A5000089187- Regional Economics and Spatial Analysis
- Supercapacitor Materials and Fabrication
- Catalysis for Biomass Conversion
- Advanced Photonic Communication Systems
- Optical Network Technologies
- Spatial and Panel Data Analysis
- Advancements in Battery Materials
- Mesoporous Materials and Catalysis
- Musculoskeletal pain and rehabilitation
- Magnetic Properties and Applications
- Advanced Battery Materials and Technologies
- Magnetic properties of thin films
- HER2/EGFR in Cancer Research
- Advanced Fiber Laser Technologies
- Estrogen and related hormone effects
- Liver Disease and Transplantation
- Balance, Gait, and Falls Prevention
- HIV/AIDS drug development and treatment
- Fiscal Policy and Economic Growth
- Analytical Chemistry and Sensors
- Biofuel production and bioconversion
- Underwater Vehicles and Communication Systems
- Housing Market and Economics
- Fibromyalgia and Chronic Fatigue Syndrome Research
- Advanced Optical Network Technologies
Jimei University
2023-2025
Lanzhou University of Technology
2006-2024
University Medical Center Groningen
2022-2024
University of Groningen
2021-2024
Zhejiang Shuren University
2021-2024
Tsinghua University
2002-2024
Hangzhou Red Cross Hospital
2024
Third Xiangya Hospital
2016-2022
Central South University
2016-2022
Northwestern University
2021-2022
Breast cancer remains a leading cause of death in women, representing significant unmet medical need. Here, we disclose our discovery efforts culminating clinical candidate, 35 (GDC-9545 or giredestrant). is an efficient and potent selective estrogen receptor degrader (SERD) full antagonist, which translates into better antiproliferation activity than known SERDs (1, 6, 7, 9) across multiple cell lines. Fine-tuning the physiochemical properties enabled once daily oral dosing preclinical...
A series of amino acid ester prodrugs the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-540215) was prepared in an effort to improve aqueous solubility and oral bioavailability parent compound. These were evaluated for their ability liberate drug vitro vivo systems. The l-alanine prodrug 8 (also known as brivanib alaninate/BMS-582664) selected a development candidate is presently phase II clinical trials.
Several lactam analogues of the epothilones were prepared using a concise semisynthetic approach starting with unprotected natural products. Highlighted in this strategy is novel regio- and stereoselective Pd(0)-catalyzed azidation reaction macrocyclic lactone. Subsequent reduction macrolactamization resulting azide acid intermediates provided desired macrolactams satisfactory overall yields. The entire three-step sequence was streamlined into "one-pot" process for epothilone B-lactam,...
A series of substituted 4-(4-fluoro-1H-indol-5-yloxy)pyrrolo[2,1-f][1,2,4]triazine-based inhibitors vascular endothelial growth factor receptor-2 kinase is reported. Structure−activity relationship studies revealed that a methyl group at the 5-position and alkoxy 6-position pyrrolo[2,1-f][1,2,4]triazine core gave potent compounds. Biochemical potency, selectivity, pharmacokinetics were optimized in vitro safety liabilities minimized to afford BMS-540215 (12), which demonstrated robust...
A novel redox-mediated gel polymer (PVA–H<sub>2</sub>SO<sub>4</sub>–ARS) is prepared, and a symmetric supercapacitor using the as electrolyte activated carbon electrode also assembled.
Regulated cell death (RCD), distinct from accidental death, refers to a process of well-controlled programmed with well-defined pathological mechanisms. In the past few decades, various terms for RCDs were coined, and some them have been implicated in pathogenesis types acute kidney injury (AKI). Cisplatin is widely used as chemotherapeutic drug broad spectrum cancers, but its usage was hampered because being highly nephrotoxic. Cisplatin-induced AKI commonly seen clinically, it also serves...
