A5032103164- Photochemistry and Electron Transfer Studies
- Free Radicals and Antioxidants
- Carbohydrate Chemistry and Synthesis
- Mycobacterium research and diagnosis
- Ubiquitin and proteasome pathways
- Glycosylation and Glycoproteins Research
- Endoplasmic Reticulum Stress and Disease
- Porphyrin and Phthalocyanine Chemistry
- Microbial Natural Products and Biosynthesis
- Histone Deacetylase Inhibitors Research
- Spectroscopy and Quantum Chemical Studies
- Luminescence and Fluorescent Materials
- Photochromic and Fluorescence Chemistry
- Cancer therapeutics and mechanisms
- Pharmacological Effects of Natural Compounds
- Synthesis and biological activity
- Fungal Biology and Applications
- Chemical Synthesis and Analysis
- PI3K/AKT/mTOR signaling in cancer
- Cellular transport and secretion
- Synthesis and Biological Evaluation
- Radical Photochemical Reactions
- Bacteriophages and microbial interactions
- Molecular Sensors and Ion Detection
- Drug Solubulity and Delivery Systems
Liaoning University
2017-2025
Ball State University
2019-2025
Yuxi Normal University
2018-2024
University of Cambridge
2023
University of Surrey
2023
Wuhan University
2018-2022
Renmin Hospital of Wuhan University
2018-2022
Beijing Friendship Hospital
2021-2022
Capital Medical University
2021-2022
Beijing Luhe Hospital Affiliated to Capital Medical University
2020
Tumor-associated macrophages (TAM) are prominent components of tumor microenvironment (TME) and capable promoting cancer progression. However, the mechanisms for formation M2-like TAMs remain enigmatic. Here, we show that lactate is a pivotal oncometabolite in TME drives macrophage M2-polarization to promote breast proliferation, migration, angiogenesis. In addition, identified activation ERK/STAT3, major signaling molecules pathway, deepens our molecular understanding how educates TAMs....
// Xianmin Mu 1, * , Ting Zhao Che Xu 1 Wei Shi 4 Biao Geng Jiajia Shen 2 Chen Zhang Jinshun Pan Jing Yang Hu Yuanfang Lv Hao Wen Qiang You 3 Department of Biotherapy, Second Affiliated Hospital, Nanjing Medical University, Nanjing, Jiangsu 210011, China Surgery, Immunology, 211166, Drug Screening and Evaluation, Chia Tai Tianqing Pharmaceutical Group Co., Ltd, 210023, These authors have contributed equally to this work Correspondence to: You, email: Qiang.You@njmu.edu.cn Keywords:...
Significance Tumors promote angiogenesis to facilitate their growth and metastasis; thus, inhibition of is a promising strategy for treating cancer. During angiogenesis, endothelial cells (EC) are stimulated by proangiogenic factors proliferate migrate, leading the formation new blood vessels. Understanding mechanisms regulating EC function therefore essential development antiangiogenic interventions. Here, we identify novel mechanism regulation recently discovered inhibitor itraconazole,...
Ipomoeassin F is a potent natural cytotoxin that inhibits growth of many tumor cell lines with single-digit nanomolar potency. However, its biological and pharmacological properties have remained largely unexplored. Building upon our earlier achievements in total synthesis medicinal chemistry, we used chemical proteomics to identify Sec61α (protein transport protein Sec61 subunit alpha isoform 1), the pore-forming translocon, as direct binding partner ipomoeassin living cells. The...
Abstract The heterotrimeric Sec61 complex is a major site for the biogenesis of transmembrane proteins (TMPs), accepting nascent TMP precursors that are targeted to endoplasmic reticulum (ER) by signal recognition particle (SRP). Unlike most single-spanning membrane proteins, integration type III TMPs completely resistant small molecule inhibitors translocon. Using siRNA-mediated depletion specific ER components, in combination with potent inhibitor ipomoeassin F (Ipom-F), we show utilise...
The proton transfer reaction in methyl 5-R-salicylate is found to be highly sensitive the presence of specific substituents resonance with hydroxyl group, leading different fluorescence behaviors substituents.
The antifungal drug itraconazole was recently found to exhibit potent antiangiogenic activity and has since been repurposed as an investigational anticancer agent. Itraconazole shown exert its through inhibition of the mTOR signaling pathway, but molecular mechanism action unknown. We identified mitochondrial protein VDAC1 a target mediator activation AMPK, upstream regulator mTOR. However, could not account for previously reported cholesterol trafficking by itraconazole, which also...
The ESIPT-fluorescence deactivation is caused by ISC and phosphorescence.
Ipomoeassin F, a macrolide glycoresin containing an embedded disaccharide, possesses potent in vitro antitumor activity with unknown mechanism of function. It inhibits tumor cell growth single-digit nanomolar IC50 values, superior to many clinical chemotherapeutic drugs. To facilitate translation its bioactivity into protein function for drug development, we report here new synthesis the gram-scale production ipomoeassin F (3.8% over 17 linear steps) from commercially available starting...
Chaihu Shugan San (CSS) is a common antidepressant prescription in traditional Chinese medicines. However, its active ingredients and mechanisms are unknown. The aim of this study was to explore the potential pharmacological CSS for treatment major depressive disorder (MDD).Active compounds were screened using Traditional Medicine Systems Pharmacology database. Compound-related targets retrieved SwissTargetPrediction MDD-related determined DisGeNET, Therapeutic Target Database DrugBank...
Different substituents and benzene ring numbers had significant effects on the fluorescence phenomenon of 2-aryloxazoline derivatives as observed in an experiment. Here, we select five with different (2u, 2ad, 2af, 2ai, 2ah) to analyze phenomena. For 2ah, first, geometric structures are optimized based density functional theory time-dependent methods. The analysis obtained bond parameters reveals variation hydrogen interactions from S0 S1 states. Second, calculated absorption emission...
ABSTRACT In order to produce proteins essential for their propagation, many pathogenic human viruses, including SARS-CoV-2, the causative agent of COVID-19 respiratory disease, commandeer host biosynthetic machineries and mechanisms. Three major structural proteins, spike, envelope membrane are amongst several SARS-CoV-2 components synthesised at endoplasmic reticulum (ER) infected cells prior assembly new viral particles. Hence, inhibition protein synthesis ER is an attractive strategy...
Many methyl benzoate derivatives were found to show intramolecular charge transfer (ICT), proton transfer, and other properties, which have extensive applications in lasing media, metal ion sensors, active materials, fluorescence probe fields. However, the intrinsic relationship reaction mechanism between excited-state (ESIPT) ICT with different substituents not been explained. In this paper, density functional theory time-dependent methods used study ESIPT behaviors of p-aminosalicylic acid...
Ipomoeassin F (Ipom-F) is a plant-derived macrocyclic resin glycoside that potently inhibits cancer cell growth through blockage of Sec61-mediated protein translocation at the endoplasmic reticulum. Recently, detailed structural information on how Ipom-F binds to Sec61α was obtained using Cryo-EM, which discovered polar interactions between asparagine-300 (N300) in and four oxygens are crucial. One from carbonyl group C-4 fatty acid chain. In contrast, our previous structure–activity...
The drivers of tissue necrosis in Mycobacterium ulcerans infection (Buruli ulcer disease) have historically been ascribed solely to the directly cytotoxic action diffusible exotoxin, mycolactone. However, its role clinically evident vascular component disease aetiology remains poorly explained. We now dissected mycolactone’s effects on human primary endothelial cells vitro. show that mycolactone-induced changes morphology, adhesion, migration, and permeability are dependent at Sec61...