A5034166240- Chemical Synthesis and Analysis
- Asymmetric Synthesis and Catalysis
- Computational Drug Discovery Methods
- Catalytic C–H Functionalization Methods
- Sulfur-Based Synthesis Techniques
- Synthesis and biological activity
- Catalytic Cross-Coupling Reactions
- Synthetic Organic Chemistry Methods
- SARS-CoV-2 and COVID-19 Research
- Multicomponent Synthesis of Heterocycles
- Click Chemistry and Applications
- Cyclopropane Reaction Mechanisms
- Chemical Synthesis and Reactions
- Synthesis of heterocyclic compounds
- Ubiquitin and proteasome pathways
- Nanoplatforms for cancer theranostics
- Synthesis and Biological Evaluation
- Protein Structure and Dynamics
- Synthesis and Characterization of Heterocyclic Compounds
- Protein Degradation and Inhibitors
- Quinazolinone synthesis and applications
- Oxidative Organic Chemistry Reactions
- Synthesis and Catalytic Reactions
- Peptidase Inhibition and Analysis
- Immunotherapy and Immune Responses
Center for Life Sciences
2020-2025
Peking University
2015-2025
Beijing National Laboratory for Molecular Sciences
2018-2025
Wuhan Institute of Technology
2023
Chinese Academy of Medical Sciences & Peking Union Medical College
2020-2022
Qingdao University
2021
Yuhuangding Hospital
2021
State Key Laboratory for Structural Chemistry of Unstable and Stable Species
2018-2020
Academy of Medical Sciences
2020
Tianjin University
2018
Abstract Cellular senescence, a persistent state of cell cycle arrest, accumulates in aged organisms, contributes to tissue dysfunction, and drives age-related phenotypes. The clearance senescent cells is expected decrease chronic, low-grade inflammation improve repair capacity, thus attenuating the decline physical function organisms. However, selective effective different types has proven challenging. Herein, we developed prodrug strategy design new compound based on increased activity...
COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CLpro) of SARS-CoV-2 preferred target broad spectrum anti-coronavirus drug discovery. We studied anti-SARS-CoV-2 activity S. baicalensis its ingredients. found that ethanol extract major component, baicalein, inhibit 3CLpro in vitro with IC50's 8.52 µg/ml 0.39 µM, respectively. Both them replication Vero cells EC50's 0.74 2.9 While baicalein mainly...
Highly infiltrative and invasive glioma cells obscure the boundary between tumor normal brain tissue, making it extremely difficult to precisely diagnose completely remove. The combination of multimodal imaging with effective treatments guide surgery therapy accurately is desperately needed for in brain. Here, we report a biomimetic catalase-integrated-albumin phototheranostic nanoprobe (ICG/AuNR@BCNP) realize imaging, amplify phototherapy, after penetrating blood–brain barrier, accumulating...
Cancer progression and treatment-associated cellular stress impairs therapeutic outcome by inducing resistance. Endoplasmic reticulum (ER) is responsible for core events. Aberrant activation of sensors their downstream components to disrupt homeostasis have emerged as vital regulators tumor well response cancer therapy. Here, an orchestrated nanophotoinducer (ERsNP) results in specific ER-homing, induces hyperthermia mounting oxidative associated reactive oxygen species (ROS), provokes...
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Abstract The COVID-19 pandemic calls for rapid development of effective treatments. Although various drug repurpose approaches have been used to screen the FDA-approved drugs and candidates in clinical phases against SARS-CoV-2, coronavirus that causes this disease, no magic bullets found until now. In study, we directed message passing neural network first build a broad-spectrum anti-beta-coronavirus compound prediction model, which gave satisfactory predictions on newly reported active...
Intrinsically disordered proteins (IDPs) play crucial roles in cellular processes and hold promise as drug targets. However, the dynamic nature of IDPs remains poorly understood. Here, we construct a single-molecule electrical nanocircuit based on silicon nanowire field-effect transistors (SiNW-FETs) functionalize it with an individual c-Myc bHLH-LZ domain to enable label-free, situ, long-term measurements at level. We use device study interaction Max and/or small molecule inhibitors....
Abstract COVID-19 has become a global pandemic that threatens millions of people worldwide. There is an urgent call for developing effective drugs against the virus (SARS-CoV-2) causing this disease. The main protease SARS-CoV-2, 3C-like (3CL pro ), highly conserved across coronaviruses and essential maturation process viral polyprotein. Scutellariae radix (Huangqin in Chinese), root Scutellaria baicalensis been widely used traditional Chinese medicine to treat infection related symptoms....
Abstract Deep generative models have advanced drug discovery but often generate compounds with limited structural novelty, providing constrained inspiration for medicinal chemists. To address this, we develop TransPharmer, a model that integrates ligand-based interpretable pharmacophore fingerprints pre-training transformer (GPT)-based framework de novo molecule generation. TransPharmer excels in unconditioned distribution learning, generation, and scaffold elaboration under pharmacophoric...
Intrinsically disordered proteins or intrinsically regions (IDPs) have gained much attention in recent years due to their vital roles biology and prevalence various human diseases. Although IDPs are perceived as attractive therapeutic targets, rational drug design targeting remains challenging because of conformational heterogeneity. Here, we propose a hierarchical computational strategy for IDP virtual screening (IDPDVS) applied it the discovery p53 transactivation domain I (TAD1) binding...
GPR40 is a G protein-coupled receptor (GPCR) whose endogenous ligands have recently been identified as medium- and long-chain free fatty acids (FFAs), it thought to play an important role in insulin release. Despite recent research efforts, much still remains unclear our understanding of its pharmacology, mainly because the receptor-ligand interaction has not analyzed directly. To study pharmacology more direct fashion, we developed flow cytometry-based binding assay. FLAG-tagged protein was...
We here report a unique and efficient copper bromide mediated pallado-catalyzed coupling of protecting group-free 2-thiouracil derivatives with organostannanes. The nature the appears to be crucial for successful cross coupling.
The efficient asymmetric Michael addition reactions of aryl methyl ketones with 2-furanones were catalyzed by a simple and commercially available chiral 1,2-diphenyl-1,2-ethanediamine p-TSA·H2O as cocatalyst good yields (up to 95%) excellent enantioselectivities >99% ee). A bi-functional catalytic mechanism for the reaction was proposed.
Abstract A copper‐catalyzed cascade dehydrogenative and dehalogenative reaction of halogenated 6‐phenyl‐4,5‐dihydropyridazin‐3(2 H )‐ones to 6‐phenylpyridazin‐3(2 has been developed. Moreover, the catalytic system consisting copper(II) acetate/sodium carbonate/pyridine exhibits high reactivity selectivity with oxygen as terminal oxidant.
A Pd-catalyzed Cu-mediated desulfurative Sonogashira cross-coupling reaction of thioamide-type quinolone derivatives was proposed for the construction C<sub>sp</sub><sup>2</sup>–C<sub>sp</sub> bonds.