A5100337073- Microbial Natural Products and Biosynthesis
- Prostate Cancer Treatment and Research
- Fungal Biology and Applications
- Advanced Breast Cancer Therapies
- Berberine and alkaloids research
- Marine Sponges and Natural Products
- Synthesis and Biological Activity
- Phytochemical Studies and Bioactivities
- Cancer Genomics and Diagnostics
- Reproductive Biology and Fertility
- Healthcare and Venom Research
- Glioma Diagnosis and Treatment
- Cancer Treatment and Pharmacology
- RNA Interference and Gene Delivery
- Chemical synthesis and alkaloids
- CRISPR and Genetic Engineering
- Lung Cancer Research Studies
- Analytical Chemistry and Chromatography
- Plant-based Medicinal Research
- Phytochemical compounds biological activities
- Natural product bioactivities and synthesis
- Epigenetics and DNA Methylation
- Alkaloids: synthesis and pharmacology
- PARP inhibition in cancer therapy
- Cancer-related Molecular Pathways
University of South Carolina
2019-2025
Lanzhou University
2003-2025
University of South Carolina Sumter
2017-2025
Sunshine Hospital
2022-2025
Shenyang Pharmaceutical University
2013-2025
Fujian Agriculture and Forestry University
2025
Lanzhou University Second Hospital
2025
Qingdao Agricultural University
2024
First Affiliated Hospital of Guangzhou Medical University
2024
State Key Laboratory of Respiratory Disease
2024
OBJECTIVE To evaluate the effects of tirzepatide on body composition, appetite, and energy intake to address potential mechanisms involved in weight loss with tirzepatide. RESEARCH DESIGN AND METHODS In a secondary analysis randomized, double-blind, parallel-arm study, 15 mg (N = 45), semaglutide 1 44), placebo 28) were assessed at baseline week 28. RESULTS Tirzepatide treatment demonstrated significant reductions compared semaglutide, resulting greater fat mass reduction. significantly...
In this work an optimization of the solvent-free acetylation cellulose with acetic anhydride under microwave heating iodine as a catalyst was performed. The optimized parameters included irradiation power from 300 W to 800 W, reaction time between 5 40 min, temperature 80 130 °C, and amount 1 15 mol%. extent measured by yield degree substitution (DS), which determined back-titration method. Acetylated characterized FT-IR, CP/MAS 13C-NMR, WRXD, thermogravimetric analysis. results showed that...
PARP is essential for recognition and repair of DNA damage. In preclinical models, inhibitors modulate topoisomerase I inhibitor-mediated This phase study determined the MTD, dose-limiting toxicities (DLT), pharmacokinetics (PK), pharmacodynamics (PD) veliparib, an orally bioavailable PARP1/2 inhibitor, in combination with irinotecan.
Abstract We have conducted a detailed transcriptomic, proteomic and phosphoproteomic analysis of CDK8 its paralog CDK19, alternative enzymatic components the kinase module associated with transcriptional Mediator complex implicated in development diseases. This was performed using genetic modifications selective CDK8/19 small molecule inhibitors potent PROTAC degrader. inhibition cells exposed to serum or agonists NFκB protein C (PKC) reduced induction signal-responsive genes, indicating...
Mediator kinases CDK19 and CDK8, pleiotropic regulators of transcriptional reprogramming, are differentially regulated by androgen signaling but both upregulated in castration-resistant prostate cancer (CRPC). Genetic or pharmacological inhibition CDK8 reverses the phenotype restores sensitivity CRPC xenografts to deprivation vivo. Prolonged CDK8/19 inhibitor treatment combined with castration not only suppresses growth also induces tumor regression cures. Transcriptomic analysis revealed...
An optimized isomerization method was developed by heating all-E-astaxanthin in ethyl acetate (70 °C) with I-TiO2 catalyst, yielding 22.7% and 16.9% of 9Z- 13Z-astaxanthin, respectively, 2 h, 92-95% purity after semipreparative HPLC purification. 13Z-Astaxanthin had higher antioxidant activity than all-E- 9Z-astaxanthins oxygen radical absorbing capacity assay for lipophilic compounds, photochemiluminescence, cellular (CAA) assays, 9Z-astaxanthin DPPH radical-scavenging lower CAA assay. All...
