Highly Selective Red-Emitting Fluorescent Probe for Imaging Cancer Cells in Situ by Targeting Pim-1 Kinase

Guo, Shigang; Fan, Jiangli; Wang, Benhua; Xiao, Ming; Li, Yueqing; Du, Jianjun; Peng, Xiaojun

doi:10.1021/acsami.7b14553

Cited by 27 publications

(23 citation statements)

References 42 publications

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“…First, a fluorescent dansyl derivative of a pyrrolo[2,3- a ]carbazole-based PIM-1 inhibitor (fluorescent probe PCC-13) was reported to penetrate the plasma membrane and locate to the cytoplasm in live cells [ 46 ]. Later, a red-emitting fluorescent probe NB-BF targeting PIM-1 kinase was developed for the imaging of cancer cells [ 47 ]. NB-BF was prepared by conjugating 5-bromobenzofuran-2-carboxylic acid (a PIM-1 inhibitor possessing an IC 50 value of 8.5 μM) with a red-emitting fluorophore Nile blue via hexanediamine linker.…”

Section: Resultsmentioning

confidence: 99%

Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family

et al. 2021

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We performed an X-ray crystallographic study of complexes of protein kinase PIM-1 with three inhibitors comprising an adenosine mimetic moiety, a linker, and a peptide-mimetic (d-Arg)6 fragment. Guided by the structural models, simplified chemical structures with a reduced number of polar groups and chiral centers were designed. The developed inhibitors retained low-nanomolar potency and possessed remarkable selectivity toward the PIM kinases. The new inhibitors were derivatized with biotin or fluorescent dye Cy5 and then applied for the detection of PIM kinases in biochemical solutions and in complex biological samples. The sandwich assay utilizing a PIM-2-selective detection antibody featured a low limit of quantification (44 pg of active recombinant PIM-2). Fluorescent probes were efficiently taken up by U2OS cells and showed a high extent of co-localization with PIM-1 fused with a fluorescent protein. Overall, the developed inhibitors and derivatives represent versatile chemical tools for studying PIM function in cellular systems in normal and disease physiology.

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Section: Resultsmentioning

confidence: 99%

Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family

et al. 2021

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“…Thus, excited electron transfers from ICT state to the ground state, which produces a change in D–A molecule emission . Based on the charge transfer, PET and ITC are common mechanisms for designing fluorescence switches . By using PET and ICT fluorescent probes 1,8‐naphthalimide as energy donor, a series FRET systems were realized .…”

Section: Resultsmentioning

confidence: 99%

Fluorescent Platforms Based on Organic Molecules for Chemical and Biological Detection

Wang

Liu

Zhu

et al. 2018

Physica Rapid Research Ltrs

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Fluorescent platforms based on organic molecules have attracted great attention in the field of chemical and biological detection because of their high detection efficiency and sensitivity. Strategies in fluorescent platform design with controlled luminescence properties based on Förster resonance energy transfer, excimer/exciplex formation, and metal‐enhanced fluorescence mechanisms are reviewed herein. Attention is focused on the photophysical processes of fluorescent molecules in their interactions with other components as well as with the target. Color‐ and intensity‐tunable luminescence from energy or electron transfer and the electronic structures of fluorescent molecules are discussed. On the basis of the photophysical properties of fluorescent molecules, their responsive fluorescence signals, which reflect specific inter‐ and intra‐molecular interactions, are particularly effective for chemical and biological detection.

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“…Diseased cells are always accompanied by overexpressed enzymes in the cytoplasm, which are efficient biomarkers for screening cancer cells . The universal principle of enzyme targeting depends on the unique catalytic activity of enzymes.…”

Section: Cds For Bioimaging and Diagnosticsmentioning

confidence: 99%

Carbon Dots for In Vivo Bioimaging and Theranostics

Fan

et al. 2019

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Carbon dots (CDs), a kind of carbon material discovered accidentally, exhibit unexpected advantages in fluorescence imaging/sensing such as photostability, biocompatibility, and low toxicity. For emerging theranostics, an interdiscipline created by integrating therapy and diagnostics, CDs are good candidates when they are combined with targeted chemo/gene/photodynamic/photothermal therapeutic moieties. Here, the development of CDs in nanomedicine is reviewed from their use as original imaging agents and/or drug carriers to multifunctional theranostic systems. Finally, the challenges and prospects of the next‐generation of CD‐based theranostics for clinical applications are also discussed.

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Highly Selective Red-Emitting Fluorescent Probe for Imaging Cancer Cells in Situ by Targeting Pim-1 Kinase

Cited by 27 publications

References 42 publications

Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family

Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family

Fluorescent Platforms Based on Organic Molecules for Chemical and Biological Detection

Carbon Dots for In Vivo Bioimaging and Theranostics

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