsequent C−N bond formation reaction of indolines with aryl alkyl isocyanates at room temperature are reported. These transformations allow the generation N ‐aroylurea functionality C7‐position indolines, which is known as a crucial scaffold found in biologically active molecules. In addition, synthesis pyrroloindolidione derivatives also described through sequential C6‐amidation intramolecular cyclization C7‐amidated indolines. All...
New potential chemotherapeutic strategies are required to overcome multidrug resistance (MDR) in cancer. This study investigated the anticancer effect of a novel anthracene derivative MHY412 on doxorubicin-resistant human breast cancer (MCF-7/Adr) cells. We measured cell viability and expression apoptosis-related genes; addition, antitumor activity was confirmed using an vivo tumor xenograft model. significantly inhibited proliferation MCF-7/Adr MCF-7 cells concentration-dependent manner....
Abstract Childhood Sjögren’s disease represents critically unmet medical needs due to a complete lack of immunological and molecular characterizations. This study presents key immune cell subsets their interactions in the periphery childhood disease. Here we show that single-cell RNA sequencing identifies IFN gene-enriched monocytes, CD4 + T effector memory, XCL1 NK cells as potential players disease, especially those with recurrent parotitis, which is chief symptom prompting clinical visits...