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10.1021/acsinfecdis.7b00197

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suck abstract from ncbi


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pmid29436819
      ACS+Infect+Dis 2018 ; 4 (4 ): 431-444
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  • Fragment-Based Screening of a Natural Product Library against 62 Potential Malaria Drug Targets Employing Native Mass Spectrometry #MMPMID29436819
  • Vu H ; Pedro L ; Mak T ; McCormick B ; Rowley J ; Liu M ; Di Capua A ; Williams-Noonan B ; Pham NB ; Pouwer R ; Nguyen B ; Andrews KT ; Skinner-Adams T ; Kim J ; Hol WGJ ; Hui R ; Crowther GJ ; Van Voorhis WC ; Quinn RJ
  • ACS Infect Dis 2018[Apr]; 4 (4 ): 431-444 PMID29436819 show ga
  • Natural products are well known for their biological relevance, high degree of three-dimensionality, and access to areas of largely unexplored chemical space. To shape our understanding of the interaction between natural products and protein targets in the postgenomic era, we have used native mass spectrometry to investigate 62 potential protein targets for malaria using a natural-product-based fragment library. We reveal here 96 low-molecular-weight natural products identified as binding partners of 32 of the putative malarial targets. Seventy-nine (79) fragments have direct growth inhibition on Plasmodium falciparum at concentrations that are promising for the development of fragment hits against these protein targets. This adds a fragment library to the published HTS active libraries in the public domain.
  • |Antimalarials/*isolation & purification/*pharmacology [MESH]
  • |Biological Products/*isolation & purification/*pharmacology [MESH]
  • |Drug Evaluation, Preclinical/*methods [MESH]
  • |Mass Spectrometry/*methods [MESH]
  • |Plasmodium falciparum/*drug effects/growth & development [MESH]
  • |Protein Binding [MESH]


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