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In this article, we describe a no-wash small-molecule fluorescent probe for detecting and imaging p53- MDM2 protein-protein interaction based on an environment-sensitive fluorescent turn-on mechanism. After extensive biological examination, this probe L1 exhibited practical activity and selectivity in vitro and in cellulo. [ABSTRACT FROM AUTHOR]

G-protein-coupledreceptors (GPCRs), a superfamily of cell-surfacereceptors that are the targets of about 40% of prescription drugson the market, can sense numerous critical extracellular signals.Recent breakthroughs in structural biology, especially in holo-formX-ray crystal structures, have contributed to our understanding ofGPCR signaling. However, actions of GPCRs at the cellular and molecularlevel, interactions between GPCRs, and the role of protein dynamicsin receptor activities still remain controversial. To overcome thesedilemmas, fluorescent probes of GPCRs have been employed, which haveadvantages of in vivo safety and real-timemonitoring. Various probes that depend on specific mechanisms and/ortechnologies have been used to study GPCRs. The present review focuseson surveying the design and applications of fluorescent probes forGPCRs that are derived from small molecules or using protein-labelingtechniques, as well as discussing some design strategies for new probes. [ABSTRACT FROM AUTHOR]

Although hydrogen sulfide (HS) has been known as a toxic gas with unpleasant rotten egg smell, the correlation between HS and physiological processes has attracted scientists to develop brand new methods to monitor such a gaseous molecule in vitro and in vivo. Herein, we described a couple of coumarin-based fluorescent probes ( 1a and 1b) that can be activated by reduction of azide to amine in the presence of HS. It should be emphasized that probe 1b demonstrated high selectivity and sensitivity for HS over other relevant reactive sulfur species in vitro, as well as identified exogenous HS in living cells. [ABSTRACT FROM AUTHOR]

Abstract: In this study, we report a novel water-soluble umbelliferone-based fluorescent probe for hydrogen peroxide. This probe shows very large increases (up to 100-fold) in fluorescent intensity upon reaction with hydrogen peroxide, and good selectivity over other reactive oxygen species (ROS). [Copyright &y& Elsevier]

Iron plays an essential role in biological system. An approach for in vivo imaging of this metal ion is needed to investigate its complex contributions to physiological and pathological processes. Herein, we present a bioluminescent probe FP-1 as a powerful tool for targeting Fe2+ detection in vitro and in vivo. The turn-on sensing scheme is based on the caged strategy of luciferin-luciferase system. FP-1 not only can detect accumulations of exogenous Fe2+ in living animal, but also has the capability of monitoring labile endogenous Fe2+ levels in animal model of sepsis. Implementation of this technique provides a valuable opportunity for understanding underlying mechanisms of Fe2+ in biological processes and disease states. Image 1 • A novel bioluminescent probe for visualizing Iron (II) has been developed with high sensitivity and selectivity. • This probe was successfully appied to detect exogenous Fe2+ in living animal and monitor labile endogenous Fe2+ levels in animal disease model. [ABSTRACT FROM AUTHOR]

To detect γ-Glutamyl Transpeptidase (GGT) activity in vitro and in vivo, a bioluminescence probe with high sensitivity and specificity was well designed and synthesized. This probe can be recognized by GGT and release strong bioluminescence with its further reaction with luciferase. The performance of this probe was demonstrated in vitro and in cells. Finally, we applied the probe for detection of GGT activity in xenograft model. [ABSTRACT FROM AUTHOR]

Nicotinamide phosphoribosyl transferase (NAMPT) has been regarded as an attractive target for cancer therapy. However, there is a lack of chemical tools for real-time visualization and detection of NAMPT. Herein, the first fluorescent and theranostic probes were designed for imaging NAMPT, which had dual functions of diagnosis and treatment. The designed probes possessed good affinity and environmental sensitivity to NAMPT with a turn-on mechanism and were successfully applied in fluorescence detecting and imaging of NAMPT at the level of living cells and tissue sections. They also effectively inhibited tumor cell proliferation and arrested cell cycle at the G2 phase. These fluorescent probes enabled detection and visualization of NAMPT, representing effective chemical tools for the pathological diagnosis and treatment of cancer. [Display omitted] • The first turn-on fluorescent and theranostic probes possessing good affinity and environmental sensitivity to NAMPT. • Probes were applied in fluorescence detecting and imaging of NAMPT at the level of living cells and tissue sections. • These probes also effectively inhibited tumor cell proliferation and arrested cell cycle at the G2 phase. [ABSTRACT FROM AUTHOR]

C-mesenchymal-epithelia transition factor (c-Met) is highly expressed in various solid tumors such as gastric cancer, liver cancer, and lung cancer, playing a pivotal role in the growth, maintenance, and development of different tumor cells. In this study, three small-molecule fluorescent probes (5, 11, 16) targeting c-Met were developed, and their design strategies were also initially explored. In general, the fluorescence properties of the probes themselves could meet the imaging requirements, and they have shown sufficient inhibitory activities against c-Met, especially probe 16 , reflecting the targeting and acceptance. Also, fluorescence polarization assays and flow cytometry analysis verified the binding between the probes and c-Met. Cell imaging confirmed that these probes could be used to label c-Met on living cells. It is of positive significance for the development of c-Met kinase inhibitors and tumor pathology research. [Display omitted] • Fluorescent probes (5, 11, 16) targeting c-Met were developed. • Design strategies of the probes were explored. • The probes showed strong inhibitory activities against c-Met, especially probe 16. • The binding between probes and c-Met was verified. • The probes could be used to label c-Met on living cells. [ABSTRACT FROM AUTHOR]

Abstract: Herein, we report the design and synthesis of two naphthalimide-based fluorescent probes. These probes provided high on/off signal ratios and exhibited good selectivity towards thiols over other analytes. Thus, they were identified as good sensors for the detection of thiols both in living cells and in rabbit plasma samples. [Copyright &y& Elsevier]

Abstract: This study reports a benzothiazole-based fluorescent probe with simple structure for thiols. This probe exhibited high on/off signal ratios and good selectivity toward thiols over other analytes, and was successfully applied to the imaging of thiols in living cells. [Copyright &y& Elsevier]

Histone deacetylases (HDACs) are proteases that can catalyze the deacetylation of histones to inhibit gene transcription. Since mutations and/or aberrant expression of various HDACs are frequently associated with human diseases, particularly cancers, HDACs are important therapeutic targets for many human tumors. However, there are still relatively few studies on HDAC small molecule fluorescent probes. Herein, we designed and synthesized a class of environment-sensitive fluorescent inhibitors with a switch mechanism to study HDAC activity. In vitro, the enzyme inhibition activity of compound 6b was comparable to the positive control drug SAHA, and it presented suitable imaging in living cells and tumor-tissue slices. This environment-sensitive fluorescent inhibitor provides a new idea for the diagnosis and treatment of HDACs-related diseases. [ABSTRACT FROM AUTHOR]