Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed in many cancers, where it ...impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, and is associated with inferior prognosis. Pharmacological inhibition of LSD1 has been reported to significantly attenuate tumor progression in vitro and in vivo in a range of solid tumors and acute myeloid leukemia. This review will present the structural aspects of LSD1, its role in carcinogenesis, a comparison of currently available approaches for screening LSD1 inhibitors, a classification of LSD1 inhibitors, and its potential as a drug target in cancer therapy.
The rhodium(iii) complex 1 was identified as a potent Wee1 inhibitor in vitro and in cellulo. It decreased Wee1 activity and unscheduled mitotic entry, and induced cell damage and death in ...TP53-mutated triple-negative breast cancer cells. 1 represents a promising scaffold for further development of more potent metal-based Wee1 antagonists.
Transition metal complexes have attracted interest in the fields of cancer therapy, medical and environmental detection, and materials of organic light-emitting diodes (OLED). Recently, iridium(
iii
...) complexes have been explored in a reaction based way for luminescence monitoring and imaging due to their salient photophysical properties, including large Stokes shifts, long-lived luminescence and high luminescent quantum yields. This frontier article will introduce recent developments and applications of iridium(
iii
) complexes as luminescent probes for ions and biomolecules. Our outlook for this class of complexes is also discussed.
This frontier article introduces recent developments and applications of iridium(
iii
) complexes as luminescent probes for ions and biomolecules.
In recent years, transition metal complexes with their prominent photophysical properties have emerged as versatile chemosensors to probe different target analytes, including metal ions. By ...incorporating specific metal ion receptors, various iridium(III) complex-based cation sensors have been developed using different mechanisms. In this review, we survey examples of iridium(III) complex-based metal ion chemosensors that have been reported in the literature. Their design, mechanism and outlook will also be discussed.
IntroductionEpidemic obesity (‘globobesity’) has led to a considerable rise in the prevalence and incidence of many disabling conditions, including cognitive dysfunction. Recent evidence has ...suggested that habitual exercise can alleviate the deleterious effects of obesity on cognitive functioning across the lifespan. Given that there is a potential link among obesity, exercise, cognitive health and brain-derived neurotrophic factor (BDNF), this systematic review aims to critically appraise interventional trials on exercise and BDNF and to estimate the pooled effect of exercise training on BDNF levels among healthy individuals with overweight and obesity.Methods and analysisSix electronic databases—PubMed, MEDLINE, EMBASE, Web of Science, Ovid Nursing Database and SPORTDiscus—will be searched from their inception through December 2022. Only interventional studies, including randomised controlled trials and quasi-experimental studies, with full text available and reported in English will be included. The primary outcomes will be changes in BDNF levels among healthy subjects with overweight and obesity following either acute or chronic bouts of exercise interventions. Two reviewers will independently conduct data extraction and risk of bias assessment for included trials using the Physiotherapy Evidence Database Scale. We will produce a narrative synthesis, with findings categorised by sex, age groups and types of exercise training. Data will be extracted and pooled for meta-analyses using random-effects models.Ethics and disseminationNo formal ethical approval is required for this systematic review. The findings of this review will be disseminated through peer-reviewed publications.PROSPERO registration numberCRD42023414868.
A G-quadruplex-based platform has been developed for the time-resolved monitoring of ochratoxin A (OTA). The simple platform displays good sensitivity for OTA with a detection limit of 40 nM via ...steady-state emission spectroscopy. Notably, the platform showed a detection limit of 10.8 nM via time-resolved emission spectroscopy (TRES), which is about 4 times more sensitive than steady-state mode. Moreover, the probe showed excellent selectivity for OTA over other mycotoxins. Furthermore, OTA was successfully detected in actual herbal plant extracts samples. Our platform is the first to detect OTA using TRES to distinguish between the target signals versus the auto-fluorescence of real samples. This platform shows improved detection speed, accuracy and sensitivity with simple operation, low cost, and no requirement for complicated pre-processing.
•A G-quadruplex-based platform has been developed for the monitoring of OTA in herbal plant extracts samples.•This platform exhibits promising advantages including easy operation, low-cost and no complicated pre-processing required.•This platform allows the probe signal to be separated from intense background fluorescence.•The simple platform displays good sensitivity for OTA via time-resolved emission spectroscopy (TRES).
Investigating the role of lysosome dysfunction in cancer requires the development of efficient probes for lysosomes. We report herein a cyclometalated iridium(iii) complex (Ir-Ly) as a luminescent ...probe for visualizing lysosomes in cancer cells. The morpholine and hydroxy moieties within Ir-Ly provide suitable hydrophilicity and responsiveness to pH. Importantly, Ir-Ly exhibits a large Stokes shift, long lifetime and high photostability, which are important advantages for lysosome tracking in living cells.
/Objective. An explosion in global obesity epidemic poses threats to the healthcare system by provoking risks of many debilitating diseases, including cognitive dysfunction. Physical activity has ...been shown to alleviate the deleterious effects of obesity-associated cognitive deficits across the lifespan. Given the strong neuroprotective role of brain-derived neurotrophic factor (BDNF) and exercise training as a known modulator for its elevation, this systematic review sought to examine the strength of the association between exercise and BDNF levels in healthy people with overweight and obesity.
Six electronic databases (PubMed, MEDLINE, EMBASE, Web of Science, Ovid Nursing Database, and SPORTDiscus) were searched from their inceptions through December 2022. The primary outcome of interest was BDNF levels. Interventional studies (randomized and quasi-experimental) with English full text available were included. Risk of bias of the included studies was assessed using the Physiotherapy Evidence Database Scale. Data were extracted for meta-analyses by random-effects models.
Thirteen studies (n = 750), of which 69.2% (9/13) had low risk of bias, were included. In the meta-analysis, exercise interventions had no significant effect on resting BDNF levels (standardized mean difference: −0.30, 95% CI -0.80 to 0.21, P = 0.25). Subgroup analyses also indicated no effects of age and types of control groups being compared on moderating the association.
To further inform the role of BDNF in obesity-related cognitive functioning, rigorous studies with larger samples of participants and raw data available were imperatively deserved.
The high reactivity of alkyl halides towards nucleophiles renders them as acutely toxic and mutagenic agents. Therefore, it is urgent to develop simple, sensitive, and selective methods for the ...detection of alkylating agents in a wide range of scenarios. Herein, we have designed and synthesized a novel cyclometalated iridium(III) complex Ir_1 as a rapid and effective chemosensor for a range of alkyl halides based on cycloaddition reaction. Ir_1 displayed an enhanced luminescence with the increase of BnBr-thiourea concentration, within a linear range of 0.8–8 μM BnBr-thiourea, and the detection limit at a signal-to-noise ratio of 3 was as low as 0.39 μM.
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•An iridium(III) complex probe Ir_1 for alkyl halide detection has been synthesized.•Ir_1 underwent a cycloaddition reaction with S-benzylthiouronium.•Ir_1 showed high selectivity for alkyl halides.
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