Publications by authors named "G E Peckham"
As the desire for a shortened design/make/test/learn cycle increases in early drug discovery, the pressure to rapidly deliver drug metabolism pharmacokinetic data continues to rise. From a bioanalytical standpoint, assays are challenging because they are amenable to automation and thus capable of generating a high number of samples for analysis. To keep up with analysis demands, automated method development workflows, rapid sample analysis approaches and efficient data analysis software must be utilized.
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- A new class of H-PGDS inhibitors, specifically 2-phenylimidazo[1,2-a]pyridine-6-carboxamide, was discovered through a virtual screening process at GlaxoSmithKline.
- Detailed analysis of crystal structures and structure-activity relationships (SAR) resulted in the identification of a powerful, orally active imidazopyridine inhibitor, designated as 20b.
- The text discusses the identification of two types of inhibitors, their synthesis processes, and the challenges encountered during the research.
Article Synopsis
- GlaxoSmithKline and Astex Pharmaceuticals identified GSK2894631A as a strong H-PGDS inhibitor but faced CNS toxicity with prolonged high doses.
- To reduce brain penetration, they developed aza-quinolines, modifying nitrogen positions to improve enzyme compatibility.
- The research culminated in discovering 1,8-naphthyridine, a potent and safer H-PGDS inhibitor effective in various inflammatory models without CNS side effects.
With the goal of discovering more selective anti-inflammatory drugs, than COX inhibitors, to attenuate prostaglandin signaling, a fragment-based screen of hematopoietic prostaglandin D synthase was performed. The 76 crystallographic hits were sorted into similar groups, with the 3-cyano-quinoline 1a (FP IC = 220,000 nM, LE = 0.43) being a potent member of the 6,6-fused heterocyclic cluster.
View Article and Find Full Text PDFPortable detection and quantitation methods for (anthrax) spores in pure culture or in environmental samples are lacking. Here, an amperometric immunoassay has been developed utilizing immunomagnetic separation to capture the spores and remove potential interferents from test samples followed by amperometric measurement on a field-portable instrument. Antibody-conjugated magnetic beads and antibody-conjugated glucose oxidase were used in a sandwich format for the capture and detection of target spores.
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