A5100415336- Catalytic C–H Functionalization Methods
- Radical Photochemical Reactions
- Sulfur-Based Synthesis Techniques
- Synthesis and Catalytic Reactions
- Fluorine in Organic Chemistry
- Cancer-related gene regulation
- Chemical Synthesis and Analysis
- Epigenetics and DNA Methylation
- Oxidative Organic Chemistry Reactions
- Catalytic Cross-Coupling Reactions
- Nanoparticle-Based Drug Delivery
- RNA Interference and Gene Delivery
- Asymmetric Hydrogenation and Catalysis
- Synthetic Organic Chemistry Methods
- Chemical Synthesis and Reactions
- Cyclopropane Reaction Mechanisms
- Asymmetric Synthesis and Catalysis
- Carbohydrate Chemistry and Synthesis
- Enzyme Catalysis and Immobilization
- Glycosylation and Glycoproteins Research
- Drug Transport and Resistance Mechanisms
- Cancer therapeutics and mechanisms
- Inflammasome and immune disorders
- Catalytic Alkyne Reactions
- RNA modifications and cancer
Soochow University
2016-2025
Kunming Institute of Precious Metals
2023-2025
Central South University
2009-2025
Hunan University
2022-2025
State Key Laboratory of Chemobiosensing and Chemometrics
2025
Tsinghua–Berkeley Shenzhen Institute
2025
Second Xiangya Hospital of Central South University
2025
Buchang Pharma (China)
2022-2025
Xi'an Jiaotong University
2011-2025
Shaanxi Institute of International Trade & Commerce
2022-2025
EZH2 or EZH1 is the catalytic subunit of polycomb repressive complex 2 that catalyzes methylation histone H3 lysine 27 (H3K27). The trimethylation H3K27 (H3K27me3) a transcriptionally post-translational modification. Overexpression and hypertrimethylation have been implicated in number cancers. Several selective inhibitors reported recently. Herein we disclose UNC1999, first orally bioavailable inhibitor has high vitro potency for wild-type mutant as well EZH1, closely related...
Among epigenetic "writers", "readers", and "erasers", the lysine methyltransferases G9a GLP, which catalyze mono- dimethylation of histone H3 9 (H3K9me2) nonhistone proteins, have been implicated in a variety human diseases. A "toolkit" well-characterized chemical probes will allow biological disease hypotheses concerning these proteins to be tested cell-based animal models with high confidence. We previously discovered potent selective G9a/GLP inhibitors including cellular probe UNC0638,...
Cerebral ischemia–reperfusion injury (CIRI), a cause of cerebral dysfunction during infarction treatment, is closely associated with mitochondrial viscosity and hydrogen peroxide (H2O2). However, the accurate measurement H2O2 levels in CIRI challenging because lack sufficient selectivity blood–brain barrier (BBB) penetration existing monitoring tools related to CIRI, hampering exploration role CIRI. To address this issue, we designed an activatable fluorescent probe, mitochondria-targeting...
SAR exploration of the 2,4-diamino-6,7-dimethoxyquinazoline template led to discovery 8 (UNC0224) as a potent and selective G9a inhibitor. A high resolution X-ray crystal structure G9a-8 complex, first cocrystal with small molecule inhibitor, was obtained. The validated our binding hypothesis will enable structure-based design novel inhibitors. is useful tool for investigating biology its roles in chromatin remodeling.
Protein lysine methyltransferase G9a, which catalyzes methylation of 9 histone H3 (H3K9) and 373 (K373) p53, is overexpressed in human cancers. Genetic knockdown G9a inhibits cancer cell growth, the dimethylation p53 K373 results inactivation p53. Initial SAR exploration 2,4-diamino-6,7-dimethoxyquinazoline template represented by 3a (BIX01294), a selective small molecule inhibitor GLP, led to discovery 10 (UNC0224) as potent with excellent selectivity. A high resolution X-ray crystal...
Here we described a paclitaxel (PTX) nanocrystal formulation using d-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) as the sole excipient for overcoming multidrug resistance (MDR), key challenge in current cancer therapy. To best of our knowledge, it is first report on PTX nanocrystals which can reverse MDR. TPGS serves surfactant to stabilize and P-gp inhibitor The size morphology were studied by transmission electron microscopy, crystalline structure was determined powder X-ray...
Protein lysine methyltransferase G9a plays key roles in the transcriptional repression of a variety genes via dimethylation 9 on histone H3 (H3K9me2) chromatin as well nonhistone proteins including tumor suppressor p53. We previously reported discovery UNC0321 (3), most potent inhibitor to date, structure-based design and structure-activity relationship (SAR) exploration quinazoline scaffold represented by BIX01294 (1). Despite its very high vitro potency, compound 3 lacks sufficient...
Chromatin modulators are emerging as attractive drug targets, given their widespread implication in human cancers and susceptibility to pharmacological inhibition. Here we establish the histone methyltransferase G9a/EHMT2 a selective regulator of fast proliferating myeloid progenitors with no discernible function hematopoietic stem cells (HSCs). In mouse models acute leukemia (AML), loss G9a significantly delays disease progression reduces cell (LSC) frequency. We connect this its activity...
Targeted delivery remains the major challenge for application of small interfering RNA (siRNA). We have developed a lipid/calcium/phosphate (LCP) nanoparticle (NP) to improve siRNA efficiency. The LCP NP was prepared by using microemulsion technology form calcium/phosphate (CaP) core and further coated with cationic lipids. final grafted polyethylene glycol (PEG) anisamide (AA) ligand on surface target sigma receptor-expressing B16F10 melanoma cells. exhibited 40 nm particle size, +25 mV...
Copper-catalyzed direct conversion of benzylic alcohols to aryl nitriles was realized using NH3(aq.) as the nitrogen source, O2 oxidant and TEMPO co-catalyst. Furthermore, copper-catalyzed one-pot synthesis primary amides from also achieved.
Multifunctional membrane-core nanoparticles, composed of calcium phosphate cores, arginine-rich peptides, cationic and PEGylated lipid membranes, galactose targeting ligands, have been developed as synthetic vectors for efficient nuclear delivery plasmid DNA subsequent gene expression in hepatocytes vivo. Targeted particles exhibited rapid extensive hepatic accumulation were predominantly internalized by hepatocytes, while the inclusion such peptides LCP was sufficient to elicit high degrees...
A convenient and practical protocol is developed for radical vicinal difunctionalization of unactivated alkenes under transition-metal-free conditions.
The key property of protein–nanoparticle conjugates is the bioactivity protein. ability to accurately modulate activity protein on nanoparticles at interfaces important in many applications. In work reported here, modulation protein–gold nanoparticle (AuNP) by specifically orienting and varying surface density was investigated. Different orientations were achieved introducing cysteine (Cys) residues specific sites for binding gold. We chose Escherichia coli inorganic pyrophosphatase (PPase)...
A redox-neutral, mild, and simple protocol is developed for the synthesis of α-trifluoromethylated ketones from vinyl azides upon visible-light irradiation.
A mild and simple protocol is developed for the synthesis of terminal alkenes <italic>via</italic> site-specific C–C bond formation upon visible-light irradiation.
Minimizing energy loss is crucial for breaking through the efficiency bottleneck of organic solar cells (OSCs). The main mechanism can be attributed to non-radiative recombination (ΔEnr) that occurs due exciton-vibration coupling. To tackle this challenge, tuning intramolecular noncovalent interactions strategically utilized tailor novel fused ring electron acceptors (FREAs). Upon comprehensive analysis both theoretical and experimental results, approach effectively enhance molecular...