A5001620453- Cerebrovascular and Carotid Artery Diseases
- Cardiovascular Health and Disease Prevention
- Acute Ischemic Stroke Management
- Intracranial Aneurysms: Treatment and Complications
- Advanced MRI Techniques and Applications
- Traumatic Brain Injury and Neurovascular Disturbances
- Cardiac Imaging and Diagnostics
- Protein Kinase Regulation and GTPase Signaling
- Cardiovascular Disease and Adiposity
- MRI in cancer diagnosis
- Synthesis and biological activity
- Quinazolinone synthesis and applications
- Coronary Interventions and Diagnostics
- Moyamoya disease diagnosis and treatment
- Angiogenesis and VEGF in Cancer
- Advanced X-ray and CT Imaging
- PI3K/AKT/mTOR signaling in cancer
- Cytokine Signaling Pathways and Interactions
- Cardiovascular Function and Risk Factors
- Cancer Mechanisms and Therapy
- Autopsy Techniques and Outcomes
- Synthesis and Characterization of Heterocyclic Compounds
- HER2/EGFR in Cancer Research
- Click Chemistry and Applications
- Cancer, Hypoxia, and Metabolism
Shanghai Jiao Tong University
2013-2025
Renji Hospital
2013-2025
Dalian Polytechnic University
2023-2025
Gansu University of Traditional Chinese Medicine
2023-2024
Fudan University
2024
Chongqing Medical University
2024
Qingdao University of Science and Technology
2022-2023
Xian Central Hospital
2021
University of Washington
2021
Huazhong Agricultural University
2020
Inhibition of the VEGF signaling pathway has become a valuable approach in treatment cancers. Guided by X-ray crystallography and molecular modeling, series 2-aminobenzimidazoles 2-aminobenzoxazoles were identified as potent inhibitors VEGFR-2 (KDR) both enzymatic HUVEC cellular proliferation assays. In this report we describe synthesis structure−activity relationship benzoxazoles, culminating identification benzoxazole 22 selective inhibitor displaying good pharmacokinetic profile. Compound...
Abstract A simultaneous noncontrast angiography and intraplaque hemorrhage (SNAP) MR imaging technique is proposed to detect both luminal stenosis in atherosclerosis patients a single scan. Thirteen with diagnosed carotid atherosclerotic plaque were admitted after informed consent. All scans performed on 3T system SNAP, 2D time‐of‐flight magnetization‐prepared 3D rapid acquisition gradient echo sequences. The SNAP sequence utilized phase sensitive acquisition, was designed provide positive...
Inhibition of angiogenesis is a promising and clinically validated approach for limiting tumor growth survival. The receptor tyrosine kinase Tie-2 expressed almost exclusively in the vascular endothelium required developmental vessel maturation. However, significance signaling not well understood. In order to evaluate therapeutic utility inhibiting signaling, we developed series potent orally bioavailable small molecule inhibitors with selectivity over other kinases, especially those that...
Background: Intracranial atherosclerotic disease (ICAD) tends to affect multiple arterial segments, and previous studies rarely performed a comprehensive plaque analysis of the entire circle Willis for evaluation recurrent stroke risk. We aimed investigate features ICAD on 3D magnetic resonance vessel wall imaging (MR-VWI) their relationships with acute stroke. Methods: Patients either ischemic (within 4 weeks after stroke) or chronic (after 3 months due intracranial underwent...
Despite the high morbidity and mortality, effective therapies for heart failure with preserved fraction (HFpEF) are limited as poor understand of its pathophysiological basis. This study was aimed to characterize cellular heterogeneity potential mechanisms HFpEF at single-cell resolution. An mouse model induced by a high-fat diet N-nitro-L-arginine methyl ester. Cells from hearts were subjected sequencing. The key protein expression measured Immunohistochemistry immunofluorescence staining....
Lck, or lymphocyte specific kinase, is a cytoplasmic tyrosine kinase of the Src family expressed in T-cells and NK cells. Genetic evidence from knockout mice human mutations demonstrates that Lck activity critical for T-cell receptor-mediated signaling, leading to normal development activation. A small molecule inhibitor expected be useful treatment T-cell-mediated autoimmune inflammatory disorders and/or organ transplant rejection. In this paper, we describe structure-guided design,...
Casein kinase 1 delta (CK1δ) and its closest homologue CK1ε are key regulators of diverse cellular growth survival processes such as Wnt signaling, DNA repair, circadian rhythms. We report three crystal structures the domain human CK1δ, one apo two complexed with a potent selective CK1δ/ε inhibitor PF670462 in different forms. These provide molecular basis for strong specific interactions suggest clues further development inhibitors.
