A Hit-to-Lead optimisation programme was carried out on the high throughput screening hit, the triazolethiol 1, resulting in the discovery of the potent, orally bioavailable triazolethiol CXCR2 receptor antagonist 45.
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Apigenin, a dietary flavonoid with notable anti-cancer properties, has emerged as a promising candidate for the treatment of neurodegenerative disorders, particularly Alzheimer's disease (AD). While extensively studied for its ability to modulate key molecular pathways in cancers, apigenin also exerts neuroprotective effects by reducing neuroinflammation, protecting neurons from oxidative stress, and enhancing neuronal survival and synaptic plasticity. This dual functionality makes apigenin an intriguing therapeutic option for diseases like AD, where kinase dysregulation plays a central role.
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Bacterial biofilms are surface-attached communities consisting of non-replicating persister cells encased within an extracellular matrix of biomolecules. Unlike bacteria that have acquired resistance to antibiotics, persister cells enable biofilms to demonstrate innate tolerance toward all classes of conventional antibiotic therapies. It is estimated that 50-80% of bacterial infections are biofilm associated, which is considered the underlying cause of chronic and recurring infections.
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View Article and Find Full Text PDFDevelopment of a Second-Generation, Chemical Probe for PIKfyve.
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