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1.
Org Lett ; 23(19): 7661-7665, 2021 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-34546062

RESUMO

We describe a straightforward, postmodification synthesis for a family of thiophene-fused BODIPY dimers and tetramers through transforming flexible sulfur bridges into coplanar thiophene fusions. FeCl3 was used as a bifunctional oxidant for both intramolecular and intermolecular oxidative aromatic coupling reactions. Oxidative fusion and dimerization gave strong red-shift absorptions from 509 nm for a BODIPY monomer to 830 nm for a tetramer.

2.
Int J Nanomedicine ; 16: 6129-6140, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34511910

RESUMO

Purpose: With the development of nanomedicine, microwave ablation enhanced by multifunctional nanoplatforms has been widely studied for synergistic cancer therapy. Though scientists have got a lot of significant achievements in this field, the detailed molecular mechanisms and potential targets of microwave ablation enhanced by multifunctional nanoplatforms still need further exploration. In this study, we found that a kind of magnetite Fe3O4 nanoparticles (Fe3O4 NPs) could induce severe endoplasmic reticulum stress and activate cancer apoptosis under the irradiation of mild microwave. Methods: In this study, plenty of studies including cell immunofluorescence, mitochondrial membrane potential, electron microscopy, atomic force microscopy and microwave ablation in vivo were conducted to explore the molecular mechanisms and potential targets of microwave ablation enhanced by the Fe3O4 NPs. Results: The IRE1-ASK1-JNK pathway was strongly activated in A375 cells treated with both Fe3O4 NPs and mild microwave. The endoplasmic reticulum of the A375 cells was significantly dilated and exhibited ballooning degeneration. By investigating the mitochondrial membrane potential (ΔΨm), we found that the mitochondria of cancer cells had been significantly damaged under microwave treatment coupled with Fe3O4 NPs. In addition, melanoma of B16F10-bearing mice had also been effectively inhibited after being treated with Fe3O4 NPs and microwave. Conclusion: In this study, we found that a kind of magnetite Fe3O4 nanoparticles could induce severe ER stress and activate cancer apoptosis under mild microwave irradiation. Apparent apoptosis had been observed in the A375 cells under a scanning electron microscope and transmission electron microscope. Moreover, melanoma had also been inhibited effectively in vivo. As a result, the endoplasmic reticulum stress is a promising target with clinical potential in nanomedicine and cancer therapy.

3.
J Org Chem ; 2021 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-34590860

RESUMO

A Cu(I)-promoted oxidative dimerization of BODIPY dyes was developed to give a series of α,α- ethylene-bridged BODIPY dimers and trimers for the first time. This methodology does not need harsh conditions but relies on the singlet-electron-transfer process between alkylated BODIPYs and Cu(I) salt to generate BODIPY-based radical species, which undergo a selective radical homocoupling reaction. Moreover, these resultant dimers and trimers showed high attenuation coefficients, small line widths of the absorption and emission, and intense fluorescence.

4.
Org Lett ; 23(18): 7220-7225, 2021 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-34463517

RESUMO

An efficient strategy for building sulfur-bridged oligo-BODIPYs based on the SNAr reaction is described. These oligo-BODIPYs showed broadband and strong visible-near-infrared (NIR) light absorption, strong intramolecular exciton coupling, and efficient intersystem crossing (ISC). Generation of 1O2 as well as O2•- under irradiation was found to give high reactive oxygen species generation efficiencies for those oligomers.

5.
Biol Direct ; 16(1): 13, 2021 08 06.
Artigo em Inglês | MEDLINE | ID: mdl-34362407

RESUMO

BACKGROUND: Growing evidence has demonstrated that long non-coding RNAs (lncRNAs) can function as modulators in the development of triple-negative breast cancer (TNBC). However, the function of lncRNA small nucleolar RNA host gene 8 (SNHG8) in TNBC remains unclear. Therefore, our study aimed at investigating the role of SNHG8 in the proliferation and migration of TNBC cells. METHODS: SNHG8 expression was evaluated using RT-qPCR assay. Cell proliferation and migration were assessed by EdU, colony formation and Transwell assays. The levels of proteins related to EMT process were examined by western blot assay. The interaction among SNHG8, miR-335-5p and pygopus family PHD finger 2 (PYGO2) was detected by RIP assay, RNA pull down assay and luciferase reporter assay. RESULTS: SNHG8 expression was significantly up-regulated in TNBC cells. SNHG8 silencing obviously inhibited TNBC cell proliferation, migration and EMT process. Moreover, SNHG8 acted as a sponge to sequester miR-335-5p in TNBC cells. Besides, PYGO2 was proven as a target gene of miR-335-5p, and SNHG8 promoted TNBC cell proliferation, migration and EMT process through regulating miR-335-5p and PYGO2. CONCLUSIONS: Totally, our study indicated that SNHG8 promoted TNBC cell proliferation and migration by regulating the miR-335-5p/PYGO2 axis.