Abstract Systemic inflammation is related to disease progression and prognosis in patients with advanced cirrhosis. However, the mechanisms underlying initiation of are still not fully understood. The role CD169 + monocyte/macrophage cirrhotic systemic was undetected. Flow cytometry analysis used detect percentage phenotypes monocytes as well their proinflammatory function patient-derived tissue blood. Transcriptome differences between − were also compared. Additionally, a mouse model...
<title>Abstract</title> Biothiols play essential roles in various biological processes and are closely associated with diseases such as cancer, neurodegenerative disorders, cardiovascular so on. To monitor biothiols organisms living cells, we present the synthesis of a novel intramolecular charge transfer (ICT)-based probe, HCD, by coupling hemicyanine dye 2,4-dinitrobenzenesulfonyl chloride. The HCD exhibits remarkable sensitivity, low detection limit 0.32µM, 0.72µM 0.27 µM for Cys, Hcy,...
The pyrrolo[2,1-f][1,2,4]triazine nucleus was identified as a novel kinase inhibitor template which effectively mimics the well-known quinazoline scaffold. Attachment of 4-((3-chloro-4-fluorophenyl)amino) substituent to provided potent biochemical inhibitors tyrosine activity EGFR, well inhibition cellular proliferation human colon tumor cell line DiFi. 4-((3-hydroxy-4-methylphenyl)amino) VEGFR-2 also showed effects on VEGF-dependent umbilical vein endothelial cells. Biological maintained...
In this investigation, a potentially novel signaling pathway in gentamicin-induced acute kidney injury-worsened by overexpression of proximal tubular enzyme, myo-inositol oxygenase (MIOX)-was elucidated. WT, MIOX-transgenic (MIOX-Tg), and MIOX-KO mice were used. Gentamicin was administered to induce injury. MIOX-Tg had severe lesions associated with increased serum creatinine proteinuria. Lesions relatively mild, no rise albuminuria mice. Transfection HK-2 cells MIOX-pcDNA led reactive...
[reaction: see text]. A series of 12alpha,13alpha-aziridinyl epothilone derivatives were synthesized in an efficient manner from A. The final semisynthetic route involves a formal double-inversion stereochemistry at both the C12 and C13 positions. All aziridine analogues tested for effects on tubulin binding polymerization cytotoxicity. results indicate that moiety is viable isosteric replacement epoxide case epothilones.
A series of substituted 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines was identified as potent and selective inhibitors the tyrosine kinase activity growth factor receptors VEGFR-2 (Flk-1, KDR) FGFR-1. The enzyme kinetics associated with inhibition compound 50 (K(i) = 52 +/- 3 nM) confirmed that pyrrolo[2,1-f][1,2,4]triazine analogues are competitive ATP. Several demonstrated low-nanomolar VEGF- FGF-dependent human umbilical vein endothelial cell (HUVEC)...
A novel approach to photonically generate binary digital modulation radio frequency (RF) signals is proposed. In the proposed system, short optical pulses are converted into high RF based on pulse shaping followed by dispersion induced frequency-to-time mapping technique. And generated coded using a fast electro-optical switch polarization modulation. By properly configuring signals, including amplitude-shift keying (ASK), frequency-shift (FSK) and phase-shift (PSK) with required bit pattern...
An immunochromatographic test strip using gold nanoparticles-staphylococcus aureus monoclonal antibody conjugates was developed for the rapid and convenient detection of staphylococcus based on a double-antibody sandwich format. The limit rate this is 10(3) CFU /mL 98.7%, respectively. It could be used in food results can visually identified by naked eye within 10 min. Compared with conventional bacterial methods, assay has several advantages including simple, fast, low-cost, favorable...
In this paper, to describe accurately the spatial structure of Tokyo metropolitan area, cubic-spline density function approach is applied and modified. It shown that, during 1975-85 decade, there was a substantial suburbanisation in whole study while its three directional regions displayed different patterns. identifying determinants dynamics, varying-parameter model proposed confirm that increasing income decreasing transportation cost would cause suburbanisation. The differences region are...