A5101793627- Heat shock proteins research
- Computational Drug Discovery Methods
- ATP Synthase and ATPases Research
- Synthesis and biological activity
- Cancer therapeutics and mechanisms
- Melanoma and MAPK Pathways
- Enzyme function and inhibition
- Glutathione Transferases and Polymorphisms
- Protein Hydrolysis and Bioactive Peptides
- Biochemical and Molecular Research
- Bladder and Urothelial Cancer Treatments
- RNA modifications and cancer
- Pelvic floor disorders treatments
- Bioactive Compounds and Antitumor Agents
- Urinary Bladder and Prostate Research
- Urological Disorders and Treatments
- Coenzyme Q10 studies and effects
- Cancer, Hypoxia, and Metabolism
- Toxin Mechanisms and Immunotoxins
- Insect Utilization and Effects
- Fibroblast Growth Factor Research
- Biochemical effects in animals
- Mitochondrial Function and Pathology
- Redox biology and oxidative stress
- Urinary Tract Infections Management
Second Affiliated Hospital of Chongqing Medical University
2022-2024
Chongqing Medical University
2022-2024
Dalian Medical University
2022-2024
Chinese Academy of Tropical Agricultural Sciences
2023
Beijing Chao-Yang Hospital
2014-2023
Spice and Beverage Research Institute
2023
Capital Medical University
2013-2023
Baoding People's Hospital
2015-2020
Ministry of Education
2019
Beijing Normal University
2019
Abstract EML4–ALK gene rearrangements define a unique subset of patients with non–small cell lung carcinoma (NSCLC), and the clinical success anaplastic lymphoma kinase (ALK) inhibitor crizotinib in this population has become paradigm for molecularly targeted therapy. Here, we show that Hsp90 ganetespib induced loss expression depletion multiple oncogenic signaling proteins ALK-driven NSCLC cells, leading to greater vitro potency, superior antitumor efficacy, prolonged animal survival...
SIRT7 plays a critical role in dissembling and deactivating ATM when DNA damage repair is completed.
Activating BRAF kinase mutations serve as oncogenic drivers in over half of all melanomas, a feature that has been exploited the development new molecularly targeted approaches to treat this disease. Selective BRAF(V600E) inhibitors, such vemurafenib, typically induce initial, profound tumor regressions within group patients; however, durable responses have hampered by emergence drug resistance. Here, we examined activity ganetespib, small-molecule inhibitor Hsp90, melanoma lines harboring...
Mutant KRAS is a feature of more than 25% non-small cell lung cancers (NSCLC) and represents one the most prevalent oncogenic drivers in this disease. NSCLC tumors with respond poorly to current therapies, necessitating pursuit new treatment strategies. Targeted inhibition molecular chaperone Hsp90 results coordinated blockade multiple signaling pathways tumor cells has thus emerged as an attractive avenue for therapeutic intervention human malignancies. Here, we examined activity...
Systemic chemotherapy using two-drug platinum-based regimens for the treatment of advanced stage non-small cell lung cancer (NSCLC) has largely reached a plateau effectiveness. Accordingly, efforts to improve survival and quality life outcomes have more recently focused on use molecularly targeted agents, either alone or in combination with standard care therapies such as taxanes. The molecular chaperone heat shock protein 90 (Hsp90) represents an attractive candidate therapeutic...
Abstract Activating mutations and/or overexpression of FGFR3 are common in bladder cancer, making an attractive therapeutic target this disease. In addition, gene rearrangements have recently been described that define a unique subset tumors. Here, selective HSP90 inhibitor, ganetespib, induced loss FGFR3-TACC3 fusion protein expression and depletion multiple oncogenic signaling proteins RT112 cells, resulting potent cytotoxicity comparable with the pan-FGFR tyrosine kinase inhibitor BGJ398....
5-Fluorouracil (5-FU) combined with radiotherapy is a common treatment strategy to treat human cancers, but the underlying mechanisms of this combination remain unclear.Here, we report that NAD + -dependent deacetylase sirtuin-7 (SIRT7) protein levels were decreased due 5-FU exposure rendering colorectal cancer cells sensitive radiation.We found SIRT7 downregulation was mediated via Tat-binding Protein 1 (TBP1) proteasome-dependent pathway.Specifically, TBP1 dephosphorylated at tyrosine 381...
Abstract Purpose: Treatment options for patients with triple-negative breast cancer (TNBC) are largely limited to systemic chemotherapies, which have shown disappointing efficacy in the metastatic setting. Here, we undertook a comprehensive evaluation of activity ganetespib, potent inhibitor HSP90, this malignancy. Experimental Design: The antitumor and antimetastatic ganetespib was investigated using TNBC cell lines xenograft models. Combinatorial drug analyses were performed...
Androgen ablation therapy represents the first line of therapeutic intervention in men with advanced or recurrent prostate tumors. However, incomplete efficacy and lack durable response to this clinical strategy highlights an urgent need for alternative treatment options improve patient outcomes. Targeting molecular chaperone heat shock protein 90 (Hsp90) a potential avenue as its inhibition results coordinate blockade multiple oncogenic signaling pathways cancer cells. Moreover, Hsp90 is...
Summary Heat shock protein 90 (Hsp90) is a molecular chaperone essential for the stability and function of multiple cellular client proteins, number which have been implicated in pathogenesis breast cancer. Here we undertook comprehensive evaluation activity ganetespib, selective Hsp90 inhibitor, this malignancy. With low nanomolar potency, ganetespib reduced cell viability panel hormone receptor-positive, HER2-overexpressing, triple-negative inflammatory cancer lines vitro. Ganetespib...
