@article{fdi:010093043,
  title = {{N}ew potent {EV}-{A}71 antivirals targeting capsid},
  author = {{R}oux, {H}. and {T}ouret, {F}ranck and {C}oluccia, {A}. and {K}houmeri, {O}. and {D}i {G}iorgio, {C}. and {M}ajdi, {C}. and {S}ciò, {P}. and {S}ilvestri, {R}. and {V}anelle, {P}. and {R}oche, {M}.},
  editor = {},
  language = {{ENG}},
  abstract = {{T}he enterovirus is a genus of single-stranded, highly diverse positive-sense {RNA} viruses, including {H}uman {E}nterovirus {A}-{D} and {H}uman {R}hinovirus {A}-{C} species. {T}hey are responsible for numerous diseases and some infections can progress to life-threatening complications, particularly in children or immunocompromised patients. {T}o date, there is no treatment against enteroviruses on the market, except for polioviruses (vaccine) and {EV}-{A}71 (vaccine in {C}hina). {F}ollowing a decrease in enterovirus infections during and shortly after the ({SARS}-{C}ov2) lockdown, enterovirus outbreaks were once again detected, notably in young children. {T}his reemergence highlights on the need to develop broad-spectrum treatment against enteroviruses. {O}ver the last year, our research team has identified a new class of small-molecule inhibitors showing anti-{EV} activity. {T}argeting the well-known hydrophobic pocket in the viral capsid, these compounds show micromolar activity against {EV}-{A}71 and a high selectivity index ({SI}) (5h: {EC}50, {MRC}-5 = 0.57 ?{M}, {CC}50, {MRC}-5 >20 ?{M}, {SI} > 35; {EC}50, {RD} = 4.38 ?{M}, {CC}50, {RD} > 40 ?{M}, {SI} > 9; 6c: {EC}50, {MRC}-5 = 0.29 ?{M}, {CC}50, {MRC}-5 >20 ?{M}, {SI} > 69; {EC}50, {RD} = 1.66 ?{M}, {CC}50, {RD} > 40 ?{M}, {SI} > 24; {R}eference: {V}apendavir {EC}50, {MRC}-5 = 0.36 ?{M}, {CC}50, {MRC}-5 > 20 ?{M}, {EC}50, {RD} = 0.53 ?{M}, {CC}50, {RD} > 40 ?{M}, {SI} > 63). {T}he binding mode of these compounds in complex with enterovirus capsids was analyzed and showed a series of conserved interactions. {C}onsequently, 6c and its derivatives are promising candidates for the treatment of enterovirus infections.},
  keywords = {},
  booktitle = {},
  journal = {{E}uropean {J}ournal of {M}edicinal {C}hemistry},
  volume = {276},
  numero = {},
  pages = {116658 [18 ]},
  ISSN = {0223-5234},
  year = {2024},
  DOI = {10.1016/j.ejmech.2024.116658},
  URL = {https://www.documentation.ird.fr/hor/fdi:010093043},
}