Tuning Second Near-Infrared Fluorescence Activation by Regulating the Excited-State Charge Transfer Dynamics Change Ratio.

Second near-infrared (NIR-II) fluorescence imaging holds great promise for studying biopathological processes with high spatial resolution. However, developing activatable NIR-II fluorescent probes (AFPs) remains challenging due to insufficient signal activation in response to biomarkers and labor-intensive probe optimization. Here, we identify the excited-state charge transfer dynamics change ratios (δ) as a critical determinant of the fluorescence "turn-on" ratio of AFPs.

Membrane Disruption-Enhanced Photodynamic Therapy against Gram-Negative Bacteria by a Peptide-Photosensitizer Conjugate.

Photodynamic therapy (PDT) emerges as a promising strategy for combating bacteria with minimal drug resistance. However, a significant hurdle lies in the ineffectiveness of most photosensitizers against Gram-negative bacteria, primarily attributable to their characteristic impermeable outer membrane (OM) barrier. To tackle this obstacle, we herein report an amphipathic peptide-photosensitizer conjugate (PPC) with intrinsic outer membrane disruption capability to enhance PDT efficiency against Gram-negative bacteria.

Sono-Driven STING Activation using Semiconducting Polymeric Nanoagonists for Precision Sono-Immunotherapy of Head and Neck Squamous Cell Carcinoma.

Immunotherapy has offered new opportunities to treat head and neck squamous cell carcinoma (HNSCC); however, its clinical applications are hindered by modest therapeutic outcomes and the "always-on" pharmacological activity of immunomodulatory agents. Strategies for precise spatiotemporal activation of antitumor immunity can tackle these issues but remain challenging. Herein, a semiconducting polymeric nanoagonist (SPNM) with in situ sono-activatable immunotherapeutic effects for precision sono-immunotherapy of HNSCC is reported.

Effects of semi-deep water irrigation on hybrid indica rice lodging resistance.

Recently, rice-aquatic animal integrated farming (RAAIF) has grown rapidly in China due to its favorable benefits and the lower application of pesticides and fertilizers. However, rice lodging occurs frequently under RAAIF, which restricts rice yield. We assumed that semi-deep water irrigation may cause weaker rice-lodging resistance since it is the most significant environmental factor for RAAIF that distinguishes it from rice monoculture.

Biomimetic control of charge transfer in MOFs by solvent coordination for boosting photocatalysis.

The role of the coordination solvent in MOFs with photocatalysis can't be ignored. Novel [Ni(PTCA)·sol]-MOFs with a 3D open wavy-layered structure are selected for in-depth study by imitating the internal environment of a chameleon. The results confirm that the coordination solvent can modulate the band structure and the polarity is the key to accelerate the formation of intermediate H*.

Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer.

Androgen receptor (AR) is an effective therapeutic target for the treatment of prostate cancer. We report herein the design, synthesis, and biological evaluation of highly effective proteolysis targeting chimeras (PROTAC) androgen receptor (AR) degraders, such as compound A031. It could induce the degradation of AR protein in VCaP cell lines in a time-dependent manner, achieving the IC 50 value of less than 0.

Palladium catalyzed reductive Heck coupling and its application in total synthesis of (-)-17-nor-excelsinidine.

Monoterpene indole alkaloids, bearing a highly substituted piperidine ring, are a structurally diverse class of bioactive natural products, found in various parts of the world. Herein, we reported the construction of the key piperidine ring palladium catalyzed reductive Heck coupling with a good selective manner, avoiding the usage of stoichiometric, highly toxic, air sensitive and moisture sensitive Ni(COD). To further showcase the value of this methodology, we realized the total synthesis of the structurally unique zwitterionic monoterpene indole alkaloid (-)-17-nor-excelsinidine in 9 steps, in which the key ammonium-acetate connection (N4-C16) of (-)-17-nor-excelsinidine was constructed oxidative coupling in excellent yield and high regioselectivity under NBS/pyridine from the enolate of geissoschizine.