Latest ArticlesDNA-encoded chemical libraries technology has become a novel approach to finding hit compounds in early drug discovery. The chemical space in a DEL would be expanded to realize its full potential, especially when integrating privileged scaffold dihydroquinazoline that has demonstrated a variety of diverse bioactivities. Driven by the requirement of parallel combinatorial synthesis, we here report a facile synthesis of on-DNA dihydroquinazolinone from aldehyde and anthranilamide. This DNA-compatible reaction was promoted by antimony trichloride, which has been proven to accelerate the reaction and improve conversions. Notably, the broad substrate scope of aldehydes and anthranilamides was explored under the mild reaction condition to achieve moderate-to-excellent conversion yields. We further applied the reaction into on-DNA macrocyclization, obtaining macrocycles embedded dihydroquinazolinone scaffold in synthetically useful conversion yields.
Cancer immunotherapy harnesses the immune system to attack tumors and has received extensive attention in recent years. Cancer vaccines as an important branch of immunotherapy are designed for delivering tumor antigens to antigen-presenting cells (APCs) to stimulate a strong immune response to against tumors, representing a potentially therapeutic and prophylactic effect with the long-term anti-cancer benefits. Nevertheless, the disappointing outcomes of their clinical use might be attributed to dilemma in antigen selection, immunogenicity, lymph nodes (LNs) targeting ability, lysosomal escape ability, immune evasion, etc. Nanotechnology, aiming to overcome these barriers, has been utilized in cancer vaccine development for decades. Numerous preclinical and clinical studies demonstrate positive results in nanomaterials-based cancer vaccines with considerable improvement in the vaccine efficacy. In this review, we systematically introduced the characteristics of nanovaccines and highlighted the different types of nanomaterials used for cancer vaccine design. In addition, the opportunities and challenges of the emerging nanotechnology-based cancer vaccines were discussed.
Nature chooses phosphorylation as a key modification to modulate and program the functions of proteins. Various phosphorylated peptides (PPs) have been widely identified and investigated by biologists, but the possibility that PPs could become a building unit for artificial materials is neglected. Here we report for the first time a supramolecular assembly of PPs with the assistance of dysprosium ions (Dy3+). Dy3+ bridges multiple phosphate groups in double-phosphorylated peptides (di-PPs), and braid these peptide chains into nanofibers. The assembly occurs inside nanochannels and blocks the channels, leading to prominent "ON–OFF" switching in transmembrane ionic current. The di-PPs' assembling process could be dynamically regulated by the addition or deletion of phosphate groups under the control of kinases or phosphatases. This study proves the huge potential of PPs being utilized as materials via self-assembling, which will promote the design of novel bio-inspired artificial materials and devices.
Residual antibiotics in food pose a serious long-term threat to human health. Therefore, an on-site visualization method for antibiotic detection is required. However, the requirements of traditional antibiotic testing methods in terms of operator proficiency and equipment cost hinder the rapid point-of-care-testing detection of suspected samples. Herein, we reported an integrated microfluidic device combining a microfluidic chip containing cruciform valves with immunochromatographic strips for the rapid detection of multiple antibiotics in milk. The rapid qualitative and quantitative analysis of four types of antibiotics (sulfonamides, β-lactams, streptomycin, and tetracyclines) was performed using mobile phone photography and mobile phone application analysis. The detection time was maintained at 10 min. The limits of detection (LODs) for the four antibiotics were 0.15, 0.12, 0.25, and 0.29 ng/mL, respectively, and the selectivity for the different antibiotics was observed even in a highly complex matrix. This device successfully integrated separation and real-time detection onto a chip and might provide a promising perspective for the detection of multiple antibiotics in milk.
π-Electron coupling of pendant conjugated segment in π-stacked semiconducting polymers always causes the formation of defect trapped sites and further quenched high-band excitons, which is harmful to the performance and stability of deep-blue polymer light-emitting diodes (PLEDs). Herein, considerate of “defect” carbazole (Cz) electromers in poly(N-vinylcarbazole) (PVK), a series of fluorene units are introduced into pendant segments (PVCz-DMeF, PVCz-FMeNPh and PVCz-DFMeNPh) to suppress the strong π-electron coupling of pendant Cz units and enhance radiative transition toward fabricating sable PLEDs. Compared to PVCz-FMeNPh and PVCz-DFMeNPh, PVCz-DMeF spin-coated films show a relatively efficient deep-blue emission, completely similar to its single pendant chromophore, confirmed an extremely weak charge-transfer and electron coupling between adjacent pendant segments. Therefore, PLEDs based on PVCz-DMeF present stable and deep-blue emission with a high color purity (0.17, 0.08), associated with extremely weak defect emission at 600~700 nm (induced by carbazole electromers). Finally, PLEDs based on PVCz-DMeF/F8BT blended films (1:1) also present the high maximum luminance (Lmax) of 6261 cd/m2 and current efficiency (CEmax) of 2.03 cd/A, confirmed slightly trapped sites formation. Therefore, precisely control the arrangement and packing model of pendant units in π-stacked polymer is an essential prerequisite for building efficient and stable emitter for optoelectronic devices.
