Smith Jessica M, Vierling Ryan J, Meyers Caren Freel
Department of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA.
Medchemcomm. 2012;3:65-67. doi: 10.1039/C1MD00233C. Epub 2011 Oct 26.
DXP synthase catalyzes the formation of 1-deoxy-D-xylulose 5-phosphate, an essential precursor in pathogen isoprenoid biosynthesis. The selective inhibition of this ThDP-dependent transformation is a challenging goal in the development of isoprenoid biosynthesis inhibitors. Potent, selective inhibitors could lead to new anti-infective agents. Here, we demonstrate selective inhibition of E. coli DXP synthase by butylacetylphosphonate.
1-脱氧-D-木酮糖-5-磷酸合酶催化1-脱氧-D-木酮糖-5-磷酸的形成，1-脱氧-D-木酮糖-5-磷酸是病原体类异戊二烯生物合成中的一种必需前体。在类异戊二烯生物合成抑制剂的开发中，选择性抑制这种依赖硫胺素焦磷酸（ThDP）的转化是一个具有挑战性的目标。强效、选择性抑制剂可能会产生新的抗感染药物。在此，我们证明了丁基乙酰膦酸酯对大肠杆菌1-脱氧-D-木酮糖-5-磷酸合酶具有选择性抑制作用。
