Search

In the evolving landscape of surveillance and security applications, the task of person re-identification(re-ID) has significant importance, but also presents notable difficulties. This task entails the process of accurately matching and identifying persons across several camera views that do not overlap with one another. This is of utmost importance to video surveillance, public safety, and person-tracking applications. However, vision-related difficulties, such as variations in appearance, occlusions, viewpoint changes, cloth changes, scalability, limited robustness to environmental factors, and lack of generalizations, still hinder the development of reliable person re-ID methods. There are few approaches have been developed based on these difficulties relied on traditional deep-learning techniques. Nevertheless, recent advancements of transformer-based methods, have gained widespread adoption in various domains owing to their unique architectural properties. Recently, few transformer-based person re-ID methods have developed based on these difficulties and achieved good results. To develop reliable solutions for person re-ID, a comprehensive analysis of transformer-based methods is necessary. However, there are few studies that consider transformer-based techniques for further investigation. This review proposes recent literature on transformer-based approaches, examining their effectiveness, advantages, and potential challenges. This review is the first of its kind to provide insights into the revolutionary transformer-based methodologies used to tackle many obstacles in person re-ID, providing a forward-thinking outlook on current research and potentially guiding the creation of viable applications in real-world scenarios. The main objective is to provide a useful resource for academics and practitioners engaged in person re-ID.

Inflammation is the body's response to defence against infection or injury, and is associated with the progression of many diseases, such as inflammatory bowel disease (IBD) and rheumatoid arthritis (RA). LCA, a dibenzylbutane lignan extracted from the roots of traditional medicinal plant Litsea cubeba(Lour.) Pers., has demonstrated promising anti-inflammatory activity. In this study, a series of novel LCA derivatives were designed, synthesized, and evaluated for anti-inflammatory activity. Lipopolysaccharide (LPS)-induced RAW 264.7 cell model experiments showed that compound 10h(at 20 μM of concentration) had the strongest inhibitory effect on NO release, and inhibited the secretion and gene expression levels of interleukin (IL)-1β, IL-6, and tumor necrosis factor (TNF)-α in vitro.In addition, western blot, immunofluorescence, and molecular docking showed that the anti-inflammatory mechanism of compound 10hmay be related to the nuclear factor (NF)-κB signalling pathway. In vivostudies based on a carrageenan-induced mouse paw edema model have shown significant anti-inflammatory activity of compound 10hat 20 mg kg−1. Preliminary in vitroand in vivostudies indicate that compound 10hhas the potential to be developed as a novel anti-inflammatory agent.

Polycomb Repressive Complex 1 (PRC1) is associated with transcriptional silencing, and its dysregulation plays an important role in various cancers. Well-characterized PRC1 inhibitors can facilitate the exploration of PRC1 inhibition as therapeutic agents. By employing an NMR-based fragment screening approach, we have previously identified a very weak millimolar ligand RB-1, which directly binds to RING1B-BMI1. Then, we reported a low-micromolar PRC1 inhibitor, RB-3, which is active in leukemic cells, showing inhibition of H2A ubiquitylation and modulation of target genes. Here, we describe details of the optimization campaign of RB-1into potent PRC1 inhibitors by guiding the SAR employing two NMR approaches and a probe-based biochemical assay. These efforts, combined with medicinal chemistry optimization, resulted in the development of RB-3and slightly improved RB-4. We have demonstrated that RB-4binds to both RING1A and RING1B proteins and inhibits the activity of RING1B-BMI1 and RING1B-PCGF1, representing both canonical and noncanonical PRC1 complexes.

A highly efficient and mild method for [3 ​+ ​2] cycloaddition of β-sulfonyl-α,β-unsaturated ketones with terminal allenoates was well-explored and developed. The reactions were successfully performed by applying multifunctional chiral phosphine P6which was screened from eight chiral phosphorus reagents to finally result in a variety of enantioenriched sulfone-substituted cyclopentenes with two chiral centers (up to 81% yield with 94% ee). Moreover, 2.5 ​mol% catalytic equivalents were proved to be feasible when this reaction was performed on a 10 ​mmol scale.

Phosphorylated di-, tri- and tetra-saccharides of β-1,2-mannan antigen derived from Candida albicans(C. albicans) cell wall were synthesized and covalently conjugated with keyhole limpet hemocyanin (KLH) and human serum albumin (HSA) viaa bifunctional linker under mild conditions. The semi-synthetic β-1,2-mannoside–KLH conjugates were evaluated for the immunization of BALB/c mice. The ELISA results revealed that all three conjugates could elicit high levels of specific IgG antibodies and the acquired antisera could effectively identify the β-1,2-mannan epitope. Furthermore, the immunofluorescence and flow cytometry assays also uncovered that the induced antibodies, especially that obtained from immunization with β-1,2-mannotriose–KLH conjugate (1b), could bind well to fungi cell. Eventually, the structure–immunogenicity relationship analysis of β-mannan showed that the length of oligo-β-mannoses had a big impact on their immunogenicity and β-1,2-mannotriose showed the strongest immunogenicity. The results suggested the great potential of β-1,2-mannotriose–KLH conjugate as an antifungal vaccine candidate.

