An enzyme-responsive double-locked amonafide prodrug for the treatment of glioblastoma with minimal side effects.

Amonafide (ANF), a topoisomerase II inhibitor and DNA intercalator, has exhibited promise in phase II trials but faces significant limitations due to adverse side effects. Here, we have developed a novel enzyme-triggered fluorogenic prodrug, AcKLP, that incorporates dual-locked enzyme activation, ensuring that the prodrug remains inactive until it confronts the unique enzymatic environment of glioblastoma cells. This approach minimizes premature activation and reduces toxicity to normal cells, with an IC > 100 μM for human umbilical vein endothelial cells (HUVEC) and ∼2.

Visible-ultraviolet dual-band photodetectors based on an all-inorganic CsPbCl/p-GaN heterostructure.

All-inorganic metal halide perovskites (MHPs) have attracted increasing attention because of their high thermal stability and band gap tunability. Among them, CsPbCl is considered a promising semiconductor material for visible-ultraviolet dual-band photodetectors because of its excellent photoelectric properties and suitable band gap value. In this work, we fabricated a visible-ultraviolet dual-band photodetector based on a CsPbCl/p-GaN heterojunction using the spin coating method.

Photosensitizing metal covalent organic framework with fast charge transfer dynamics for efficient CO photoreduction.

Designing artificial photocatalysts for CO reduction is challenging, mainly due to the intrinsic difficulty of making multiple functional units cooperate efficiently. Herein, three-dimensional metal covalent organic frameworks (3D MCOFs) were employed as an innovative platform to integrate a strong Ru(ii) light-harvesting unit, an active Re(i) catalytic center, and an efficient charge separation configuration for photocatalysis. The photosensitive moiety was precisely stabilized into the covalent skeleton by using a rational-designed Ru(ii) complex as one of the building units, while the Re(i) center was linked a shared bridging ligand with an Ru(ii) center, opening an effective pathway for their electronic interaction.

Discovery of potent PROTAC degraders of Pin1 for the treatment of acute myeloid leukemia.

Peptidyl-prolyl / isomerase NIMA-interacting 1 (Pin1) is overexpressed and/or overactivated in many human cancers and has been shown to play a critical role during oncogenesis. Despite the potential of Pin1 as a drug target, its successful targeting has proved to be challenging. We speculate that only blocking the enzymatic function of Pin1 with inhibitors may not be sufficient to lead to a total loss-of-function.

Deep Learning-Assisted Design of Novel Promoters in .

Deep learning (DL) approaches have the ability to accurately recognize promoter regions and predict their strength. Here, the potential for controllably designing active promoter is explored by combining multiple deep learning models. First, "DRSAdesign," which relies on a diffusion model to generate different types of novel promoters is created, followed by predicting whether they are real or fake and strength.

Engineering a molecular ruthenium catalyst into three-dimensional metal covalent organic frameworks for efficient water oxidation.

The water oxidation reaction plays an important role in clean energy conversion, utilization, and storage, but mimicking the oxygen-evolving complex of photosystem II for designing active and stable water oxidation catalysts (WOCs) is still an appealing challenge. Here, we innovatively engineered a molecular ruthenium WOC as a metal complex building unit to construct a series of three-dimensional metal covalent organic frameworks (3D MCOFs) for realizing efficient oxidation catalysis. The resultant MCOFs possessed rare 3D interlocking structures with inclined interpenetration of two-dimensional covalent rhombic nets, and the Ru sites were periodically arranged in the crystalline porous frameworks.

Ultrafast C-C and C-N bond formation reactions in water microdroplets facilitated by the spontaneous generation of carbocations.

Carbocations are important electrophilic intermediates in organic chemistry, but their formation typically requires harsh conditions such as extremely low pH, elevated temperature, strong oxidants and/or expensive noble-metal catalysts. Herein, we report the spontaneous generation of highly reactive carbocations in water microdroplets by simply spraying a diarylmethanol aqueous solution. The formation of transient carbocations as well as their ultrafast in-droplet transformations through carbocation-involved C-C and C-N bond formation reactions are directly characterized by mass spectrometry.

