A5023846352- Cancer Immunotherapy and Biomarkers
- Peptidase Inhibition and Analysis
- Protein Degradation and Inhibitors
- Immune Cell Function and Interaction
- Histone Deacetylase Inhibitors Research
- CAR-T cell therapy research
- Immunotherapy and Immune Responses
- Cancer-related gene regulation
- Cancer therapeutics and mechanisms
- Synthesis and Biological Evaluation
- Epigenetics and DNA Methylation
- Synthesis and biological activity
- Immune cells in cancer
- Advanced biosensing and bioanalysis techniques
- DNA Repair Mechanisms
- RNA Interference and Gene Delivery
- Ubiquitin and proteasome pathways
- Click Chemistry and Applications
- Nanoplatforms for cancer theranostics
- Quinazolinone synthesis and applications
- Slime Mold and Myxomycetes Research
- Eicosanoids and Hypertension Pharmacology
- Melanoma and MAPK Pathways
- RNA Research and Splicing
- Synthesis of heterocyclic compounds
Hubei Polytechnic University
2021-2025
Lishui University
2025
Indiana University School of Medicine
2025
Second Military Medical University
2025
Wenzhou Medical University
2024
Lishui City People's Hospital
2024
Southern Medical University
2018-2021
University of California, San Diego
2016-2019
Jinggangshan University
2016
Shanghai Institute for Science of Science
2010
Novel indazole and benzimidazole analogues were designed synthesized as tubulin inhibitors with potent antiproliferative activities. Among them, compound 12b exhibited the strongest inhibitory effects on growth of cancer cells an average IC50 value 50 nM, slightly better than colchicine. nearly equal potency against both, a paclitaxel-resistant cell line (A2780/T, = 9.7 nM) corresponding parental (A2780S, 6.2 nM), thus effectively overcoming paclitaxel resistance in vitro. The crystal...
A series of novel PD-L1/HDAC6 dual inhibitors were designed and synthesized, compound HP29 was identified as the most potent candidate, which demonstrated excellent selective HDAC6 inhibitory activity (IC50 = 78 nM, SI > 1282), high anti-PD-1/PD-L1 26.8 nM). Further studies showed that could bind with affinity to PD-L1 protein. Furthermore, possessed favorable in vivo pharmacokinetic properties, such decent oral bioavailability (F 15.3%). Moreover, exhibited significant antitumor efficacy a...
Novel small molecule compounds based on various scaffolds including chalcone, flavonoid, and resorcinol dibenzyl ether were designed tested for their inhibitory activity against the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) pathway. Among them, compound NP19 inhibited human PD-1/PD-L1 interaction with IC50 values of 12.5 nM in homogeneous time-resolved fluorescence (HTRF) binding assays. In addition, dose-dependently elevated IFN-γ production a coculture model...
In this work, a series of bifunctional PD-L1/CD73 (cluster differentiation 73) small-molecule inhibitors were designed and synthesized. Among them,
A series of programmed cell death-1 (PD-1)/programmed death ligand 1 (PD-L1) inhibitors based on the resorcinol diphenyl ether scaffold were discovered by incorporating hydrophilic moieties into side chain and converting corresponding hydrochloride salt. Among these compounds,
In this work, we rationally designed, synthesized, and evaluated a series of novel d-(+)-biotin-conjugated PD-L1 inhibitors for targeted cancer therapy. Among them, SWS1 exhibited the highest anti-PD-1/PD-L1 activity with an IC50 1.8 nM. addition, dose-dependently promoted tumor cell death in HepG2/Jurkat co-culture model. Importantly, displayed high antitumor efficacy B16-F10 mouse model growth inhibition 66.1%, which was better than that P18 (44.3%). Furthermore, exerted effects by...
A new biosensor was engineered to visualize Lck kinase preactivation and regulation in live T cells.