@article{fdi:010074875,
  title = {{S}ynergistic {AML} cell death induction by marine cytotoxin (+)-1({R}), 6({S}), 1'({R}), 6'({S}), 11({R}), 17({S})-fistularin-3 and bcl-2 inhibitor {V}enetoclax},
  author = {{F}lorean, {C}. and {K}im, {K}. {R}. and {S}chnekenburger, {M}. and {K}im, {H}. {J}. and {M}oriou, {C}. and {D}ebitus, {C}{\'e}cile and {D}icato, {M}. and {A}l-{M}ourabit, {A}. and {H}an, {B}. {W}. and {D}iederich, {M}.},
  editor = {},
  language = {{ENG}},
  abstract = {{T}reatment of acute myeloid leukemia ({AML}) patients is still hindered by resistance and relapse, resulting in an overall poor survival rate. {R}ecently, combining specific {B}-cell lymphoma ({B}cl)-2 inhibitors with compounds downregulating myeloid cell leukemia ({M}cl)-1 has been proposed as a new effective strategy to eradicate resistant {AML} cells. {W}e show here that 1({R}), 6({S}), 1'({R}), 6'({S}), 11({R}), 17({S})-fistularin-3, a bromotyrosine compound of the fistularin family, isolated from the marine sponge {S}uberea clavata, synergizes with {B}cl-2 inhibitor {ABT}-199 to efficiently kill {M}cl-1/{B}cl-2-positive {AML} cell lines, associated with {M}cl-1 downregulation and endoplasmic reticulum stress induction. {T}he absolute configuration of carbons 11 and 17 of the fistularin-3 stereoisomer was fully resolved in this study for the first time, showing that the fistularin we isolated from the marine sponge {S}ubarea clavata is in fact the (+)-11({R}), 17({S})-fistularin-3 stereoisomer keeping the known configuration 1({R}), 6({S}), 1'({R}), and 6'({S}) for the verongidoic acid part. {D}ocking studies and in vitro assays confirm the potential of this family of molecules to inhibit {DNA} methyltransferase 1 activity.},
  keywords = {acute myeloid leukemia ; {ABT}-199 ; {M}cl-1 ; bromotyrosine ; (+)-11({R}) 17({S})-fistularin-3 ; configuration ; anticancer drug combination},
  booktitle = {},
  journal = {{M}arine {D}rugs},
  volume = {16},
  numero = {12},
  pages = {art. 518 [19 p.]},
  ISSN = {1660-3397},
  year = {2018},
  DOI = {10.3390/md16120518},
  URL = {https://www.documentation.ird.fr/hor/fdi:010074875},
}