Functional characterization, structural basis, and regio-selectivity control of a promiscuous flavonoid 7,4'-di--glycosyltransferase from var. .

A highly efficient and promiscuous 7,4'-di--glycosyltransferase ZjOGT3 was discovered from the medicinal plant var. . ZjOGT3 could sequentially catalyse 4'- and 7--glycosylation of flavones to produce 7,4'-di--glycosides with obvious regio-selectivity.

Fragile intermediate identification and reactivity elucidation in electrochemical oxidative α-C(sp)-H functionalization of tertiary amines.

The direct α-C(sp)-H functionalization of widely available tertiary amines holds promise for the rapid construction of complex amine architectures. The activation of C(sp)-H bonds through electron transfer and proton transfer by oxidants, photoredox catalysis and electrochemical oxidation have received wide attention recently. In these reactions, the direct capture and identification of the key reactive radical intermediates are technically difficult due to their short life-time.

Realization of a multi-band terahertz metamaterial absorber using two identical split rings having opposite opening directions connected by a rectangular patch.

A multi-band metamaterial absorber in the terahertz regime using a periodically arranged surface structure placed on an ultra-thin insulating dielectric slab backed by a metallic ground plane is demonstrated in this paper. Its surface structure consists of two identical split rings having opposite opening directions connected by a rectangular patch. The surface structure can have a strong electromagnetic interaction with incident terahertz waves, thereby generating two localized resonance absorption peaks with different frequencies, and the superposition effect of these two absorption peaks gives rise to dual-band absorption.

Effects of different tempering temperatures on the properties of industrial sheet margarine.

Tempering is the final step in Industrial Sheet Margarine (ISM) production, which has a substantial influence on the structure and application characteristics. There are limited reports on how the tempering process affects the ductility and application characteristics of ISM at an industrial production scale. Herein, we investigated the physicochemical properties and ductility of the ISM made from interesterification and non-interesterification fat at various tempering temperatures (10, 15, 20, 25, and 30 °C) for 5 days.

Endowing matrix-free carbon dots with color-tunable ultralong phosphorescence by self-doping.

Color-tunable ultralong phosphorescence is urgently desired in optoelectronic applications. Herein, we report a new type of full-color-tunable ultralong phosphorescence carbon dots (CDs) without matrix-assistance by a self-doping method under ambient conditions. The phosphorescence color can be rationally tuned from blue to red by changing the excitation wavelength from 310 to 440 nm.

A fluorine-18 labeled radiotracer for PET imaging of γ-glutamyltranspeptidase in living subjects.

The expression level of γ-glutamyltranspeptidase (GGT) in some malignant tumors is often abnormally high, while its expression is low in normal tissues. Therefore, GGT is considered as a key biomarker for cancer diagnosis. Several GGT-targeting fluorescence probes have been designed and prepared, but their clinical applications are limited due to their shallow tissue penetration.

Steered polymorphic nanodomains in TiO to boost visible-light photocatalytic oxidation.

A breakthrough in enhancing visible-light photocatalysis of wide-bandgap semiconductors such as prototypical titania (TiO) cocatalyst decoration is still challenged by insufficient heterojunctions and inevitable interfacial transport issues. Herein, we report a novel TiO-based composite material composed of generated polymorphic nanodomains including carbon nitride (CN) and (001)/(101)-faceted anatase nanocrystals. The introduction of ultrafine CN results in the generation of many oxygen vacancies in the TiO lattice, and simultaneously induces the exposure and growth of anatase TiO(001) facets with high surface energy.

HPTLC screening of saccharin in beverages by densitometry quantification and SERS confirmation.

As a widely used artificially synthesized sweetener, saccharin faced numerous disputes associated with food safety. Therefore, its fast analysis in food is of crucial importance. In this study, an analytical method for the fast and reliable screening of saccharin in various beverages was established and validated, by combining HPTLC with densitometry and surface enhanced Raman spectroscopy.

Thiazolidinedione derivatives as novel GPR120 agonists for the treatment of type 2 diabetes.

