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Aggregation-Induced Emission: Lighting Up hERG Potassium Channel
摘要： Based on the scaffold of astemizole and E-4031, four AIE light-up probes (L1–L4) for Human Ether-a-go-go-Related Gene (hERG) potassium channel were developed herein using AIE fluorogen(TPE). These probes showing advantages such as low background interference, superior photostability, acceptable cell toxicity, and potent inhibitory activity, which could be used to image hERG channels at the nanomolar level. These AIE light-up probes hoped to provide guidelines for the design of more advanced AIE sensing and imaging hERG channels to a broad range of applications.
关键词： hERG channel,pharmacophore,fluorophore,cell imaging,AIE light-up probes
更新于2025-11-21 11:24:58
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Optically active crown ether-based fluorescent sensor molecules: A mini-review
摘要： This mini‐review focuses on fluorescent optically active crown ethers (polymeric derivatives are not included) reported in the literature (according to our knowledge), of which enantiomeric recognition ability, and in some cases, also inorganic cation complexation properties, were investigated by the sensitive and versatile fluorescence spectroscopy. These crown ether‐based chemosensors contain various fluorophore signaling units such as binaphthyl, anthracene, pyrene, tryptophan, benzimidazole, terpyridine, acridine, phenazine, acridone, BODIPY, and another conjugated aromatic one.
关键词： enantiomeric recognition,complexation,fluorophore,chemosensor,chiral crown ether
更新于2025-09-23 15:23:52
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A dsDNA-lighted fluorophore for monitoring protein-ligand interaction through binding-mediated DNA protection
摘要： Because of their important roles in cellular functions, life activities, drug screening, and disease treatment, the development of efficient methods for monitoring protein-ligand interaction is essential. In this study, inspired by our previous studies on DNA conformation-selective fluorescent indicators, we developed a new sensing platform for monitoring protein-ligand interaction and detecting protein activity based on binding-mediated DNA protection and the dsDNA-lighted fluorophore, ethyl-4-[3,6-bis(1-methyl-4-vinylpyridium iodine)-9H-carbazol-9-yl)] butanoate (EBCB). The ligand was purposefully linked to the 3?-terminal of a hairpin DNA probe to selectively bind with the target protein and protect the DNA from cleavage by exonuclease III. By virtue of EBCB’s outstanding capacity to discriminate DNA conformation, the protein-ligand interaction could be effectively monitored through a fluorescence change in EBCB. A high fluorescence signal was detected when the hairpin DNA was protected in the presence of the target protein, whereas a much lower signal was observed in the presence of nontarget proteins. Our results demonstrated that the proposed strategy had high potential, such as high selectivity and relatively high sensitivity, for monitoring protein-ligand interaction and detecting protein activity. We believe these results will pave the way for applying dsDNA-lighted fluorophore EBCB as an effective signal transducer for DNA conformation transformation-mediated biochemical sensing.
关键词： DNA protection,protein-ligand interaction,dsDNA-lighted fluorophore,fluorescence detection
更新于2025-09-23 15:23:52
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Enamine–azide [2+3]-cycloaddition as a method to introduce functional groups into fluorescent dyes
摘要： Fluorescent dyes are a significant research tool with various applications in modern science. However, many experiments require the preparation of covalent dye conjugates, which is impossible without the presence of a functional group on the dye molecule. Unfortunately, the introduction of such groups is often a complicated task. Herein, we report a novel approach for the introduction of functional groups into fluorescent dyes, based on the [2+3]-cycloaddition reaction of 'terminal' enamines with azides. The synthesis of such 'terminal' enamines is carried out by the condensation of formamide acetals with a methyl group that is influenced by a strong electron withdrawing group. Thus, the proposed functionalization technique requires only the presence of a methyl group in the relevant position of the initial non-functionalized fluorescent dye.
