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PDBsum entry 5g21
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References listed in PDB file
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Key reference
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Title
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Structure-Guided optimization of quinoline inhibitors ofplasmodium n-Myristoyltransferase.
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Authors
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V.Goncalves,
J.A.Brannigan,
A.Laporte,
A.S.Bell,
S.M.Roberts,
A.J.Wilkinson,
R.J.Leatherbarrow,
E.W.Tate.
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Ref.
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Medchemcomm, 2017,
8,
191-197.
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PubMed id
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Abstract
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The parasitePlasmodium vivaxis the most widely distributed cause of
recurring malaria.N-Myristoyltransferase (NMT), an enzyme that catalyses
the covalent attachment of myristate to the N-terminal glycine of substrate
proteins, has been described as a potential target for the treatment of this
disease. Herein, we report the synthesis and the structure-guided optimization
of a series of quinolines with balanced activity against bothPlasmodium
vivaxandPlasmodium falciparum N-myristoyltransferase (NMT).
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