A5080001523- Chemical Synthesis and Analysis
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Carbohydrate Chemistry and Synthesis
- Fluorine in Organic Chemistry
- PI3K/AKT/mTOR signaling in cancer
- Force Microscopy Techniques and Applications
- Regulation of Appetite and Obesity
- Synthesis and biological activity
- Click Chemistry and Applications
- Biochemical Analysis and Sensing Techniques
- Synthesis and Reactions of Organic Compounds
- Marine Sponges and Natural Products
- Advanced biosensing and bioanalysis techniques
- Microbial Natural Products and Biosynthesis
- melanin and skin pigmentation
- Lung Cancer Treatments and Mutations
- Inorganic Fluorides and Related Compounds
- Traditional and Medicinal Uses of Annonaceae
- Molecular spectroscopy and chirality
- Liver physiology and pathology
- Synthesis of heterocyclic compounds
- Metal complexes synthesis and properties
- Genetics, Bioinformatics, and Biomedical Research
- Synthetic Organic Chemistry Methods
Ningxia Normal University
2025
Ningbo University
2020-2024
Xidian University
2024
Heilongjiang University
2023
Emory University
2023
HEC Pharm (China)
2022
Sunshine Hospital
2020
Michigan State University
2004-2019
University of California, Berkeley
2019
National Institute for Nanotechnology
2019
CuI-catalyzed N-arylation of imidazoles with aryl bromides has been achieved in a near-homogeneous system that utilizes tetraethylammonium carbonate as base, 8-hydroxyquinoline ligand, and H2O cosolvent. Preliminary results chlorides are also reported.
Phosphoinositide 3-kinase α (PI3Kα) is a lipid kinase that plays key regulatory role in several cellular processes. The mutation or amplification of this humans has been implicated the growth multiple tumor types. Consequently, PI3Kα become target intense research for drug discovery. Our studies began with identification benzothiazole compound 1 from high throughput screen. Extensive SAR led to discovery sulfonamide 45 as an early lead, based on its vitro potency. Subsequent modifications...
Deregulation of c-Met receptor tyrosine kinase activity leads to tumorigenesis and metastasis in animal models. More importantly, the identification activating mutations c-Met, as well MET gene amplification human cancers, points an important target for cancer therapy. We have previously described two classes inhibitors (class I class II) that differ their binding modes selectivity profiles. The II tend activities on multiple kinases. Knowledge mode these molecules protein led design...
The furan nucleus may be considered as a latent 1,4-dicarbonyl group. Expression of this functional equivalence within generic 2-furylamide results in formation nitrogen heterocycles reaction that termed the "Aza-Achmatowicz rearrangement", by analogy with similar transformations furylcarbinols. Aza-Achmatowicz products created enantioselective form chemoenzymatic methods, and are useful intermediates synthesis novel carbacephems, unusual aminoacids, azasaccharides, piperidine izidine...
Deregulation of the receptor tyrosine kinase c-Met has been implicated in human cancers. Pyrazolones with N-1 bearing a pendent hydroxyalkyl side chain showed selective inhibition over VEGFR2. However, studies revealed generation active, nonselective metabolites. Blocking this metabolic hot spot led to discovery 17 (AMG 458). When dosed orally, significantly inhibited tumor growth NIH3T3/TPR-Met and U-87 MG xenograft models no adverse effect on body weight.
c-Met is a receptor tyrosine kinase that plays key role in several cellular processes but has also been found to be overexpressed and mutated different human cancers. Consequently, targeting this enzyme become an area of intense research drug discovery. Our studies began with the design synthesis novel pyrimidone 7, which was potent inhibitor. Subsequent SAR identified 22 as more analog, whereas X-ray crystal structure 7 bound revealed unexpected binding conformation. This latter finding led...
As part of our effort toward developing an effective therapeutic agent for c-Met-dependent tumors, a pyrazolone-based class II c-Met inhibitor, N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (1), was identified. Knowledge the binding mode this molecule in both and VEGFR-2 proteins led to novel strategy designing more selective analogues 1. Along with detailed SAR information, we demonstrate that low kinase selectivity...