关键词： Enamine,Azide,Cycloaddition,Fluorophore
更新于2025-09-23 15:22:29
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Microfluidic Sensors with Impregnated Fluorophores for Simultaneous Imaging of Spatial Structure and Chemical Oxygen Gradients
摘要： Interior surfaces of polystyrene microfluidic structures were impregnated with the oxygen sensing dye Pt(II) tetra(pentafluorophenyl)porphyrin (PtTFPP) using a solvent-induced fluorophore impregnation (SIFI) method. Using this technique, microfluidic oxygen sensors are obtained that enable simultaneous imaging of both chemical oxygen gradients and the physical structure of the microfluidic interior. A gentle method of fluorophore impregnation using acetonitrile solutions of PtTFPP at 50oC was developed leading to a 10-μm-deep region containing fluorophore. This region is localized at the surface to sense oxygen in the interior fluid during use. Regions of the device that do not contact the interior fluid pathways lack fluorophores and are dark in fluorescent imaging. The technique was demonstrated on straight microchannel and pore network devices, the latter having pillars of 300 μm diameter spaced center to center at 340 μm providing pore throats of 40 μm. Sensing within channels or pores, and imaging across the pore network devices were performed using a Lambert LIFA-P frequency domain fluorescence lifetime imaging system on a Leica microscope platform. Calibrations of different devices prepared by the SIFI method were indistinguishable. Gradient imaging showed fluorescent regions corresponding to the fluid pore network, dark pillars, and fluorescent lifetime varying across the gradient, thus providing both physical and chemical imaging. More generally, the SIFI technique can impregnate the interior surfaces of other polystyrene containers, such as cuvettes or cell and tissue culture containers, to enable sensing of interior conditions.
关键词： Oxygen,sensor,impregnation,fluorophore,chemical imaging,pore network,polystyrene,microfluidic
更新于2025-09-23 15:22:29
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Two novel fluorescent probes based on phenothiazine: synthesis and “naked-eye” colorimetric recognition of Hg2+
摘要： Two novel colorimetric and fluorescent probes 2-(1,3-dithiolanes)-10-ethyl phenothiazine (PHE–Ed) and 2-(1,3-dithianes)-10-ethyl phenothiazine (PHE–Pd) based on phenothiazine were successfully synthesized, and their structure was confirmed by NMR and high resolution mass spectra. Fluorescence investigations revealed that the synthesized probes could be used for the selective detection of Hg2+, which was accompanied with an obvious color change from colorless to light yellow. The applicable ability of the two probes was investigated by a series of competitive experiments, solid colorimetric experiments, and applied experiments, which proved that these probes showed high sensitivity and great potential to detect Hg2+ in environmental analysis systems. Furthermore, the detection mechanism of the probes was investigated by FT-IR spectra and NMR spectra, and the results indicated that the detection of Hg2+ was accomplished through the Hg2+-promoted deprotection of thioacetal.
关键词： Phenothiazine,ICT fluorophore,1,3-propanedithiol,Naked-eye,1,2-ethanedithiol
更新于2025-09-23 15:22:29
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The Impact of Photobleaching on Microarray Analysis
摘要： DNA-Microarrays have become a potent technology for high-throughput analysis of genetic regulation. However, the wide dynamic range of signal intensities of fluorophore-based microarrays exceeds the dynamic range of a single array scan by far, thus limiting the key benefit of microarray technology: parallelization. The implementation of multi-scan techniques represents a promising approach to overcome these limitations. These techniques are, in turn, limited by the fluorophores’ susceptibility to photobleaching when exposed to the scanner’s laser light. In this paper the photobleaching characteristics of cyanine-3 and cyanine-5 as part of solid state DNA microarrays are studied. The effects of initial fluorophore intensity as well as laser scanner dependent variables such as the photomultiplier tube’s voltage on bleaching and imaging are investigated. The resulting data is used to develop a model capable of simulating the expected degree of signal intensity reduction caused by photobleaching for each fluorophore individually, allowing for the removal of photobleaching-induced, systematic bias in multi-scan procedures. Single-scan applications also benefit as they rely on pre-scans to determine the optimal scanner settings. These findings constitute a step towards standardization of microarray experiments and analysis and may help to increase the lab-to-lab comparability of microarray experiment results.
