7040-92-8Relevant academic research and scientific papers
Phosphylated tyrosine in albumin as a biomarker of exposure to organophosphorus nerve agents
Williams, Nichola H.,Harrison, John M.,Read, Robert W.,Black, Robin M.
, p. 627 - 639 (2007)
The organophosphorus nerve agents sarin, soman, cyclosarin and tabun phosphylate a tyrosine residue on albumin in human blood. These adducts may offer relatively long-lived biological markers of nerve agent exposure that do not 'age' rapidly, and which ar
Solid-phase synthesis of phosphonylated peptides
MacDonald, Mary,Lanier, Marion,Cashman, John
supporting information; experimental part, p. 1951 - 1954 (2010/10/19)
We report the solid-phase syntheses of two series of phosphonylated peptides using Fmoc-protected amino acids. The peptides corresponded to regions containing phosphonylated Ser195 in the active site of butyrylcholinesterase and Tyr411 of human serum albu
Analogues with fluorescent leaving groups for screening and selection of enzymes that efficiently hydrolyze organophosphorus nerve agents
Brise?o-Roa, Luis,Hill, Jim,Notman, Stuart,Sellers, David,Smith, Andy P.,Timperley, Christopher M.,Wetherell, Janet,Williams, Nichola H.,Williams, Gareth R.,Fersht, Alan R.,Griffiths, Andrew D.
, p. 246 - 255 (2007/10/03)
Enzymes that efficiently hydrolyze highly toxic organophosphorus nerve agents could potentially be used as medical countermeasures. As sufficiently active enzymes are currently unknown, we synthesized twelve fluorogenic analogues of organophosphorus nerve agents with the 3-chloro-7-oxy-4- methylcoumarin leaving group as probes for high-throughput enzyme screening. This set included analogues of the pesticides paraoxon, parathion, and dimefox, and the nerve agents DFP, tabun, sarin, cyclosarin, soman, VX, and Russian-VX. Data from inhibition of acetylcholinesterase, in vivo toxicity tests of a representative analogue (cyclosarin), and kinetic studies with phosphotriesterase (PTE) from Pseudomonas diminuta, and a mammalian serum paraoxonase (PON1), confirmed that the analogues mimic the parent nerve agents effectively. They are suitable tools for high-throughput screens for the directed evolution of efficient nerve agent organophosphatases.
