selective inhibitors of protozoan protein n-myristoyltransferases as starting points for tropical disease medicinal chemistry programs原生动物蛋白质的选择性抑制剂n-myristoyltransferases作为起点的热带疾病药物化学项目.pdfVIP

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selective inhibitors of protozoan protein n-myristoyltransferases as starting points for tropical disease medicinal chemistry programs原生动物蛋白质的选择性抑制剂n-myristoyltransferases作为起点的热带疾病药物化学项目.pdf

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selective inhibitors of protozoan protein n-myristoyltransferases as starting points for tropical disease medicinal chemistry programs原生动物蛋白质的选择性抑制剂n-myristoyltransferases作为起点的热带疾病药物化学项目

Selective Inhibitors of Protozoan Protein N- myristoyltransferases as Starting Points for Tropical Disease Medicinal Chemistry Programs 1 ¤ 1 2 3 3 Andrew S. Bell * , James E. Mills , Gareth P. Williams , James A. Brannigan , Anthony J. Wilkinson , 4 5 5 6 7 Tanya Parkinson , Robin J. Leatherbarrow , Edward W. Tate , Anthony A. Holder , Deborah F. Smith 1 Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Kent, United Kingdom, 2 High Throughput Screening Center of Emphasis, Pfizer Worldwide Research and Development, Kent, United Kingdom, 3 Department of Chemistry, University of York, York, United Kingdom, 4 Opportunities for Partnership in Medicine, Pfizer Worldwide Research and Development, Kent, United Kingdom, 5 Institute of Chemical Biology, Department of Chemistry, Imperial College, London, United Kingdom, 6 Division of Parasitology, Medical Research Council National Institute for Medical Research, London, United Kingdom, 7 Department of Biology, University of York, York, United Kingdom Abstract Inhibition of N-myristoyltransferase has been validated pre-clinically as a target for the treatment of fungal and trypanosome infections, using species-specific inhibitors. In order to identify inhibitors of protozoan NMTs, we chose to screen a diverse subset of the Pfizer corporate collection against Plasmodium falciparum and Leishmania donovani NMTs. Primary screening hits against either enzyme were tested for selectivity over both human NMT isoforms (Hs1 and Hs2) and for broad-spectrum