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The pp60c-Src inhibitor PP1 is non-competitive against ATP
Authors:Karni Rotem  Mizrachi Sarit  Reiss-Sklan Ella  Gazit Aviv  Livnah Oded  Levitzki Alexander
Institution:Department of Biological Chemistry, The Alexander Silberman Institute of Life Sciences, The Hebrew University of Jerusalem, Israel.
Abstract:The C7-cyclitol 2-epi-5-epi-valiolone is the first precursor of the cyclitol moiety of the greek small letter alpha-glucosidase inhibitor acarbose in Actinoplanes sp. SE50. The 2-epi-5-epi-valiolone becomes phosphorylated at C7 by the ATP dependent kinase AcbM prior to the next modifications. Preliminary data gave evidences that the AcbO protein could catalyse the first modification step of 2-epi-5-epi-valiolone-7-phosphate. Therefore, the AcbO protein, the encoding gene of which is also part of the acbKMLNOC operon, was overproduced and purified. Indeed the purified protein catalysed the 2-epimerisation of 2-epi-5-epi-valiolone-7-phosphate. The chemical structure of the purified reaction product was proven by nuclear magnetic resonance spectroscopy to be 5-epi-valiolone-7-phosphate.
Keywords:Actinoplanes sp    Acarbose  Biosynthesis  C7-cyclitol
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