6.
ACS Nano ; 2021 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-34170115

RESUMO

X-ray-induced photodynamic therapy (XPDT) is overwhelmingly superior in treating deep-seated cancers. However, limitations remain, owing to a combination of the poor scintillation performance of the nanoscintillator, low energy transfer efficiency of the therapeutic nanoplatform, and hypoxic environment presented in the tumor tissue. Collectively, these reduce the curative effect of XPDT. Here, we report a highly efficient, low-dose XPDT realized by systematic optimization from scintillation efficiency, nanoplatform structure, to therapeutic approach. We developed a biocompatible, codoped CaF2 nanoscintillator that emitted sufficiently green radioluminescence that was bright enough to be seen by the naked eye. Using dendrimers as a framework, we built a nanoplatform featuring a dual-core-satellite architecture, which enabled both procedurally and spatially separate dual-loading of therapeutic agents. This strategy allowed for the fabrication of a combined XPDT and antiangiogenic therapy, resulting in a therapeutic system capable of simultaneous tumor attacks. After exposure to ultralow dose radiation, XPDT resulted in marked tumor reduction while the antiangiogenic drug effectively blocked tumor vascularization exacerbated by XPDT-mediated hypoxia, rendering a pronounced synergy effect. This system also showed high biosafety, as the agents adopted had been used clinically and both Ca and F elements were widespread in the human body. Taken together, the findings presented here provided a reference for the construction of complex, multiloading architecture in coordination with structural complexity and functional diversification. This work provided a safer and more robust application of the combined XPDT and antiangiogenesis in future clinical treatment settings.

7.
Adv Mater ; 33(30): e2004734, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34137090

RESUMO

When analyzing biological phenomena and processes, multiplexed biodetection has many advantages over single-factor biodetection and is highly relevant to both human health issues and advancements in the life sciences. However, many key problems with current multiplexed biodetection strategies remain unresolved. Herein, the main issues are analyzed and summarized: 1) generating sufficient signal to label targets, 2) improving the signal-to-noise ratio to ensure total detection sensitivity, and 3) simplifying the detection process to reduce the time and labor costs of multiple target detection. Then, available solutions made possible by designing and controlling the properties of micro- and nanomaterials are introduced. The aim is to emphasize the role that micro-/nanomaterials can play in the improvement of multiplexed biodetection strategies. Through analyzing existing problems, introducing state-of-the-art developments regarding relevant materials, and discussing future directions of the field, it is hopeful to help promote necessary developments in multiplexed biodetection and associated scientific research.

8.
Int J Biol Macromol ; 182: 1037-1046, 2021 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-33894256

RESUMO

Poly (lactic acid) (PLA) perforated membrane is typically obtained through the solvent-volatilization-induced or non-solvent-induced phase separation (NIPS) method. However, the residual organic solvents would unavoidably limit the application of PLA perforated membrane in biomedical and high-end water purification fields. Herein, an innovative solution-free method was proposed for preparing the PLA perforated membrane via a simple and environmentally friendly way. We have successfully fabricated the PLA perforated membrane using a physical foaming technique with CO2 as the blowing agent. By tuning the primary film thickness, saturation pressure, and foaming temperature, PLA perforated membrane's cell morphology could be accordingly adjusted. The PLA perforated membrane with a highly-ordered straight pore channel and high open cell content (OCC) approximately 72% was obtained under a mild condition. The formation mechanism of the PLA perforated membrane was discussed via the interaction of crystallization behavior and gas diffusion process. This green and solvent-free PLA perforated membrane possesses great potential for use in areas like the tissue engineering and high-end water purification.