To assess fast three-dimensional (3D) black-blood (BB) magnetic resonance (MR) imaging as a noninvasive alternative to intraarterial digital subtraction angiography (DSA) at quantifying moderate severe carotid artery atherosclerotic disease.Local ethics committee approval and written informed patient consent were obtained for this study. Sixty-five arteries from 52 patients with least 50% stenosis underwent 3D BB MR DSA. Quantitative measurements, including stenosis, lesion length, the...
<h3>BACKGROUND AND PURPOSE:</h3> Fractional flow measured on 3D-TOF-MRA was proposed to quantify cerebral hemodynamic changes in patients with artery stenosis. We investigated the association between fractional and perfusion symptomatic MCA <h3>MATERIALS METHODS:</h3> This prospective study approved by institutional review board, all participants provided written informed consent. From June 2015 May 2018, four hundred twenty-nine intracranial arterial stenosis were consecutively recruited...
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine of the Src family expressed in T cells and natural killer (NK) cells. Genetic evidence both mice humans demonstrates that Lck activity critical for signaling mediated by cell receptor (TCR), which leads to normal development activation. Selective inhibition expected offer new therapy treatment T-cell-mediated autoimmune inflammatory disease. Screening our kinase-preferred collection identified aminoquinazoline 1 as potent,...
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine of the Src family expressed in T cells and NK cells. Genetic evidence both mice humans demonstrates that Lck activity critical for signaling mediated by cell receptor (TCR), which leads to normal development activation. A small molecule inhibitor expected be useful treatment cell-mediated autoimmune inflammatory disorders and/or organ transplant rejection. In this paper, we describe synthesis, structure-activity relationships,...
Casein kinase 1 epsilon (CK1ε) and its closest homologue CK1δ are key regulators of diverse cellular processes. We report two crystal structures PF4800567, a potent selective inhibitor CK1ε, bound to the domains human CK1ε as well one apo structure. These provide molecular basis for strong specific interactions with suggest clues further development inhibitors.
Type 2 diabetes mellitus (T2DM) might aggravate the carotid plaque vulnerability, and increase risk for ischemic stroke. Few studies reported acute stroke subtype with characteristics in T2DM patients. This study aimed to investigate association between cerebral infarct (ACI) lesion features determined by MRI Patients cerebrovascular syndrome internal artery territory were recruited. All patients stratified into non-T2DM groups underwent both brain scans. Ipsilateral morphological...
Background: Managing unruptured intracranial aneurysms (IAs) involves balancing procedural risks with the long-term risk of rupture. Aneurysm wall enhancement (AWE) has been associated aneurysm instability and symptomatic presentation. However, assessing AWE typically relies on subjective two-dimensional visual inspection, which lack objectivity. This study aims to evaluate a predictive model for status by integrating clinical, morphological, three dimensional-AWE (3D-AWE) metrics from large...
Lipid saturation and protein oxidation influence the types amounts of volatile nonvolatile compounds by affecting lipid oxidation. This study examined three reaction modes: systems containing only fatty acids with different saturations, myofibrillar proteins (MPs), or their combinations. Sensomics (including volatilomics) metabolomics were used to analyze these systems. Results showed that MPs enhanced saturated acid oxidation, suppressed unsaturated double-bond adsorbed volatiles from...
Chitin, a major component of the fungal cell wall, triggers plant innate immunity in Arabidopsis via receptor complex including two lysine motif receptor-like kinases, AtLYK5 and AtCERK1. Although has been proposed to be chitin-binding receptor, pseudokinase domain is required mediate chitin-triggered immune responses plants. In this study, 48 AtLYK5-interacting proteins were identified using immunoprecipitation mass spectrometry assay. Among them, CALCIUM-DEPENDENT PROTEIN KINASE 5 (AtCPK5)...
The discovery of aurora kinases as essential regulators cell division has led to intense interest in identifying small molecule kinase inhibitors for the potential treatment cancer. A high-throughput screening effort identified pyridinyl-pyrimidine 6a a moderately potent dual inhibitor -A and -B. Optimization this hit resulted an anthranilamide lead (6j) that possessed improved enzyme cellular activity exhibited high level selectivity. However, subsequent analogues suffered from lack oral...
Abstract Purpose: To evaluate the performance of automatic segmentation atherosclerotic plaque components using solely multicontrast 3D gradient echo (GRE) magnetic resonance imaging (MRI). Materials and Methods: A total 15 patients with a history recent transient ischemic attacks or stroke underwent carotid vessel wall bilaterally combination 2D turbo spin (TSE) sequences GRE sequences. The TSE included T1‐weighted, T2‐weighted, contrast‐enhanced T1‐weighted scans. time‐of‐flight (TOF),...