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View article: PET-MRI biomarkers reveal efficacy of a novel NLRP3 inhibitor in Parkinson’s disease models
PET-MRI biomarkers reveal efficacy of a novel NLRP3 inhibitor in Parkinson’s disease models Open
Parkinson’s disease is one of the fastest-growing neurodegenerative disorders, with no effective treatments to modify its progression. Microglial-driven neuroinflammation, mediated by NLRP3 inflammasome activation, plays a key role in dise…
View article: Glycoproteomic measurement of site-specific polysialylation
Glycoproteomic measurement of site-specific polysialylation Open
Polysialylation is the enzymatic addition of a highly negatively charged sialic acid polymer to the non-reducing termini of glycans. Polysialylation plays an important role in development, and is involved in neurological diseases, neural t…
View article: Structure-Function Studies of Polymyxin B Lipononapeptides
Structure-Function Studies of Polymyxin B Lipononapeptides Open
The emerging threat of infections caused by highly drug-resistant bacteria has prompted a resurgence in the use of the lipodecapeptide antibiotics polymyxin B and colistin as last resort therapies. Given the emergence of resistance to thes…
View article: CCDC 1869137: Experimental Crystal Structure Determination
CCDC 1869137: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity
Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity Open
Tuberculosis and parasitic diseases, such as giardiasis, amebiasis, leishmaniasis, and trypanosomiasis, all urgently require improved treatment options. Recently, it has been shown that antitubercular bicyclic nitroimidazoles such as preto…
View article: Protein-inspired antibiotics active against vancomycin- and daptomycin-resistant bacteria
Protein-inspired antibiotics active against vancomycin- and daptomycin-resistant bacteria Open
The public health threat posed by a looming ‘post-antibiotic’ era necessitates new approaches to antibiotic discovery. Drug development has typically avoided exploitation of membrane-binding properties, in contrast to nature’s control of b…
View article: CCDC 1470361: Experimental Crystal Structure Determination
CCDC 1470361: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Identification, Synthesis, and Biological Evaluation of the Major Human Metabolite of NLRP3 Inflammasome Inhibitor MCC950
Identification, Synthesis, and Biological Evaluation of the Major Human Metabolite of NLRP3 Inflammasome Inhibitor MCC950 Open
MCC950 is an orally bioavailable small molecule inhibitor of the NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome that exhibits remarkable activity in multiple models of inflammatory disease. Incubation of MCC950 wi…
View article: Fluorescent Trimethoprim Conjugate Probes To Assess Drug Accumulation in Wild Type and Mutant <i>Escherichia coli</i>
Fluorescent Trimethoprim Conjugate Probes To Assess Drug Accumulation in Wild Type and Mutant <i>Escherichia coli</i> Open
Reduced susceptibility to antimicrobials in Gram-negative bacteria may result from multiple resistance mechanisms, including increased efflux pump activity or reduced porin protein expression. Up-regulation of the efflux pump system is clo…
View article: Nitroimidazole carboxamides as antiparasitic agents targeting Giardia lamblia, Entamoeba histolytica and Trichomonas vaginalis
Nitroimidazole carboxamides as antiparasitic agents targeting Giardia lamblia, Entamoeba histolytica and Trichomonas vaginalis Open
Diarrhoeal diseases caused by the intestinal parasites Giardia lamblia and Entamoeba histolytica constitute a major global health burden. Nitroimidazoles are first-line drugs for the treatment of giardiasis and amebiasis, with metronidazol…
View article: Activity and Predicted Nephrotoxicity of Synthetic Antibiotics Based on Polymyxin B
Activity and Predicted Nephrotoxicity of Synthetic Antibiotics Based on Polymyxin B Open
The polymyxin lipodecapeptides colistin and polymyxin B have become last resort therapies for infections caused by highly drug-resistant Gram-negative bacteria. Unfortunately, their utility is compromised by significant nephrotoxicity and …
View article: Mucin Binding Reduces Colistin Antimicrobial Activity
Mucin Binding Reduces Colistin Antimicrobial Activity Open
Colistin has found increasing use in treating drug-resistant bacterial lung infections, but potential interactions with pulmonary biomolecules have not been investigated. We postulated that colistin, like aminoglycoside antibiotics, may bi…