A5044711943- Cancer-related molecular mechanisms research
- Protein Degradation and Inhibitors
- Histone Deacetylase Inhibitors Research
- Natural product bioactivities and synthesis
- Ubiquitin and proteasome pathways
- Genomics, phytochemicals, and oxidative stress
- Synthesis and biological activity
- Curcumin's Biomedical Applications
- RNA modifications and cancer
- Peptidase Inhibition and Analysis
- Biological Activity of Diterpenoids and Biflavonoids
- Antioxidant Activity and Oxidative Stress
- Circular RNAs in diseases
- Cancer, Lipids, and Metabolism
- Ferroptosis and cancer prognosis
- Bioactive Natural Diterpenoids Research
- Nanoparticle-Based Drug Delivery
- Nanoplatforms for cancer theranostics
- Immune Response and Inflammation
- Laser-Ablation Synthesis of Nanoparticles
- Cancer, Hypoxia, and Metabolism
- Marine Sponges and Natural Products
- Selenium in Biological Systems
- Lipid metabolism and biosynthesis
- Nanoparticles: synthesis and applications
University of Florida
2023-2024
Florida College
2023-2024
Banaras Hindu University
2018-2023
University of Florida Health
2023
HDAC8 plays crucial roles in biological processes, from gene regulation to cell motility, making it a highly desirable target for therapeutic intervention. also has deacetylase-independent activity which cannot be blocked by conventional inhibitor. In this study, we report the discovery of YX862, potent and selective hydrazide-based HDAC8-proteolysis targeting chimera (PROTAC) degrader. The selectivity is achieved through rational design warhead spare HDAC3 previous HDAC3/8 dual degrader...
Abstract Cancer cells exhibit elevated lipid synthesis. In breast and other cancer types, genes involved in production are highly upregulated, but the mechanisms that control their expression remain poorly understood. Using integrated transcriptomic, lipidomic, molecular studies, here we report DAXX is a regulator of oncogenic lipogenesis. depletion attenuates, while its overexpression enhances, lipogenic gene expression, lipogenesis, tumor growth. Mechanistically, interacts with SREBP1...
Although over 100 species of Curcuma are reported, only longa is extensively studied. raktakanda, a poorly studied species, most commonly distributed in the Kerala state India. For first time, we examined efficacy different fractions (acetone, hexane, and ethyl acetate) C. raktakanda against glioma, cervical, breast cancer cell lines. As determined by mitochondrial reductase activity assay, viability cells was decreased concentration-dependent manner three fractions. The half maximal...
Abstract The sesquiterpene lactones, Isodeoxyelephantopin (IDET) and Deoxyelephantopin (DET) are known to exhibit activities against some cancer types. of these lactones breast the molecular bases is not known. We examined efficacy in preclinical model. Although both exhibited drug like properties, IDET was relatively effective comparison DET. suppressed proliferation invasive non-invasive cell lines. also colony formation migration cells. assays for Acridine Orange (AO)/Propidium Iodide...
Abstract HDAC8 plays crucial roles in biological processes and is a highly desirable target for therapeutic interventions. However, due to the conserved catalytic domain among HDACs, developing specific inhibitors these isozymes has proven challenging. also deacetylase-independent activity which cannot be blocked by an inhibitor. Previously we reported discoveries of potent HDAC3 degrader XZ9002 HDAC3/8 dual YX968. In this study, carried out further optimizations based on warhead YX968...
Abstract Intracellular lipid production in cancer cells supplies lipids to synthesize cell membranes and signaling molecules during rapid proliferation tumor growth. Cancer also utilize fatty acid oxidation (FAO) generate ATP meet their energy demand. Notably, metabolites can inhibit trigger ferroptosis due iron-dependent of polyunsaturated acids (PUFAs). Therefore, identifying regulators that maintain the intricate balance biosynthesis required for survival is critical biology therapy....
Proteolysis targeting chimeras (PROTACs) are an emerging targeted cancer therapy approach, but wide-spread clinical use of PROTAC is limited due to poor cell and penetration, instability in vivo. To overcome such issues enhance the vivo efficacy drugs, microfluidic droplet-based electroporation (µDES) was developed as a novel extracellular vesicle (EVs) transfection system, which enables high-efficient loading effective delivery Our previously YX968 drug had shown selectively degradation...
Abstract Histone deacetylases (HDACs) are enzymes that play an essential role in multiple cellular processes such as DNA transcription, translation, replication, recombination, repair, and metabolism, their dysregulation can be linked to many different diseases. Most commonly, the overexpression of HDACs is found various cancer types including hematologic cancers, well solid malignancies. Of body, class I HDACs, which consist 1, 2, 3, 8, activating oncogenes underlying tumorigenesis, disease...
Abstract Breast cancer is a significant public health issue that remains the second leading cause of death among women. Current treatment strategies for breast can contribute to severe side effects and insufficient efficacy. For example, chemotherapy, radiotherapy, hormone receptor HER2 targeted therapies lead healthy cell damage, partial, delayed effect, cardiac toxicity acquired immune resistance, respectively. An emerging alternative therapy approach proteolysis targeting chimeras...