A5052314053- Nanoparticle-Based Drug Delivery
- Cancer Genomics and Diagnostics
- Epigenetics and DNA Methylation
- Wnt/β-catenin signaling in development and cancer
- Cancer-related gene regulation
- Cancer-related Molecular Pathways
- Synthesis and biological activity
- Genomics and Rare Diseases
- Berberine and alkaloids research
- Click Chemistry and Applications
- Advanced Drug Delivery Systems
- RNA Interference and Gene Delivery
- Vitamin C and Antioxidants Research
- Genetic factors in colorectal cancer
- Cancer, Hypoxia, and Metabolism
- Metabolism, Diabetes, and Cancer
- Synthesis of Organic Compounds
- Cancer Mechanisms and Therapy
- Alkaloids: synthesis and pharmacology
- Synthesis and Characterization of Heterocyclic Compounds
- Aldose Reductase and Taurine
- Diet, Metabolism, and Disease
- Cancer therapeutics and mechanisms
- Bioinformatics and Genomic Networks
- Genetics and Neurodevelopmental Disorders
Markey Cancer Center
2017-2024
University of Kentucky
2017-2024
State Key Laboratory of Natural and Biomimetic Drugs
2019
Peking University
2019
Sun Yat-sen University
2013-2018
Beijing University of Chemical Technology
2016
Zhejiang University
2013
p53 is the most frequently mutated tumor-suppressor gene in human cancers. It has been reported that mutations result not only loss of its ability as a tumor suppressor, but also gain novel cancer-related functions contribute to oncogenesis. The present study evaluated potential silencing mutant by small interfering RNA treatment bladder cancer cells vitro.We used 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay assess cell viability and flow cytometry detect cycle...
Cancer cells undergo a significant level of “metabolic reprogramming” or “remodeling” to ensure an adequate supply ATP and “building blocks” for cell survival facilitate accelerated proliferation. preferentially use glycolysis production (the Warburg effect); however, cancer cells, including colorectal (CRC) also depend on oxidative phosphorylation (OXPHOS) production, finding that suggests both OXPHOS play roles in facilitating progression Our prior studies identified semisynthetic...
A novel berberine-mediated mitochondria-targeting nano-platform was constructed to inhibit tumor growth and bypass the multi-drug resistance problem by targeting doxorubicin mitochondria of cells.
Abstract Cancer cells undergo significant “metabolic remodeling” to provide sufficient ATP maintain cell survival and promote rapid growth. In colorectal cancer cells, is produced by mitochondrial oxidative phosphorylation substantially elevated cytoplasmic glucose fermentation (i.e., the Warburg effect). Glucose transporter 1 (GLUT1) expression significantly increased in GLUT1 inhibitors block uptake hence glycolysis crucial for addition ATP, these metabolic pathways also macromolecule...
This research aims to synthesize lipophilic berberine derivatives and evaluate their antiglioma effects on C6 U87 cells.
Cytisine-linked isoflavonoids (CLIFs) inhibit cancer cells by targeting the peroxisomal enzyme HSD17B4.
Development of high drug-loading nanomicelles targeting steroids to the brain Sijia Zheng,1,* Yanqi Xie,1,* Yuan Li,1 Ling Ning Tian,1 Wenbo Zhu,2 Guangmei Yan,2 Chuanbin Wu,1 Haiyan Hu1 1School Pharmaceutical Sciences, 2Department Pharmacology, Zhongshan School Medicine, Sun Yat-sen University, Guangzhou, People's Republic China *These authors contributed equally this workAbstract: The objective research was develop and evaluate ligand-modified deliver a steroidal compound brain. YC1...
The importance of upregulated Wnt signaling in colorectal cancers led to efforts develop inhibitors that target β-catenin this pathway. We now report several "Wnt inhibitors" allegedly actually function as mitochondrial proton uncouplers independently activate AMPK and concomitantly inhibit signaling. As expected for a process which uncoupling diminishes ATP production, uncoupler, FCCP, glucose metabolic inhibitor, 2-DG, activated inhibited Also consistent with these findings, well-known...
Abstract Structure-activity relationships (SAR) in the aurone pharmacophore identified heterocyclic variants of ( Z )-2-benzylidene-6-hydroxybenzofuran-3(2 H )-one scaffold that possessed low nanomolar vitro potency cell proliferation assays using various cancer lines, vivo prostate PC-3 xenograft and zebrafish models, selectivity for colchicine-binding site on tubulin, absence appreciable toxicity. Among leading, biologically active analogs were )-2-((2-((1-ethyl-5-methoxy-1...