Assuntos
Poliésteres/química , Polímeros/química , Solventes/química , Cristalização , Engenharia Tecidual/métodos
9.
Anal Chem ; 93(7): 3626-3634, 2021 02 23.
Artigo em Inglês | MEDLINE | ID: mdl-33557514

RESUMO

Multimodal lateral flow immunoassay (LFIA) has shown promise for improving both the flexibility and practicability of point-of-care test. We report here a facile, in situ growth method for preparing multifunctional core-shell-shell nano-sunflowers with a unique combination of color-magnetic-Raman properties. The use of Fe3O4 nanobeads with high saturation magnetization as the magnetic core allowed for robust magnetic signal strength-even after successive coatings of polydopamine and gold nanoparticles (Au NPs). Carefully selected 4-mercaptobenzonitrile molecules not only contributed to the growth of the Au NP shell but also generated a strong, surface-enhanced Raman scattering signal. The resulting nanomaterials were successfully used in the construction of multimodal LFIA with one qualitative and two alternative quantitative detection modes of different sensitivity levels. The limit of detection for the paradigm target-human chorionic gonadotropin-was 10 mIU/mL in color mode, 1.2 mIU/mL in magnetic mode, and 0.2 mIU/mL in Raman mode.


Assuntos
Helianthus , Nanopartículas Metálicas , Ouro , Humanos , Imunoensaio , Fenômenos Magnéticos , Análise Espectral Raman
10.
Nanoscale ; 13(8): 4562-4568, 2021 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-33599633

RESUMO

Environment-friendly high color purity blue zinc selenide (ZnSe) quantum dot-based light-emitting diodes (QLEDs) are promising candidates in next-generation display applications. However, due to the large bandgap of ZnSe (2.7 eV), the reported electroluminescence (EL) wavelengths of ZnSe QLEDs are mainly located within the range from purple to violet blue, and preparing blue emitting (>445 nm) ZnSe QLEDs remains challenging. Herein, we report a seed-mediated and double shell strategy to synthesize large-sized blue ZnSe/ZnS/ZnS core/shell/shell quantum dots (QDs). The as-prepared QDs possess excellent features including narrow full widths at half-maximum (11-19 nm), tunable emission wavelengths (410-451 nm), and high photoluminescence quantum yields (≥50%). Using ZnSe/ZnS/ZnS QDs as emitters in an inverted device, a color saturated blue QLED with an EL wavelength of 446 nm, a maximum luminance of 106 cd m-2, a current efficiency of 0.94 cd A-1, and an EQE of 2.62% is successfully fabricated. These results indicate that blue ZnSe QLEDs have great potential for future display technologies.

11.
ACS Nano ; 15(2): 2038-2067, 2021 02 23.
Artigo em Inglês | MEDLINE | ID: mdl-33486944

RESUMO

Innovative multifunctional nanomaterials have attracted tremendous interest in current research by facilitating simultaneous cancer imaging and therapy. Among them, antimony (Sb)- and bismuth (Bi)-based nanoparticles are important species with multifunction to boost cancer theranostic efficacy. Despite the rapid development, the extensive previous work treated Sb- and Bi-based nanoparticles as mutually independent species, and therefore a thorough understanding of their relationship in cancer theranostics was lacking. We propose here that the identical chemical nature of Sb and Bi, being semimetals, provides their derived nanoparticles with inherent multifunction for near-infrared laser-driven and/or X-ray-based cancer imaging and therapy as well as some other imparted functions. An overview of recent progress on Sb- and Bi-based nanoparticles for cancer theranostics is provided to highlight the relationship between chemical nature and multifunction. The understanding of Sb- and Bi-based nanoparticles in this way might shed light on the further design of smart multifunctional nanoparticles for cancer theranostics.


Assuntos
Bismuto , Nanoestruturas , Antimônio , Fototerapia , Nanomedicina Teranóstica
12.
Micromachines (Basel) ; 12(2)2021 Jan 22.
Artigo em Inglês | MEDLINE | ID: mdl-33499221

RESUMO

In this paper, the effects of annealing temperature and other process parameters on spin-coated indium oxide thin film transistors (In2O3-TFTs) were studied. The research shows that plasma pretreatment of glass substrate can improve the hydrophilicity of glass substrate and stability of the spin-coating process. With Fourier transform infrared (FT-IR) and X-ray diffraction (XRD) analysis, it is found that In2O3 thin films prepared by the spin coating method are amorphous, and have little organic residue when the annealing temperature ranges from 200 to 300 °C. After optimizing process conditions with the spin-coated rotating speed of 4000 rpm and the annealing temperature of 275 °C, the performance of In2O3-TFTs is best (average mobility of 1.288 cm2·V-1·s-1, Ion/Ioff of 5.93 × 106, and SS of 0.84 V·dec-1). Finally, the stability of In2O3-TFTs prepared at different annealing temperatures was analyzed by energy band theory, and we identified that the elimination of residual hydroxyl groups was the key influencing factor. Our results provide a useful reference for high-performance metal oxide semiconductor TFTs prepared by the solution method.

