Latest ArticlesVascular endothelial growth factor (VEGF)-vascular endothelial growth factor receptor (VEGFR) pathways are essential in tumor angiogenesis, growth and metastasis. Studies on anti-angiogenic therapy have been mostly focused on the blockage of VEGF-VEGFR pathways. We report an extracellularly transformable peptide-based nanomaterial to develop artificial extracellular matrix (ECM)-like networks for high-efficient blockage of natural VEGF-VEGFR interactions. The transformable peptide-based nanomaterial transforms from nanoparticles into nanofibers upon binding to VEGFR in solution. In addition, the transformable peptide-based nanomaterial forms ECM-like fibrous networks on VEGFR overexpressed cells, inhibiting the VEGF-VEGFR interactions and the subsequent angiogenesis. The tube formation is reduced by nearly 85.1% after treatment. This strategy shows excellent potential for anti-angiogenesis, and inhibition of tumor invasion and metastasis.
Polypeptides are one kind of promising biodegradable and biocompatible biomedical polymers with the structural units of various α-amino acids. Polypeptides were first polymerized by the ring-opening polymerization (ROP) of α-amino acid N-carboxyanhydrides (NCAs) by Leuchs and Hermann in 1906. In the past decades, several effective strategies, including the selection of initiators, the adjustment of reaction conditions, and the introduction of catalysts, have been reported to improve the controllability of the ROP of various α-amino acid NCAs to synthesize different polypeptides with precise chemical structures and low polydispersity indexes. In this Review, the strategies, mechanisms, challenges, and opportunities for controlled synthesis of polypeptides by the ROP of different α-amino acid NCAs have been declared.
Chromone and flavone are both central backbones of natural products and clinical medicines. Synthesis of diversely functionalized chromones and flavones constitutes significant research contents of the modern synthetic science because abundant molecular libraries of such types are crucial in providing candidate compounds for the discovery of new pharmaceuticals and functional materials. The direct C-H bond activation or functionalization on these heterocyclic backbones provides highly powerful tools for the rapid accesses to densely functionalized chromone and flavone derivatives. Considering the importance of the functionalized chromone and flavone compounds as well as the notable advances in the synthesis of such products by direct C-H activation or functionalization, we review herein the research advances in the C-H bond activation and functionalization reactions of chromone and flavones, in hope of showing the current states and promise of the research domain.
Nitriles are widely existed in many bioactive compounds, and they can be easily transformed into other functional groups. Therefore, the synthesis of nitriles under cyanide-free conditions is of significant importance. Recent advances for the synthesis of nitriles through photoinduced C-C bond cleavage of cycloketone oximes classified by the type of C-X bond forming are summarized. Various compounds possessing nitriles can be efficiently accessed via this method.
Room temperature phosphorescence (RTP) generated by small molecules has attracted great attention due to their unique potentials for biosensor, bioimaging and security protection. While, the design of RTP materials is extremely challenging for organic small molecules in non-crystalline solid state. Herein, we report a new strategy for achieving non-crystalline organic small molecules with RTP emission by modifying different phosphors onto diphenylalanine or phenylalanine derivatives. Benefiting from the skeletal structure of the amino acid derivatives, there are intermolecular hydrogen bond formation and rigidification effect, thereby minimizing the intermolecular motions and enhancing their RTP performance
Monitoring dynamics of mitochondria has become an essential approach to explore the function of mitochondria in living cells with the emergence of super-resolution fluorescence microscopy. However, long-term super-resolution imaging of mitochondria is still challenging due to the lack of photostable fluorescent probes and stable mitochondria-specific markers which are not affected by the changes of mitochondrial membrane potential. Here, we introduce a method for long-term imaging mitochondrial dynamic through the SNAP-tag fluorogenic probe based on 4-azetidinyl-naphthalimide derivatives. Using structured illumination microscopy (SIM), we observed the fusion and fission of mitochondria over a course of 16 min at 109 nm resolution. Furthermore, the interactions as well as fusion between mitochondria and lysosomes were studied during mitophagy at the nanoscale. Convincingly, the combination of SNAP-tag fluorogenic probes and super-resolution fluorescence microscopy will offer a new way to monitor dynamic mitochondria in living cells.
A new chiral bromobinaphthol-pyrene compound was developed to achieve a green circularly polarized luminescence (CPL) from its excimer with a dissymmetry factor (|glum|) value of 4.3×10-3 and a high quantum yield ΦF, solid up to 55.9%, while no CPL signals could be observed for the blue luminescence from unimolecule. Meanwhile, reversal CPL signals can be observed from both concentrated solution and solid.
Triazolopyridines are an important kind of fused-ring compounds. A HOCl-promoted triazolopyridine formation strategy is reported here for the first time in which hypochlorous acid (HOCl) mildly and efficiently promotes the formation of 1, 2, 4-triazolo[4, 3-a]pyridines NT1-NT6 from various 2-pyridylhydrazones N1-N6. N6, a rhodol-pyridylhydrazone hybrid, was developed into a fluorescent probe for the selective detection of HOCl, and successfully applied to probe endogenous HOCl in living cells and zebrafish in situ and in real time. The present intramolecular cyclization reaction is selective and atom-economical, thereby not only providing an important approach for the convenient synthesis of triazolopyridines, but also offering a general strategy for sensitive, selective and biocompatible detection of endogenous HOCl in complex biosystems.
During past few years, the construction of fluorescent metallacycles featuring the fluorescence-resonance energy transfer behavior has attracted extensive attention due to their diverse applications such as real-time monitoring the dynamics of coordination-driven self-assembly, photoswitching fluorescence-resonance energy transfer, and light-controlled generation of singlet oxygen for cancer therapy. This review focuses on the recent advances on the design principles, preparation methods, optical properties, and the wide applications of fluorescent metallacycles with the FRET property.
Iron is one of the essential trace elements in the human body. It plays an important role in human biology and pathology. Deregulation of iron levels in cells is associated with disease development. In this work, we synthesized a novel near-infrared intramolecular charge transfer (ICT) based ratiometric fluorescent probe to detect Fe2+, by using naphthalimide and indole moieties as building blocks. Our work showed that the radiometric probe has excellent selectivity, sensitivity and rapid response. Moreover, we could successfully perform real-time monitoring of Fe2+ in HeLa cells and C. elegans.
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