Sulfur incorporation generally improves Ricin inhibition in pterin-appended glycine-phenylalanine dipeptide mimics

…, G Gao, R Saito, AF Monzingo, KR Jasheway…

文献索引：Wiget, Paul A.; Manzano, Lawrence A.; Pruet, Jeff M.; Gao, Grace; Saito, Ryota; Monzingo, Arthur F.; Jasheway, Karl R.; Robertus, Jon D.; Anslyn, Eric V. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6799 - 6804

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被引用次数: 2

摘要

Abstract Several 7-aminoamido-pterins were synthesized to evaluate the electronic and biochemical subtleties observed in the 'linker space'when N-{N-(pterin-7-yl) carbonylglycyl}-l- phenylalanine 1 was bound to the active site of RTA. The gylcine–phenylalanine dipeptide analogs included both amides and thioamides. Decarboxy gly-phe analog 2 showed a 6.4- fold decrease in potency (IC 50= 128 μM), yet the analogous thioamide 7 recovered the ...