In recent years, the development of targeted covalent inhibitors has gained popularity around the world. Specific groups (electrophilic warheads) form irreversible bonds with the side chain of nucleophilic amino acid residues, thus changing the function of biological targets such as proteins. Since the first targeted covalent inhibitor was disclosed in the 1990s, great efforts have been made to develop covalent ligands from known reversible leads or drugs by addition of tolerated electrophilic warheads. However, high reactivity and “off-target” toxicity remain challenging issues. This review covers the concept of targeted covalent inhibition to diseases, discusses traditional and interdisciplinary strategies of cysteine-focused covalent drug discovery, and exhibits newly disclosed electrophilic warheads majorly targeting the cysteine residue. Successful applications to address the challenges of designing effective covalent drugs are also introduced.

Correction for ‘Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents’ by Zhen Wang et al., RSC Med. Chem., 2024, https://doi.org/10.1039/d4md00053f.

SIRT5 is a member of the sirtuin family of NAD+-dependent protein lysine deacylases implicated in a variety of physiological processes. SIRT5 removes negatively charged malonyl, succinyl, and glutaryl groups from lysine residues and thereby regulates multiple enzymes involved in cellular metabolism and other biological processes. SIRT5 is overexpressed in human breast cancers and other malignancies, but little is known about the therapeutic potential of SIRT5 inhibition for treating cancer. Here we report that genetic SIRT5disruption in breast cancer cell lines and mouse models caused increased succinylation of IDH2 and other metabolic enzymes, increased oxidative stress, and impaired transformation and tumorigenesis. We, therefore, developed potent, selective, and cell-permeable small-molecule SIRT5 inhibitors. SIRT5 inhibition suppressed the transformed properties of cultured breast cancer cells and significantly reduced mammary tumor growth in vivo, in both genetically engineered and xenotransplant mouse models. Considering that Sirt5knockout mice are generally normal, with only mild phenotypes observed, these data establish SIRT5 as a promising target for treating breast cancer. The new SIRT5 inhibitors provide useful probes for future investigations of SIRT5 and an avenue for targeting SIRT5 as a therapeutic strategy.

Polycomb repressive complex 1 (PRC1) is an essential chromatin-modifying complex that monoubiquitinates histone H2A and is involved in maintaining the repressed chromatin state. Emerging evidence suggests PRC1 activity in various cancers, rationalizing the need for small-molecule inhibitors with well-defined mechanisms of action. Here, we describe the development of compounds that directly bind to RING1B–BMI1, the heterodimeric complex constituting the E3 ligase activity of PRC1. These compounds block the association of RING1B–BMI1 with chromatin and inhibit H2A ubiquitination. Structural studies demonstrate that these inhibitors bind to RING1B by inducing the formation of a hydrophobic pocket in the RING domain. Our PRC1 inhibitor, RB-3, decreases the global level of H2A ubiquitination and induces differentiation in leukemia cell lines and primary acute myeloid leukemia (AML) samples. In summary, we demonstrate that targeting the PRC1 RING domain with small molecules is feasible, and RB-3 represents a valuable chemical tool to study PRC1 biology.

Pulmonary arterial hypertension (PAH) is a devastating disease that can lead to right ventricular failure and premature death. Although approved drugs have been shown to be safe and effective, PAH remains a severe clinical condition, and the long-term survival of patients with PAH is still suboptimal. Thus, potential therapeutic targets and new agents to treat PAH are urgently needed. In recent years, a variety of related pathways and potential therapeutic targets have been found, which brings new hope for PAH therapy. In this perspective, not only are the marketed drugs used to treat PAH summarized but also the recently developed novel pharmaceutical therapies currently in clinical trials are discussed. Furthermore, the advances in natural products as potential treatment for PAH are also updated.

Sirtuin 2 (SIRT2) is a protein lysine deacylase that has been indicated as a therapeutic target for cancer. To further establish the role of SIRT2 in cancers, it is necessary to develop selective and potent inhibitors. Here, we report the facile synthesis of novel lysine-derived thioureas as mechanism-based SIRT2 inhibitors with anticancer activity. Compounds AF8, AF10, and AF12selectively inhibited SIRT2 with IC50values of 0.06, 0.15, and 0.08 μM, respectively. Compounds AF8and AF10demonstrated broad cytotoxicity amongst cancer cell lines, but minimal toxicity in noncancerous cells. AF8and AF10inhibited the anchorage-independent growth of human colorectal cancer cell line HCT116 with GI50values of ∼7 μM. Furthermore, AF8potently inhibited tumor growth in a HCT116 xenograft murine model, supporting that SIRT2 is a viable therapeutic target for colorectal cancer.