13.
ACS Nano ; 14(4): 4336-4351, 2020 04 28.
Artigo em Inglês | MEDLINE | ID: mdl-32275394

RESUMO

The abundant species of functional nanomaterials have attracted tremendous interests as components to construct multifunctional composites for cancer theranostics. However, their distinct chemical properties substantially require a specific strategy to integrate them in harmony. Here, we report the preparation of a distinctive multifunctional composite by encapsulating small-sized semiconducting copper bismuth sulfide (CBS) nanoparticles and rare-earth down-conversion (DC) nanoparticles in larger-sized zeolitic imidazolate framework-8 (ZIF8) nanoparticles, followed by loading an anticancer drug, doxorubicin (DOX). Such composites can be used for tetramodal imaging, including traditional computed tomography and magnetic resonance imaging and, recently, for photoacoustic imaging and fluorescence imaging. With a pH-responsive release of the encapsulated components, synergistic radio-chemotherapy with a high (87.6%) tumor inhibition efficiency is achieved at moderate doses of the CBS&DC-ZIF8@DOX composite with X-ray irradiation. This promising strategy highlights the extending capacity of zeolitic imidazolate frameworks to encapsulate multiple distinct components for enhanced cancer imaging and therapy.


Assuntos
Antineoplásicos , Nanopartículas , Neoplasias , Zeolitas , Antineoplásicos/uso terapêutico , Doxorrubicina/farmacologia , Doxorrubicina/uso terapêutico , Humanos , Neoplasias/diagnóstico por imagem , Neoplasias/tratamento farmacológico
14.
Mol Phylogenet Evol ; 149: 106842, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32305509

RESUMO

Reticulate evolution resulting from hybridization and introgression has been recognized as a creative source of species and diversification in bamboos. Previous phylogenetic studies revealed that Fargesia (s.l.) (Fargesia and Yushania) was divided into the Fargesia spathe clade and the non-spathe clade. Interestingly, the Fargesia spathe clade may have originated from hybridization among other clades within Fargesia (s.l.). Understanding the hybrid origin of this clade requires a robust phylogenetic framework in which major clades within Fargesia (s.l.) are resolved. Here, we used three nuclear genes to reconstruct the evolutionary history of Fargesia (s.l.) and its allies to identify putative patterns in the origin of the Fargesia spathe clade and to examine the extent to which reticulate evolution has occurred at the interspecific level in bamboos. Bashania species form a clade with Fargesia (s.l.), which is further divided into Group I and Group II. The Fargesia spathe clade, the Alpine Bashania clade, and Fargesia yajiangensis comprise Group I, while the Bashania fargesii clade and the remaining Fargesia (s.l.) species form Group II. Incongruence between the current nuclear-based and previous plastid phylogenies demonstrate several possible hybridization events among Fargesia (s.l.) species and related taxa, which have given rise to the Fargesia spathe clade, the Phyllostachys clade, and the Ampelocalamus clade. We also detected several putative hybrid species of Fargesia (s.l.). Our results show that reticulate evolution has played a prominent role in Fargesia (s.l.) evolution, which could, in part, account for the taxonomic difficulty associated with Fargesia (s.l.) and the alpine bamboos. The study also underscores the importance of hybridization in the evolution of bamboos, at both intergeneric and intrageneric levels.


