@article{fdi:010080019,
  title = {{A} photoalkylative fluorogenic probe of guttiferone {A} for live cell imaging and proteome labeling in {P}lasmodium falciparum},
  author = {{D}uval, {R}omain and {C}ottet, {K}. and {B}laud, {M}. and {M}erckx, {A}. and {H}ouze, {S}. and {G}rellier, {P}. and {L}allemand, {M}. {C}. and {M}ichel, {S}.},
  editor = {},
  language = {{ENG}},
  abstract = {{G}uttiferone {A} ({GA}) 1, a polycyclic polyprenylated acylphloroglucinol ({PPAP}) isolated from the plant {S}ymphonia globulifera ({C}lusiaceae), constitutes a novel hit in antimalarial drug discovery. {PPAP}s do not possess identified biochemical targets in malarial parasites up to now. {T}owards this aim, we designed and evaluated a natural product-derived photoactivatable probe {AZC}-{GA} 5, embedding a photoalkylative fluorogenic motif of the 7-azidocoumarin ({AZC}) type, devoted to studying the affinity proteins interacting with {GA} in {P}lasmodium falciparum. {P}robe 5 manifested a number of positive functional and biological features, such as (i) inhibitory activity in vitro against {P}. falciparum blood-stages that was superimposable to that of {GA} 1, dose-response photoalkylative fluorogenic properties (ii) in model conditions using bovine serum albumin ({BSA}) as an affinity protein surrogate, (iii) in live {P}. falciparum-infected erythrocytes, and (iv) in fresh {P}. falciparum cell lysate. {F}luorogenic signals by photoactivated {AZC}-{GA} 5 in biological settings were markedly abolished in the presence of excess {GA} 1 as a competitor, indicating significant pharmacological specificity of the designed molecular probe relative to the native {PPAP}. {T}hese results open the way to identify the detected plasmodial proteins as putative drug targets for the natural product 1 by means of proteomic analysis.},
  keywords = {{G}uttiferone {A} ; {P}lasmodium falciparum ; 7-azidocoumarin ; photoactivation ; fluorogenesis},
  booktitle = {},
  journal = {{M}olecules},
  volume = {25},
  numero = {21},
  pages = {5139 [13 ]},
  ISSN = {1420-3049},
  year = {2020},
  DOI = {10.3390/molecules25215139},
  URL = {https://www.documentation.ird.fr/hor/fdi:010080019},
}