One of the grand challenges currently facing engineering, life sciences, and medicine is development fully functional nanorobots capable sensing, decision making, actuation. These may aid in cancer therapy, site-specific drug delivery, circulating diagnostics, advanced surgery, tissue repair. In this paper, we will discuss, from a bioinspired perspective, nanorobotics, including core design, propulsion power generation, actuation, control, system integration. Using strategies inspired...
The vanilloid receptor-1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel that predominantly expressed by peripheral neurons sensing painful stimuli. TRPV1 antagonists produce antihyperalgesic effects in animal models of inflammatory and neuropathic pain. Herein, we describe the synthesis structure-activity relationships series 2-(4-pyridin-2-ylpiperazin-1-yl)-1H-benzo[d]imidazoles as novel antagonists. Compound 46ad was among most potent analogues this series. This compound...
Glutaredoxins (GRXs) belong to the antioxidants involved in cellular stress responses. In spite of identification 48 GRX genes rice genomes, biological functions most them remain unknown. Especially, roles members family disease resistance are still lacking. Our proteomic analysis found that OsGRX20 increased by 2.7-fold after infection bacterial blight. this study, we isolated and characterized full-length nucleotide sequences gene, which encodes a protein with CPFC active site CPYC-type...
Sensitive to Apoptosis Gene (SAG), also known as RBX2 (RING box protein-2), is the RING component of SCF (SKP1, Cullin, and F-box protein) E3 ubiquitin ligase. Our previous studies have demonstrated that SAG an anti-apoptotic protein attractive anti-cancer target. We found recently Sag knockout sensitized mouse embryonic stem cells (mES) radiation blocked mES undergo endothelial differentiation. Here, we reported compared wild-type cells, Sag−/− were much more sensitive all-trans retinoic...
Bacterial blight caused by Xanthomonas oryzae pv. (Xoo) is one of the most devastating diseases rice. However, molecular mechanism underpinning Xoo resistance rice still not fully understood. Here, we report that a class II small heat shock protein gene, OsHsp18.0, whose expression was differentially induced between resistant and susceptible variety in response to infection, plays positive roles both biotic abiotic resistance. The chaperone activity OsHsp18.0 confirmed bacterium-expressed...
In this paper, a unified dynamic model for integrated mobile platform and on-board manipulator is developed. The considered as redundant robot in the model. It provides efficient convenient framework to design controller well its action plans. Combing event-based planning control method with nonlinear feedback technique, task level designed. An online kinematic redundancy resolution scheme has also been system stability proven normal operation case of appearance unexpected obstacles....
Ruthenium (Ru)-based organometallic drugs have gained attention as chemotherapeutic and bioimaging agents due to their fewer side effects excellent physical optical properties. Tuning the electronic structures of Ru complexes has been proven increase cytotoxicity cancer cells luminescent efficiency analytical probes. However, relationship between bioactivities is still unclear potential enhancement both electron donor acceptor Thus, we investigated Ru(II) by optimizing electron-withdrawing...
This paper explores a new method for action synchronization and control of telerobotic systems. The significance the is that it can effectively deal with random time-delay existing in communication channel, such as Internet. In addition, result independent human operator. First, novel non-time referenced scheme introduced. Instead using time an reference, sensor-based reference developed. As result, delay will have little impact on operations, particular stability system. Furthermore, system...
DNA sequence and structure design is very important for nanoapplications. A computer-aided tool needed exploring of interests before experimental synthesis, which a time- labor-consuming process. In this paper, an interactive software called shop proposed implemented. The visualization can generate structures by specifying, selecting, moving sequences around display corresponding structures. Using the tool, be visually inspected in three-dimensional space studies.
N-Acyl derivatives of piperazic acids display an unusual degree conformational rigidity. As a consequence, α-N-coupling acid given configuration (d or l) with α-aminoacyl unit opposite (l d) produces "heterochiral" dipeptide that exists in conformation conducive to the formation peptide turn. Piperazic and related compounds may thus be regarded as conformationally rigid analogues proline, because they are readily available either antipodal form by synthesis, should become great interest study turns.