Assuntos
Núcleo Celular/genética , Evolução Molecular , Poaceae/genética , Sequência de Bases , Teorema de Bayes , Bases de Dados Genéticas , Genes de Plantas , Marcadores Genéticos , Hibridização Genética , Filogenia , Poaceae/anatomia & histologia
15.
Sci Total Environ ; 718: 137304, 2020 May 20.
Artigo em Inglês | MEDLINE | ID: mdl-32087588

RESUMO

Fertilizer-replacement programs by the ministry of agriculture and rural affairs are extraordinary actions for environment protection and sustainable agriculture in China. A national-level survey was performed to acquire consensuses of bio-physiochemical properties for composts. A total of 116 compost samples collected from 16 provinces in China were analyzed by high throughput sequencing of bacterial 16S rRNA gene amplicons. The germination index and bacterial alpha-diversity were lower in composts from poultry manure than others. This large-scale survey revealed that bacterial communities were distinct among different composts and slightly explained by pH, moisture and total nitrogen, but not by raw material or composting process. Nevertheless, 26 OTUs affiliated with Firmicutes (Cerasibacillus, Atopostipes and Bacillus) and Actinobacteria (Thermobifida, Actinomadura and Nocardiopsis) were present in most (>90%) composts and majority of these bacterial species were possibly associated with the biodegradation of organic materials. Surprisingly, 629 potential human or animal bacterial pathogens accounting an average of 1.21% of total 16S rRNA gene were detected and these bacteria were mainly affiliated with Helicobacter, Staphylococcus, Acinotobacter, Streptococcus, Mycobacterium and Enterococcus. In summary, this study provides baseline data for the diversity and abundance of core microbiome and potential pathogens in composts.


Assuntos
Compostagem , Microbiota , Animais , Bactérias , China , Esterco , Prevalência , RNA Ribossômico 16S , Solo , Microbiologia do Solo
16.
ACS Chem Neurosci ; 11(4): 549-559, 2020 02 19.
Artigo em Inglês | MEDLINE | ID: mdl-31968160

RESUMO

The 5-HT2C receptor has emerged as a promising target in the treatment of a variety of central nervous system disorders. We have first identified aporphines as a new class of 5-HT2C receptor agonists. Structure-activity relationship results indicate that the aporphine core may be required for 5-HT2C receptor activity, and substitutions at its C1 position are important for 5-HT2C receptor activity. Our efforts to optimize our hit 15781 lead to the identification of the highly potent and selective 5-HT2C agonist 18b (MQ02-439) with an EC50 value of 104 nM and weak antagonism at the 5-HT2A and 5-HT2B receptors. The findings may serve as good starting points for the development of more potent and selective 5-HT2C agonists as valuable pharmacological tools or potential drug candidates.


Assuntos
Aporfinas/farmacologia , Receptor 5-HT2C de Serotonina/efeitos dos fármacos , Agonistas do Receptor 5-HT2 de Serotonina/farmacologia , Relação Dose-Resposta a Droga , Humanos , Ensaio Radioligante , Receptor 5-HT2A de Serotonina/efeitos dos fármacos , Receptor 5-HT2C de Serotonina/metabolismo , Relação Estrutura-Atividade
17.
Biosens Bioelectron ; 150: 111912, 2020 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-31780403

RESUMO

Aggregation-induced emission luminogens (AIEgens) have attracted considerable interest for application towards the development of various biosensors due to their unique optical properties. However, the major challenge associated with generating a suitable fluorescent signal for constructing an AIEgens-based immunoassay platform, is the complex surface modification and additional chemical reaction required to activate the AIE process. This work reports a novel AIEgens nanobeads-based fluorescence-linked immunosorbent assay (FLISA) platform wherein the fluorescent labels are hexaphenylsilole (HPS) nanobeads, which were synthesized through Shirasu porous glass (SPG) membrane emulsification method and could provide a strong, direct fluorescent signal without any pretreatment. Moreover, the particle-based signal amplification effect affords this platform significantly improved detection sensitivity for carcinoembryonic antigen (CEA) quantitation. Compared to FLISA which uses R-phycoerythrin (PE) or commercial green QDs nanobeads as fluorescent labels, this AIEgens nanobeads-based FLISA platform exhibits detection sensitivity improved up to 45-fold and 12-fold, respectively. Clinical validation experiments applying this AIEgens nanobeads-based FLISA immunoassay platform to analyze human serum samples produce results consistent with those obtained by the clinical gold-standard method, electrochemiluminescence immunoassay (ECLIA). The strong photobleaching resistance and excellent fluorescent stability of the HPS nanobeads negate the need for light shielding, which improves the efficiency and makes the operating conditions more comfortable. Thus, this AIEgens nanobeads-based FLISA platform, with attractive features including direct fluorescent signal generation and significant signal amplification, creates a new, versatile route for the application of AIEgens in biosensors and clinical diagnosis.