Hydrazine hydrate (DH) is an important fine chemical intermediate and as fuel for rockets, however, it also has serious toxic for humans and environment. Developing novel materials and methods for sensitive detection of DH in water and air is an important task. In order to effectively detect DH, a novel conductive supramolecular polymer metallogel (PQ-Ag) has been constructed by the coordination of bis-5-hydroxyquinoline functionalized pillar[5]arene (PQ5) with Ag+. The metallogel PQ-Ag could realize the multi-channel sensitive detection of DH through naked-eye, fluorescence, and electrochemical methods. The lowest limit of detection (LOD) is 0.1 mg/m3 in air and 2.68 × 10−8 mol/L in water, which is lower than the standard of the US Environmental Protection Agency (EPA) for DH of maximum allowable concentration in drinking water. More importantly, an electronic device for DH detection based on the metallogel PQ-Ag was designed and prepared, which can realize conveniently and efficiently multi-channel detection and alert of DH through sound and light alarms not only in water but also in air.
The threat to public health from bacterial infections has led to an urgent need to develop simpler, faster and more reliable bacterial detection methods. In this work, we developed a universal dual-recognition based sandwich fluorescence resonance energy transfer (FRET) sensor by using specific aptamer-modified quantum dots (Aptamer-QDs) as energy donor and lectin concanavalin A (Con A) modified gold nanoparticles (Con A-AuNPs) as energy acceptor to achieve rapid and sensitive detection of Escherichia coli (E. coli) within 0.5 h. In the presence of the target E. coli, the energy donor of Aptamer-QDs and acceptor of Con A-AuNPs were close to each other, causing changes of FRET signals. Based on the constructed FRET sensor, a linear detection range of from 102 cfu/mL to 2 × 108 cfu/mL with the detection limit of 45 cfu/mL for E. coli was achieved. Furthermore, the FRET sensor was applied to detect E. coli in the milk and orange juice with the detection limit of 300 cfu/mL and 200 cfu/mL, respectively and recovery rate from 83.1% to 112.5%. The strategy holds great promise in pathogenic bacteria detection due to its rapid and sensitivity.
Rosmarinic acid (RA) is promising as a natural and nontoxic food additive. However, many analysis methods for RA generally depend on large instruments and single signals for quantitative detection. A new up-conversion fluorescence, colorimetric and photothermal multi-modal sensing strategy is developed for the quantification of RA. β-cyclodextrin (CD) modified citric acid (Cit) wrapped NaYF4:Yb/Er-Cit-CD (Y:Yb/Er-Cit-CD) up-conversion nanocomposite has been synthesized, which emits green fluorescence at 550 nm under 980 nm near-infrared (NIR) excitation. In the presence of oxidized 3, 3′, 5, 5′-tetramethylbenzidine (oxTMB), the green fluorescence is significantly quenched attributed to the fluorescence inner filter effect (IFE) between oxTMB and Y:Yb/Er-Cit-CD. When RA is intervened, blue oxTMB is reduced to colorless 3, 3′, 5, 5′-tetramethylbenzidine (TMB) inducing the recovery of up-conversion fluorescence. At the same time, colorimetric and photothermal signals readout can be easily achieved thanks to the color indication and photothermal effect of the oxTMB. The constructed Y:Yb/Er-Cit-CD/oxTMB sensor displays high sensitivity, visibility and simplicity for RA, and the limits of detection (LOD) for fluorescence, colorimetric and photothermal were 0.004 µmol/L, 0.036 µmol/L and 0.043 µmol/L, respectively. This sensing system is successfully performed for the detection of RA in food samples.
In clinic, the combination of intravenous pembrolizumab (PD-1 monoclonal antibody) with oral Lenvatinib (LEN) exhibited an enhanced synergistic benefit for cancer therapy. However, the clinical outcomes were always limited by the problems of inconsistent pharmacokinetic profiles of two drugs, lower drug accumulation in tumor and obvious side effects during the combination therapy. Here, in situ-forming thermosensitive hydrogels based on PLGA-PEG-PLGA triblock copolymers were prepared for local administration of anti-PD1 and LEN (P&L@Gel) to improve therapeutic efficacy and safety. After peritumoral or surgical resection site injection, the significant increased concentrations of both drugs in tumor were observed with the local sustained release of P&L@Gel. In comparison with the group of intraperitoneal anti-PD1 plus oral LEN (P-ip&L-po), significantly higher tumor inhibition efficiency on CT26 tumor models could be obtained in P&L@Gel group, even at the dose of one-eighth of the former, same tumor-inhibition effects could be achieved. The enhanced antitumor efficacy of P&L@Gel group was probably associated with the 2.2 folds of increased level of CD8+ T cells and the polarization of tumor associated macrophage from M2 to M1 along with the increased drug accumulation. Moreover, compared with the obvious side effects of P-ip&L-po group, no significant changes of PLT, ALT and UA in blood, as well as IL-1α and IL-1β in mice paws were observed between P&L@Gel group and untreated group. These results suggested that local administration of anti-PD1 and LEN with thermosensitive hydrogel could offer a potential strategy for tumors or tumor postoperative adjuvant treatment.
Owing to their unique design and development, high safety and low-cost efficient cathode is still at the forefront of research for rechargeable zinc-ion batteries. However, the suitable cathode operating with ultrahigh capacity with a dendrite-free anode reaction mechanism remains challenging. In this, the first archetype of a high-rate and morphologically stabled cathode material is constructed from novel cauliflower-like nano-ZnV2S4 for aqueous zinc-ion batteries. Thus, nano-ZnV2S4 was prepared with an anion exchange reaction using ZnV2(OH)8 cauliflower-like nanostructured array as a template interestingly no morphological and shape changes were detected. The as-prepared nano-ZnV2S4 electrode reveals a specific discharge capacity of 348.2 mAh/g during 0.5 A/g with enhanced rate capability and excellent capacity retention of 89.2% at 4 A/g current density even after completing 1000 cycles.
No. 86 Xueyuan South Road, Haidian District, Beijing
010-62199257
qkjq@cast.org.cn
Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House
