Publications by authors named "P D Elkins"
Gardenia blue (GB), a widely used plant-derived food color is prepared by reaction of genipin, the aglycone of geniposide, with protein hydrolysate. Recent animal studies investigating GB toxicity have indicated blue coloration in the gastrointestinal tract, kidneys and mesenteric lymph nodes in rodents following dietary administration. This study investigated the uptake and disposition of [C]GB in male and female rats and mice administered 100 or 1000 mg/kg by gavage.
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- 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.
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.
ACS Med Chem Lett
February 2020
We report herein the discovery of isoxazole amides as potent and selective SET and MYND Domain-Containing Protein 3 (SMYD3) inhibitors. Elucidation of the structure-activity relationship of the high-throughput screening (HTS) lead compound provided potent and selective SMYD3 inhibitors. The SAR optimization, cocrystal structures of small molecules with SMYD3, and mode of inhibition (MOI) characterization of compounds are described.
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