A5046699631- Ubiquitin and proteasome pathways
- Peptidase Inhibition and Analysis
- Multiple Myeloma Research and Treatments
- Glycosylation and Glycoproteins Research
- Genetic factors in colorectal cancer
- Protein Degradation and Inhibitors
- Lung Cancer Treatments and Mutations
- Natural Compounds in Disease Treatment
- Cancer therapeutics and mechanisms
- Cancer, Lipids, and Metabolism
- Colorectal Cancer Treatments and Studies
- Genetics and Neurodevelopmental Disorders
- HER2/EGFR in Cancer Research
Shanxi Medical University
2024
Nanjing Forestry University
2016-2020
A series of novel dipeptidyl boronic acid compounds were designed, synthesized and biologically investigated for the inhibition β5 subunit 20S proteasome several showed high activities with IC50 values less than 10 nM. Some these potently inhibited multiple myeloma (MM) cancer cell lines It was reported that both β2 subunits strongly increased cytotoxicity inhibitors in solid tumor cells, so some evaluated triple-negative breast line MDA-MB-231. The results three active vivo pharmacokinetic...
Abstract Background Proteasome inhibition demonstrates highly effective impact on multiple myeloma (MM) treatment. Here, we aimed to examine anti-tumor efficiency and underlying mechanisms of a novel well tolerated orally applicable proteasome inhibitor NNU546 its hydrolyzed pharmacologically active form NNU219. Methods Enzyme activities assays was performed evaluate the effect NNU219 proteasome. To explore anti-MM activity related mechanism, in vitro such as cell viability, cycle apoptosis...
Colorectal cancer (CRC) is one of the most common digestive tract malignant tumors, which has a high mortality rate especially for patients with CRC recurrence. However, pathological mechanism recurrence unclear. In this study, we integrated multiple cohort datasets and databases to clarify verify potential key candidate biomarkers signal transduction pathways in CRC. As results, 628 DEGs were identified from GSE33113 GSE2630 their function pathway analyzed. 14 hub genes related screened...
Proteasome inhibition demonstrates highly effective impact on multiple myeloma (MM) treatment.Here, we aimed to examine anti-tumor efficiency and underlying mechanisms of a novel well tolerated orally applicable proteasome inhibitor NNU546 its hydrolyzed pharmacologically active form NNU219. NNU219 showed more selective catalytic subunits less off-target effect than bortezomib ex vivo.Moreover, intravenous oral administration either or led sustained pharmacodynamic inhibitions activities...