GPR120, also called FFAR4, is preferentially expressed in the intestines, and can be stimulated by long-chain free fatty acids to increase the secretion of glucagon-like peptide-1 (GLP-1) from intestinal endocrine cells. It is known that GLP-1, as an incretin, can promote the insulin secretion from pancreatic cells in a glucose-dependent manner. Therefore, GPR120 is a potential drug target to treat type 2 diabetes.

Colorectal Cancer-Derived Small Extracellular Vesicles Promote Tumor Immune Evasion by Upregulating PD-L1 Expression in Tumor-Associated Macrophages.

Tumor-associated macrophages (TAMs) are one of the most abundant cell types in colorectal cancer (CRC) tumor microenvironment (TME). Recent studies observed complicated "cross-talks" between cancer cells and macrophages in TME. However, the underlying mechanisms are still poorly elucidated.

Universal endogenous antibody recruiting nanobodies capable of triggering immune effectors for targeted cancer immunotherapy.

Developing monoclonal antibodies (mAbs) for cancer immunotherapy is expensive and complicated. Nanobodies are small antibodies possessing favorable pharmacological properties compared with mAbs, but have limited anticancer efficacy due to the lack of an Fc region and poor pharmacokinetics. In this context, engineered universal endogenous antibody-recruiting nanobodies (UEAR Nbs), as a general and cost-effective approach, were developed to generate functional antibody-like nanobodies that could recapitulate the Fc biological functions for cancer immunotherapy.

3D fluorescence confocal microscopy of InGaN/GaN multiple quantum well nanorods from a light absorption perspective.

A nanostructure of InGaN/GaN multiple quantum well (MQW) nanorods (NRs) was fabricated using top-down etching with self-organized nickel (Ni) nanoparticles as masks on the wafer. The optical properties of InGaN/GaN MQW NRs were discussed by experiment and theory from a light absorption perspective. Three-dimensional (3D) optical images of NRs were successfully obtained by confocal laser scanning microscopy (CLSM) for physical observation of the optical phenomenon of InGaN/GaN MQW NRs.

Synthesis of 2-ethoxycarbonylthieno[2,3-]quinolines in biomass-derived solvent γ-valerolactone and their biological evaluation against protein tyrosine phosphatase 1B.

A series of 2-ethoxycarbonylthieno[2,3-]quinolines were synthesized in the bio-derived "green" solvent γ-valerolactone (GVL) and evaluated for their inhibitory activities against PTP1B, the representative compound 6a displayed an IC value of 8.04 ± 0.71 μM with 4.

Multi-band terahertz superabsorbers based on perforated square-patch metamaterials.

This paper presents a multi-band terahertz superabsorber with a surface structure that consists of a square metallic patch with a very small rectangular hole whose area is only 3.94% of the square patch. The introduction of a rectangular hole in the square patch plays an important role in achieving multi-band absorption.

Protective effects of selenium-enriched peptides from against high-fat diet induced obesity and its associated metabolic disorders in mice.

Selenium-enriched peptides from (CSP) have excellent antioxidant functions but little is known about their effects on obesity and associated metabolic disorders in mice fed with a high-fat diet (HFD). In this study, C57BL/6 mice were fed a HFD with or without CSP supplementation (CSPL: 26 μg Se per kg bw per d; CSPH: 104 μg per kg bw per d) for 10 weeks. The results showed that both CSPL and CSPH could ameliorate overweight gain, excess fat accumulation, serum lipid metabolism, and insulin resistance.

Extraction and purification of ε-poly-l-lysine from fermentation broth using an ethanol/ammonium sulfate aqueous two-phase system combined with ultrafiltration.

ε-Poly-l-lysine (ε-PL) serves as a natural food preservative and is manufactured mainly by extraction from microbial fermentation broth using ion-exchange chromatography. In order to develop an alternative purification strategy, an environmentally friendly alcohol/salt aqueous two-phase system (ATPS) was explored in this study for ε-PL extraction. A study of the separation of ε-PL in different alcohol/salt systems showed that ethanol/ammonium sulfate ATPS exhibited the highest ε-PL partition coefficient and recovery ratio.