Publications by authors named "C H Lumb"
The development of new antimalarials is required because of the threat of resistance to current antimalarial therapies. To discover new antimalarial chemotypes, we screened the Janssen Jumpstarter library against the asexual parasite and identified the 7--substituted-3-oxadiazole quinolone hit class. We established the structure-activity relationship and optimized the antimalarial potency.
View Article and Find Full Text PDFThe tachykinin neuropeptide substance P (SP) is the canonical agonist peptide for the neurokinin 1 receptor (NK R). More recently, it has also been shown to activate the Mas-related G protein-coupled receptor X2 (MRGPRX2) receptor on mast cells (MCs), triggering degranulation and release of inflammatory mediators. SP undergoes rapid C-terminal truncation in vivo by a number of proteases to generate the metabolites SP(1-9)-COOH and in particular SP(1-7)-COOH.
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- This study explores the nicotinic acetylcholine receptor (nAChR) gene family in D. melanogaster to identify specific receptor subunits that insects use to respond to various insecticides, including neonicotinoids, spinosyns, and sulfoximines.
- Using CRISPR/Cas9 gene editing, the researchers created mutants for several nAChR subunit genes and discovered that the spinosad insecticide specifically targets the Dα6 subunit, while neonicotinoids target multiple receptor subtypes.
- The results indicate a significant overlap in resistance mechanisms among different insect species, with certain mutations in subunit genes strongly correlating with
Objective: To understand health-related issues in women following mesh-augmented prolapse surgery.
Design: Inductive thematic analysis of free-text comments from participants in a cross-sectional study of laparoscopic mesh sacrohysteropexy.
Setting: Tertiary urogynaecology centres, United Kingdom.
Nanoparticle-mediated drug delivery is especially useful for targets within endosomes because of the endosomal transport mechanisms of many nanomedicines within cells. Here, we report the design of a pH-responsive, soft polymeric nanoparticle for the targeting of acidified endosomes to precisely inhibit endosomal signalling events leading to chronic pain. In chronic pain, the substance P (SP) neurokinin 1 receptor (NKR) redistributes from the plasma membrane to acidified endosomes, where it signals to maintain pain.
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