Abstract Purpose: AZD1775 is a first-in-class Wee1 inhibitor with dual function as DNA damage sensitizer and cytotoxic agent. A phase I study of for solid tumors suggested activity against brain tumors, but preclinical indicated minimal blood–brain barrier penetration in mice. To resolve this controversy, we examined the pharmacokinetics pharmacodynamics patients first-recurrence, glioblastoma. Patients Methods: Twenty adult received single dose prior to tumor resection enrolled either...
Abstract Purpose: Beyond enumeration, circulating tumor cells (CTCs) can provide genetic information from metastatic cancer that may facilitate a greater understanding of biology and enable precision medicine approach. Experimental Design: CTCs paired leukocytes men with castration-resistant prostate (mCRPC) were isolated blood through red cell lysis, CD45 depletion, flow sorting based on EpCAM/CD45 expression. We next performed whole genomic copy number analysis matched patient (germline)...
Effusin A (1), a spirobicyclic N,O-acetal derivative with an unprecedented 3′,3a′,5′,6′-tetrahydrospiro[piperazine-2,2′-pyrano[2,3,4-de]chromene] ring system, and spiro-polyketide-diketopiperazine hybrid dihydrocryptoechinulin D (2) were isolated from mangrove rhizosphere soil derived fungus, Aspergillus effuses H1-1. Their structures determined by detailed spectroscopic analysis. (1) occurred as racemates, the enantiomers of which separated characterized online HPLC-ECD analysis their...
Indotertine A (1), a hybrid isoprenoid with condensed pentacyclic skeleton, together two related isoprenoids, drimentines F (2) and G (3), were isolated from reeds rhizosphere soil derived actinomycete Streptomyces sp. CHQ-64. Their structures including absolute configurations elucidated by spectroscopic methods, X-ray single crystal diffraction analysis, TDDFT ECD calculations. Drimentines (3) showed strong cytotoxicity against human cancer cells lines IC50's down to 1.01 μM, while 1 2 no...
Two new sesquiterpenes, microsphaeropsisin B (1) and C (2), two de-O-methyllasiodiplodins, (3R, 7R)-7-hydroxy-de-O-methyllasiodiplodin (4) (3R)-5-oxo-de-O-methyllasiodiplodin (5), together with one natural product (6) twelve known compounds (3, 7-17), were isolated from the co-cultivation of mangrove endophytic fungus Trichoderma sp. 307 aquatic pathogenic bacterium Acinetobacter johnsonii B2. Their structures, including absolute configurations, elucidated by extensive analysis spectroscopic...
Endothelial dysfunction is a critical factor during the initiation of cardiovascular complications in diabetes. Berberine can ameliorate endothelial induced by However, underlying mechanisms remain unclear. The aim this study was to investigate protective effect and mechanism berberine on palmitate-induced human umbilical vein cells (HUVECs). cell viability HUVECs determined MTT assays. Nitric oxide (NO) level production reactive oxygen species (ROS) were supernatants or cultured HUVECs....
// Kathryn E. Ware 1, 2 , Jason A. Somarelli Daneen Schaeffer 3 Jing Li 4 Tian Zhang Sally Park Steven R. Patierno Jennifer Freedman Wen-Chi Foo 8 Mariano Garcia-Blanco 5, 6 Andrew J. Armstrong 2, 7 1 Department of Medicine, Division Medical Oncology, Duke University Center, Durham, NC, USA Genitourinary Cancer Institute, Translational Research, Janssen Research and Development, Spring House, PA, Hematology Wake Forest School Winston-Salem, 5 Molecular Genetics Microbiology, Biochemistry...
CDK8/19 kinases, which mediate transcriptional reprogramming, have become an active target for cancer drug discovery. Several small-molecule inhibitors showed in vivo efficacy and two entered clinical trials, with no significant toxicities reported. However, Clarke et al. (eLife 2016; 5; e20722) found severe systemic toxicity associated potent inhibitors, Cmpd3 (CCT251921) Cmpd4 (MSC2530818), suggested that their was due to on-target effects. Here, we compared five inhibitors: Cmpd3, Cmpd4,...
Breast cancers (BrCas) that overexpress oncogenic tyrosine kinase receptor HER2 are treated with HER2-targeting antibodies (such as trastuzumab) or small-molecule inhibitors lapatinib). However, most patients metastatic + BrCa have intrinsic resistance and nearly all eventually become resistant to therapy. Resistance drugs frequently involves transcriptional reprogramming associated constitutive activation of different signaling pathways. We investigated the role CDK8/19 Mediator kinase, a...