A5103835664- Ubiquitin and proteasome pathways
- Peptidase Inhibition and Analysis
- Multiple Myeloma Research and Treatments
- Nanoparticle-Based Drug Delivery
- Nanoplatforms for cancer theranostics
- Endoplasmic Reticulum Stress and Disease
- RNA Interference and Gene Delivery
- Glycosylation and Glycoproteins Research
- Retinoids in leukemia and cellular processes
- Genetics and Neurodevelopmental Disorders
- Protein Degradation and Inhibitors
- Extracellular vesicles in disease
- Analysis of environmental and stochastic processes
- Cancer Mechanisms and Therapy
- Photodynamic Therapy Research Studies
- Fluorine in Organic Chemistry
- Ginseng Biological Effects and Applications
- Neuroblastoma Research and Treatments
- Immune cells in cancer
- Graphene and Nanomaterials Applications
- Evaluation and Optimization Models
- Biological Activity of Diterpenoids and Biflavonoids
- Drug Transport and Resistance Mechanisms
- Technology Assessment and Management
- Adenosine and Purinergic Signaling
Nanjing Forestry University
2016-2025
Northwest University
2018
Qingdao University
2018
Xidian University
2010
Simcere Pharmaceutical (China)
2009
Hefei First People's Hospital
1990
Multidrug resistance (MDR) remains one of the major reasons for inefficiency many chemotherapeutic agents in cancer therapy. In this study, a D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) and polylysine-deoxycholic acid copolymer (PLL-DA) co-modified cationic liposome coating with hyaluronic (HA) was constructed co-delivery paclitaxel (PTX) chemosensitizing agent, sorafenib (SOR) to treat MDR cancer. The multifunctional (HA-TPD-CL-PTX/SOR) presented good stability against rat...
An extensive structure-activity relationship (SAR) study of 72 dipeptidyl boronic acid proteasome inhibitors constructed from β-amino acids is reported. SAR analysis revealed that bicyclic groups at the R¹ position, 3-F substituents R² and bulky aliphatic R³ position were favorable to activities. Enzymatic screening results showed compound 78, comprising all these features, was most active inhibitor against 20S human less than a 2 nM level, as marketed drug bortezomib. Cellular assays...
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...
Preparation of MF-FA nanoparticles and the release behavior drugs in tumor cells.
VCP/p97 plays an important role in endoplasmic reticulum related degradation pathways, and inhibition of p97 was shown to induce ER stress subsequently cell death a variety solid tumors hematoma. For acute myeloid leukemia (AML) cells, activity leads the accumulation ubiquitylated proteins, activation unfolded protein response (UPR) apoptosis. We have designed synthesized series novel 5,6,7,8-tetrahydropyridine[2,3-d]pyrimidine derivatives. After synthesizing all target compounds, optimal...
Background: Submucosal laryngeal carcinoma (SLC) is a rare subtype of transglottic (TLC) and usually originates from the center ventricle. Nearly 70% TLC cases are confined to larynx 30% show external infiltrations. Early stage asymptomatic shows occult lesions tends grow into lateral parapharyngeal space. Case Summary: We present an unusual case submucosal moderately poor differentiated squamous cell (SCC) characterized by thyroid mass, hoarseness, dyspnea as main symptoms. In this case,...
A 3D pharmacophore model had been generated for a series of dipeptide proteasome inhibitors containing boron atoms using Catalyst. data set consisting 24 was selected on the basis information content structures and activity as required by Catalyst/HypoGen program. The built able to predict other known not included in generation. Based analysis best hypotheses, some novel were designed predicted. Three boronic acid SMNT 1, 2, 3, synthesized biologically assayed. It turned out that three...
Triple‐negative breast cancer (TNBC) is an aggressive subtype, which has poor prognosis due to the lack of effective targeted drugs. KPT‐330, inhibitor nuclear export protein CRM‐1, been widely used in clinical medicine. Y219, a novel proteasome designed by our group, shows superior efficacy, reduced toxicity, and off‐target effects as compared bortezomib. In this study, we investigated synergistic effect KPT‐330 Y219 against TNBC cells, well underlying mechanisms. We report that combination...
FHND6091, a novel N-capped dipeptidyl boronic acid proteasome inhibitor with promising pharmacological properties, entirely converted into active form FHND6081 under physiological conditions. The proteasome, key component of the ubiquitin-proteasome pathway (UPP), has emerged as validated target multiple myeloma (MM) therapeutics. FHND6091 is selective oral that binds irreversibly to β5 submit 20S and exerts anti-cancer roles. In this study, we investigated metabolic stability, metabolite...
Abstract Carfilzomib, a second-generation proteasome inhibitor, has significantly improved the survival rate of multiple myeloma (MM) patients, but its clinical application is still restricted by drug resistance and cardiotoxicity. Here, we identified novel D395, assessed efficacy in treating MM as well cardiotoxicity at preclinical level. The activities purified intracellular proteasomes were measured to determine effect D395 on proteasome. CCK-8 flow cytometry experiments designed evaluate...
A novel and efficient preparation of epoxyketone intermediates for the synthesis carfilzomib its derivatives has been developed. Compared to reported methods, this highly stereoselective, environmentally friendly, low-cost method can be used in scaling up derivatives.