Pathological aggregation of essentially dissociated Transthyretin (TTR) monomer proteins, driven by misfolding and self-interaction, is associated with Transthyretin amyloidosis (ATTR) disease. The TTR monomer proteins consist of several fragments that tend to self-aggregate. Recent experimental studies showed that the sequence of residues TTR91–96plays an important role in self-aggregation. However, the mechanisms underlying the misfolding and aggregation of the TTR91–96monomers are still unknown. In this study, we used microsecond molecular dynamics simulations to investigate the misfolding and self-assembly of TTR91–96Octamers. We also investigated E92P and V94P mutants for comparative analysis. The analysis indicates that hydrophobic interactions and π–π stacking patterns play important roles in reducing the β-sheet content in the V94P and E92P mutants. Additionally, our findings reveal the conformational transition of TTR91–96octamer from closed β-barrel, open β-barrel to the β-bilayer aggregation. We further elucidate the dynamic mechanism of the transition from intermediate states to stable states. Overall, our research may contribute to the development of drug design to combat fibrous amyloid fibrous diseases.

Directly blocking the Keap1–Nrf2 pathway is a promising strategy for the mitigation of acute lung injury (ALI). Peptide Keap1–Nrf2 inhibitors have been reported to have a high Keap1 binding affinity. However, these inhibitors showed weak activity in cells and/or animals. In this study, we designed a series of linear peptides from an Nrf2-based 9-mer Ac-LDEETGEFL-NH2. To improve the cellular activity, we further designed cyclic peptides based on the crystal complex of Keap1 with a linear peptide. Among them, cyclic 9-mer ZC9targeting Keap1 showed a better affinity (KD2= 51 nM). Specifically, it exhibited an acceptable water solubility (>38 mg/mL), better cell permeability, cell activity, and metabolic stability (serum t1/2> 24 h). In the in vitro LPS-induced oxidative damages and ALI model, ZC9showed significant dose–response reversal activity without apparent toxicity. In conclusion, our results suggested ZC9as a lead cyclic peptide targeting the Keap1–Nrf2 pathway for ALI clinical treatment.

Lithium-ion batteries are at risk of immersion in seawater during practical applications, presenting a substantial safety challenge. In this work, the thermal runaway characteristics and degree of corrosion of 18,650 lithium-ion batteries were examined at various NaCl concentrations and states of charge (SOCs). Results indicate that corrosion increases with both NaCl concentration and SOC. The onset time (tTR) and onset temperature (TTR) of thermal runaway decrease with increasing SOC. The TTRis considerably higher for batteries immersed in 5 % NaCl solution compared to batteries without immersion and immersed in 2.5 % NaCl solution, while the tTRdemonstrates the opposite trend. The maximum temperature (Tmax) of thermal runaway initially increases and then decreases with increasing salt concentration for batteries with SOC >100 %, while it decreases as salt concentration increases for batteries with SOC <100 %. The mass loss of immersion increases with the increase in salt concentration and SOC. The mass loss and peak heat flux during thermal runaway of batteries immersed in salt solution are significantly lower than those of fresh batteries. These results will contribute to a better understanding of the thermal runaway risk of lithium-ion batteries with different SOCs following immersion in salt solution.

Artemisinin is isolated from Artemisia annua L. with peroxide-containing sesquiterpene lactone structure. Because of its unique structural characteristics and promising anticancer, antivirus activities, it has recently received increasing attention. The aim of this review is to summarize recent discoveries of artemisinin's novel derivatives with new pharmaceutical effects beyond malaria with a focus on its antitumor and antivirus activity, as well as potential results of combination therapy with other clinical drugs.

Splitting touching cells is important for medical image processing and analysis system. In this paper, a novel strategy is proposed to separate ellipse-like or circle-like touching cells in which different algorithms are used according to the concave-point cases of touching domains. In the strategy, a concave-point extraction and contour segmentation methods for cells in series and in parallel are used for the images with distinct concave points, and an improved watershed algorithm with multi-scale gradient and distance transformation is adopted for the images with un-distinct or complex concave points. In order to visualize each whole cell, ellipse fitting is used to process the segments. Experimental results show that, for the cell images with distinct concave points, both of the two algorithms can achieve good separating results, but the concave-point based algorithm is more efficient. However, for the cell images with unobvious or complex concave points, the improved watershed based algorithm can give satisfying segmenting results.

Development of non‐coke ironmaking process in China is presented. It is concluded that coal‐based rotary kiln is still the main process for direct reduced iron (DRI) production in the near future in China. The most important problems of DRI production in China are small production scale and heavy environment pollution. Now the gas‐based shaft furnace process has become one of the significant processes of DRI production in China. The market demand for DRI production in China is continuously increasing. Due to the tense supply of coking coal and its heavy environmental load, more steel plants in China will use smelting reduction (SR) technology.

Dispiro peroxides (III),(VI),(VIII), and (X) are prepared either by coozonolysis of oxime ether (I) and ketoester (II), or by acid‐catalyzed condensation of β‐hydroperoxy alcohols (V) with adamantanone (IV) or cyclohexanone (IX), or by Re2O7‐catalyzed condensation of dihydroperoxide esters (VII) with adamantanone (IV).

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.