A5014795145- Advanced Photocatalysis Techniques
- Ga2O3 and related materials
- Hippo pathway signaling and YAP/TAZ
- Catalytic C–H Functionalization Methods
- Neurotransmitter Receptor Influence on Behavior
- Synthesis and Catalytic Reactions
- Lymphoma Diagnosis and Treatment
- Cancer therapeutics and mechanisms
- Computational Drug Discovery Methods
- Vanadium and Halogenation Chemistry
- Synthesis and biological activity
- Receptor Mechanisms and Signaling
- ZnO doping and properties
- Chromatin Remodeling and Cancer
- Neuroscience and Neuropharmacology Research
- Protein Degradation and Inhibitors
Chinese Academy of Medical Sciences & Peking Union Medical College
2024
Sichuan University
2016
West China Hospital of Sichuan University
2016
Discovery of the first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for treatment Burkitt lymphoma.
Enhancing the selectivity of alpha2-adrenoceptor (α2A-AR) agonists remains an unresolved issue. Herein, we reported design α2A-AR agonist using conformation constraint method, beginning with medetomidine. The structure–activity relationship indicated that 8-substituent chromane derivatives exerted most pronounced effect on agonistic activity. Compounds A9 and B9 were identified as promising, exhibiting EC50 values 0.78 0.23 nM, respectively. Their indexes surpassed dexmedetomidine (DMED) by...
Interferon regulatory factor-7 (IRF-7) is involved in pulmonary infection and pneumonia. Here, a synthetic strategy that combined quantitative structure–activity relationship (QSAR)-based virtual screening vitro binding assay was described to identify new potent mediator ligands of IRF-7 from natural products. In the procedure, QSAR scoring function developed validated using Gaussian process (GP) regression structure-based set protein–ligand affinity data. By integrating hotspot pocket...
Regioselective benzanilide bromination that generates either regioisomer from the same starting material is desirable. Herein, we develop switchable site-selective C(sp2)-H by promoter regulation. This protocol leads to regiodivergent brominated single substrate via selection of promoters. The demonstrates excellent regioselectivity and good tolerance functional groups with high yields. utility effectiveness this method has been well exemplified in late-stage modification biologically...