关键词： photobleaching,microarray,cyanine dye,bioanalytics,fluorophore,bioinformatics,DNA
更新于2025-09-23 15:22:29
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Label-free in situ Monitoring of DNA Hybridization Chain Reaction using Sequence-selective Minor-groove Binding Fluorophores
摘要： A novel label-free in situ monitoring system for hybridization chain reaction (HCR) using DNA minor-groove binding fluorophores, Hoechst 33258 (Hoe) or quinone cyanine-dithiazole (QCy-DT), has been developed. Two unmodified hairpin oligodeoxyribonucleotides having incomplete double-stranded AATT sequences enabled target-dependent formation of probe binding sites, i.e., AATT double-strand, in HCR product, and fluorescence enhancement of minor-groove binding fluorophores in situ. Using this system, target DNA can be detected by the fluorescence enhancement of Hoe and QCy-DT in a real-time in situ manner. Further development of a label-free, isothermal detection system might provide a cost-effective and user-friendly method for nucleic acid detection.
关键词： Label-free,Hybridization chain reaction,Minor-groove binding fluorophore,Fluorescence,In situ detection
更新于2025-09-23 15:22:29
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Synthesis and Evaluation of Multifunctional Fluorescent Inhibitors with Synergistic Interaction of PSMA and Hypoxia for Prostate Cancer
摘要： Prostate cancer is one of the most common cancers in the world. It is widely known that prostate-specific membrane antigen (PSMA) is highly expressed in prostate cancer, and hypoxia is a common characteristic of many solid tumors, including prostate cancer. In this study, we designed multifunctional fluorescent inhibitors to target PSMA and tumor hypoxia in order to increase the tumor uptake of inhibitors. Novel PSMA inhibitors were prepared using lysine as the backbone to connect three different functional groups: the glutamate-urea-lysine (GUL) structure for inhibiting PSMA, 2-nitroimidazole for the hypoxia-sensitive moiety, and a near-infrared fluorophore (sulfo-Cyanine 5.5). According to the in vitro PSMA binding assay, novel fluorescent inhibitors were demonstrated to have nanomolar binding affinities. Multifunctional inhibitor 2 with one 2-nitroimidazole had a similar inhibitory activity to inhibitor 1 that did not contain the hypoxia targeting moiety, but multifunctional inhibitor 3 with two 2-nitroimidazoles showed lower inhibitory activity than inhibitor 1 due to the bulky structure of the hypoxia-sensitive group. However, in vivo optical imaging and ex vivo biodistribution studies indicated that both multifunctional inhibitors 2 and 3 had higher accumulation in tumors than inhibitor 1 due to a synergistic combination of PSMA and hypoxia targeting moieties. These observations suggest that this novel multifunctional strategy might be a promising approach to improve the diagnosis and therapy of prostate cancer.
关键词： multifunctional inhibitors,hypoxia,near-infrared fluorophore,Prostate cancer,2-nitroimidazole,PSMA
更新于2025-09-23 15:21:21
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Identification of Protein Targets of Bioactive Small Molecules Using Randomly Photomodified Probes
摘要： Identifying protein targets of bioactive small molecules often requires complex, lengthy development of affinity probes. We present a method for stochastic modification of small molecules of interest with a photoactivatable phenyldiazirine linker. The resulting isomeric mixture is conjugated to a hydrophilic copolymer decorated with biotin and a fluorophore. We validated this approach using known inhibitors of several medicinally relevant enzymes. At least a portion of the stochastic derivatives retained their binding to the target, enabling target visualization, isolation, and identification. Moreover, the mix of stochastic probes could be separated into fractions and tested for binding affinity. The structure of the active probe could be determined and the probe re-synthesized to improve binding efficiency. Our approach can thus enable rapid target isolation, identification, and visualization, while providing information required for subsequent synthesis of an optimized probe.
关键词： bioactive small molecules,target isolation,protein targets,target identification,stochastic modification,target visualization,photoactivatable phenyldiazirine linker,biotin,fluorophore,hydrophilic copolymer
更新于2025-09-23 15:21:21