Aberrant activation of Wnt signaling triggered by mutations in either Adenomatous Polyposis Coli (APC) or CTNNB1 (β-catenin) is a hallmark colorectal cancers (CRC). As part program to develop epigenetic regulators for cancer therapy, we developed carboxamide-substituted benzhydryl amines (CBAs) bearing aryl heteroaryl groups that selectively targeted histone lysine demethylases (KDMs) and functioned as inhibitors the pathway. A biotinylated variant N-((5-chloro-8-hydroxyquinolin-7-yl)...
Abstract The development of cancer involves the accumulation somatic mutations in a number key biological pathways. Delineating order pathway during tumorigenesis is very important to understand mechanisms and inform new therapeutic targets. A statistical computational methods have been proposed for estimating based on mutation profile data from cohort patients. However, one major issue current that they do not account intra-tumor heterogeneity (ITH), which limits their abilities accurately...
Cancer somatic driver mutations associated with genes within a pathway often show mutually exclusive pattern across cohort of patients. This mutational signal has been frequently used to distinguish from passenger and investigate relationships among mutations. Current methods for de novo discovery patterns are limited because the heterogeneity in background mutation rate can confound patterns, presence highly mutated lead spurious patterns. In addition, most only focus on number pre-selected...
In recent years, specific transportation mechanisms on the blood–brain barrier (BBB) are extensively employed for brain-targeted drug delivery via colloidal nanocarriers. However, in this study, we purposed to exploit sodium-dependent vitamin C transporter 2 (SVCT2)-mediated blood–cerebrospinal fluid enhance central nervous system penetration of highly hydrophilic ibuprofen (IBU) by synthesizing a SVCT2-targeted chemical (CDS), ibuprofen-C6-O-ascorbic acid (IAA). The physicochemical...
Abstract Developing effective treatments for colorectal cancers through combinations of small-molecule approaches and immunotherapies present intriguing possibilities managing these otherwise intractable cancers. During a broad-based, screening effort against multiple cancer cell lines, we identified indole-substituted quinolines (ISQ), such as N7,N7-dimethyl-3-(1-methyl-1H-indol-3-yl)quinoline-2,7-diamine (ISQ-1), potent in vitro inhibitors several lines. We found that ISQ-1 inhibited Wnt...
Fluorinated, phenylethynyl-substituted heterocycles that possessed either an N-methylamino or N,N-dimethylamino group attached to including pyridines, indoles, 1H-indazoles, quinolines, and isoquinolines inhibited the proliferation of LS174T colon cancer cells in which inhibition cyclin D1 induction cyclin-dependent kinase inhibitor-1 (i.e., p21Wif1/Cip1) served as a readout for antineoplastic activity at cellular level. On molecular level, these agents, particularly...
The development of cancer involves the accumulation somatic mutations in several essential biological pathways. Delineating temporal order pathway during tumorigenesis is crucial for comprehending mechanisms underlying and identifying potential targets therapeutic intervention. Several computational statistical methods have been introduced estimating based on mutation profile data from a cohort patients. However, one major issue current that they do not take into account intra-tumor...
Despite progress, the combination therapy of a nanoscale delivery system and its loaded drug to increase efficiency anticancer treatment still remains challenge. In this study, taking advantage ascorbic acid with activity, complex nanovehicles were designed constructed by co-assembly amphiphilic block polymers poly(ascorbyl acrylate)-block-poly(lactic acid) (PAA-b-PLA) maleimide-decorating poly(ethylene glycol)-block-poly(lactic (Mal-PEG-b-PLA) in aqueous solution. The nanoparticles' large...
Objective Larotaxel is a new chemical structure drug, which has not been marketed worldwide. Accordingly, the standard identification and quantification methods for larotaxel remain unclear. The spectrometric analyses were performed verifying weight molecular formula, of larotaxel. Besides, method was developed measuring in liposomes. Methods studied by using mass spectrometry (MS), infra-red (IR), nuclear magnetic resonance (NMR) ultraviolet-visible (UV-vis) techniques. absorption...
Although high-throughput, cancer cell-line screening is a time-honored, important tool for anti-cancer drug development, this process involves the testing of each, individual in cell-line. Despite availability robotic liquid handling systems, remains time-consuming and costly investment. The Broad Institute developed new method called Profiling Relative Inhibition Simultaneously Mixtures (PRISM) to screen mixture barcoded, tumor cell-lines. methodology significantly improved efficiency large...
Abstract In an effort to screen natural compounds and their derivatives as novel agents for cancer treatment, we developed two semisynthetic nature compounds, A14 A52, which have potencies in vitro cell proliferation studies against LS174T PC-3 cells the mid-nanomolar range. inhibited more than 90% of around 300 nM also vivo prostate xenografts nude mice. Cell morphology comparisons with known antineoplastic suggested that disrupted microtubule organization. tubulin polymerization assay this...