Assuntos
Anticorpos Imobilizados/química , Antígeno Carcinoembrionário/sangue , Corantes Fluorescentes/química , Técnicas de Imunoadsorção , Nanopartículas/química , Técnicas Biossensoriais/métodos , Dimerização , Humanos , Imunoadsorventes/química , Nanopartículas/ultraestrutura
18.
J Sep Sci ; 43(3): 639-647, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31705607

RESUMO

A novel green hydrophilic levofloxacin imprinted polymer was presented via one-step polymerization in water using ionic liquid 1,6-hexa-3,3'-bis-1-vinylimidazolium bromine with multiple hydrophilic groups and 2-hydroxyethyl methacrylate as a co-functional monomer. Adsorption experiment revealed that the ionic liquid significantly improved the water compatible of imprinted polymer, and the excellent recognition of molecularly imprinted polymer for levofloxacin in water corresponds to the synergetic effect of H-bonding and the electrostatic and π-π interactions between the levofloxacin and co-functional monomer. Furthermore, the adsorption process of the imprinted material towards levofloxacin fitted the Langmuir model, and the maximum binding amount of levofloxacin onto the imprinted and corresponding non-imprinted polymer were 16.45 and 6.82 mg/g at 25°C, respectively. After optimizing the parameters affecting solid phase extraction performance, an enrichment and determination system was achieved to separate and detect levofloxacin from water and sediment samples with recoveries that ranged from 83.67 to 101.33% and relative standard deviation of less than 5.59%.


Assuntos
Líquidos Iônicos/química , Levofloxacino/análise , Polímeros/química , Poluentes Químicos da Água/análise , Água/química , Interações Hidrofóbicas e Hidrofílicas , Estrutura Molecular
19.
Theranostics ; 9(24): 7210-7221, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31695763

RESUMO

Suspension arrays based on optical encoded microspheres have attracted great attention for multiplexed detection in gene analysis, protein profiling, early disease diagnosis, treatment monitoring and so on. However, the fluorescence stability of barcodes and detection sensitivity require further improvement to meet the increasing demands of "precision diagnosis". Methods: This work reports a novel suspension array platform based on extremely stable AIEgens (AIE33 and AIE NIR800) microbeads as barcodes and AIEgens (1,1,2,3,4,5-Hexaphenyl-1H-silole, HPS) nanobeads as fluorescent signal reporter coupled with flow cytometry for multiplexed detection. Results: Due to the excellent fluorescent signal amplification effect of the HPS nanobeads, our multiplex assay showed enhanced detection sensitivity, compared to multiplex assay using QDs nanobeads (up to 3-fold improvement) and commercial organic dye of phycoerythrin (up to 5-fold improvement) as the fluorescent signal reporters. Conclusion: Furthermore, validating experiments showed similar detection performance to the clinical gold-standard method of ImmunoCAP for allergen detection in patient serum samples, demonstrating the suspension array platform based on AIEgens microbeads with excellent fluorescence stability and AIEgens nanobeads with strong signal amplification ability is promising for high-sensitivity multiplexed bioassay applications.


Assuntos
Luminescência , Microesferas , Nanopartículas/química , Alérgenos/análise , Animais , Emulsões/química , Limite de Detecção , Compostos de Silício/química , Espectrometria de Fluorescência , Espectrofotometria Ultravioleta
20.
Curr Top Med Chem ; 19(23): 2114-2127, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31475899

RESUMO

The Ras proteins play an important role in cell growth, differentiation, proliferation and survival by regulating diverse signaling pathways. Oncogenic mutant K-Ras is the most frequently mutated class of Ras superfamily that is highly prevalent in many human cancers. Despite intensive efforts to combat various K-Ras-mutant-driven cancers, no effective K-Ras-specific inhibitors have yet been approved for clinical use to date. Since K-Ras proteins must be associated to the plasma membrane for their function, targeting K-Ras plasma membrane localization represents a logical and potentially tractable therapeutic approach. Here, we summarize the recent advances in the development of K-Ras plasma membrane localization inhibitors including natural product-based inhibitors achieved from high throughput screening, fragment-based drug design, virtual screening, and drug repurposing as well as hit-to-lead optimizations.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Avaliação Pré-Clínica de Medicamentos , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Proteína Oncogênica p21(ras)/metabolismo , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/uso terapêutico , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Reposicionamento de Medicamentos , Humanos , Mutação , Neoplasias/genética , Neoplasias/patologia , Proteína Oncogênica p21(ras)/genética
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