Abstract Because of their pleiotropic effects on critical oncoproteins, inhibitors HSP90 represent a promising new class therapeutic agents for the treatment human cancer. However, pharmacologic inactivation subsequently triggers heat shock response that may mitigate full benefit these compounds. To overcome this limitation, clinically feasible method was sought to block HSP synthesis induced by potent inhibitor ganetespib. An immunoassay screen 322 late-stage or approved drugs performed...
Summary Acetes chinensis is a marine shrimp found in the coastal waters of China. The was hydrolysed by pepsin to prepare hydrolysates with angiotensin I‐converting enzyme (ACE) inhibitory activity. hydrolysate highest ACE activity resulted from 3–5 h incubation at 45 °C and pH 2.5 pepsin. Gel filtration RP‐HPLC were used separate peptides hydrolysate. gel fraction molecular weight range 1320 Da 311 exerted inhibition This separated into fifteen fractions, which F9 showed 92.7% Its peptide...
Small molecule inhibitors of epidermal growth factor receptor (EGFR) tyrosine kinase activity, such as erlotinib and gefitinib, revolutionized therapy for non-small cell lung cancer (NSCLC) patients whose tumors harbor activating EGFR mutations. However, mechanisms to overcome the invariable development acquired resistance agents, well realizing their full clinical potential within context wild-type (WT-EGFR) disease, remain be established. Here, antitumor efficacy targeted (TKIs) HSP90...
Abstract The clinical benefits of chemotherapy are commonly offset by insufficient drug exposures, narrow safety margins, and/or systemic toxicities. Over recent decades, a number conjugate-based targeting approaches designed to overcome these limitations have been explored. Here, we report on an innovative strategy that utilizes HSP90 inhibitor–drug conjugates (HDC) for directed tumor chemotherapeutic agents. STA-12-8666 is HDC comprises inhibitor fused SN-38, the active metabolite...
Abstract Liver hepatocellular carcinoma (LIHC) is one of the main cancers worldwide and has high morbidity mortality rates. Although previous studies have shown that ANXA10 expressed at low levels in LIHC tumor tissues, biological function still unclear. Therefore, we utilized TCGA, TIMER, GEPIA2, TISIDB, LinkedOmics, ssGSEA algorithms CIBERSORT methodology to preliminarily evaluate potential mechanism LIHC. In vitro experiments were used further verify some functions ANXA10. Consequently,...
Three types of proteins including sarcoplasmic protein, myofibrillar protein and stromal were isolated from Paphia undulate muscle tissue. Myofibrillar had the highest content (45.42%), followed by (31.20%) (20.69%). Analysis DSC found that denaturation temperatures 53.4C, 47.23C 55.73C, respectively. The three fractions contained higher contents essential amino acids, alkaline, hydrophobic branched chain acid. Protein hydrolysates prepared with trypsin revealed a good radical scavenging...
Summary Peptic hydrolysate with angiotensin I‐converting enzyme (ACE) inhibitory activity was prepared from Acetes chinensis . The 3 kDa ultrafiltration filtrates (UF‐IV) of the desalted exerted a potent ACE IC50 being 0.67 mg mL −1 fractions molecular weight located between 611 and 240 Da achieved total percentage 63.6% in UF‐IV, mean peptide length about 5.6–2.1. Gastrointestinal digestions were simulated on UF‐IV addressed their effect activity. could survive or be maintained active form...
This paper presents an exhaust emission comparison for light-duty in-use compressed natural gas (CNG)-gasoline flexible-fuel vehicles under the ECE 15 driving cycle protocol. The aim of this study is to provide a scientific basis determining level emissions reduction gasoline fuelled with CNG. characteristics and CNG are experimentally measured parabolic fits data performed obtain relationship between CO, HC, NO x levels vehicle mileage. As mileage exceeds 200 000 km, changes in gradually...
Under near-infrared (NIR) laser irradiation, ICG–antigen conjugate-based nanovaccines enhanced the cross-presentation of antigens and induced cytotoxic T lymphocyte response.
Desloratadine, a potent antagonist for human histamine H1 receptor, has been revealed to exhibit antihistaminic activity and anti-inflammatory activity. However, it is not yet known whether desloratadine any effect on the biological behaviors of tumor cells. In this study, we aimed investigate effects cell growth invasion in bladder cancer EJ SW780 cells vitro. We observed that inhibited viability dose- time-dependent manner. Desloratadine treatment was also suppress colony-formation ability...
Hepatocellular carcinoma (HCC) is one of the most common malignant tumors that lacks an efficient therapeutic approach because its elusive molecular mechanisms. This study aimed to investigate biological function and potential mechanism formin-binding protein 4 (FNBP4) in HCC.FNBP4 expression tissues cells were detected by quantitative real-time PCR (qRT‒PCR), Western blot, immunohistochemistry (IHC). The Kaplan-Meier method was used explore correlation between FNBP4 clinical survival. MTT,...
A facile and efficient one-pot three-step procedure for the preparation of 2-(1-benzofuran-2-yl)quinoline-3-carboxylic acid derivatives is described, featuring three different synthetic transformations, namely Williamson ether synthesis, hydrolysis an ester group at quinoline ring C-3 position, intramolecular electrophilic cyclization reaction between aldehyde salicylaldehyde methylene C-2 position.