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| Florean, Cristina; Kim, Kyung Rok; Schnekenburger, Michael; Kim, Hyun-jung; Moriou, Celine; Debitus, Cecile; Dicato, Mario; Al-mourabit, Ali; Han, Byung Woo; Diederich, Marc. |
| Treatment of acute myeloid leukemia (AML) patients is still hindered by resistance and relapse, resulting in an overall poor survival rate. Recently, combining specific B-cell lymphoma (Bcl)-2 inhibitors with compounds downregulating myeloid cell leukemia (Mcl)-1 has been proposed as a new effective strategy to eradicate resistant AML cells. We 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 Suberea clavata, synergizes with Bcl-2 inhibitor ABT-199 to efficiently kill Mcl-1/Bcl-2-positive AML cell lines, associated with Mcl-1 downregulation and endoplasmic reticulum stress induction. The absolute configuration of carbons 11 and 17 of the fistularin-3... |
| Tipo: Text |
Palavras-chave: Acute myeloid leukemia; ABT-199; Mcl-1; Bromotyrosine; (+)-11(R); 17(S)-fistularin-3; Configuration; Anticancer drug combination. |
| Ano: 2018 |
URL: https://archimer.ifremer.fr/doc/00476/58783/62419.pdf |
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| Moriou, Céline; Lacroix, Damien; Petek, Sylvain; El-demerdash, Amr; Trepos, Rozenn; Leu, Tinihauarii Mareva; Florean, Cristina; Diederich, Marc; Hellio, Claire; Debitus, Cecile; Al-mourabit, Ali. |
| Chemical investigation of the South-Pacific marine sponge Suberea clavata led to the isolation of eight new bromotyrosine metabolites named subereins 1–8 (2–9) along with twelve known co-isolated congeners. The detailed configuration determination of the first representative major compound of this family 11-epi-fistularin-3 (11R,17S) (1) is described. Their chemical characterization was achieved by HRMS and integrated 1D and 2D NMR (nuclear magnetic resonance) spectroscopic studies and extensive comparison with literature data. For the first time, a complete assignment of the absolute configurations for stereogenic centers C-11/17 of the known members (11R,17S) 11-epi-fistularin-3 (1) and 17-deoxyfistularin-3 (10) was determined by a combination of... |
| Tipo: Text |
Palavras-chave: Sponge; Verongiida; Suberea clavata; Bromotyrosine; Fistularin-3; Acetylcholinesterase inhibition; Antifouling. |
| Ano: 2021 |
URL: https://archimer.ifremer.fr/doc/00684/79581/82258.pdf |
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