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. 2016 Jun 13;29(6):805-819.
doi: 10.1016/j.ccell.2016.04.013. Epub 2016 May 26.

Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance

Michaël Cerezo  1 , Abdelali Lehraiki  1 , Antoine Millet  2 , Florian Rouaud  1 , Magali Plaisant  1 , Emilie Jaune  1 , Thomas Botton  1 , Cyril Ronco  2 , Patricia Abbe  1 , Hella Amdouni  2 , Thierry Passeron  3 , Veronique Hofman  4 , Baharia Mograbi  5 , Anne-Sophie Dabert-Gay  6 , Delphine Debayle  6 , Damien Alcor  1 , Nabil Rabhi  7 , Jean-Sébastien Annicotte  7 , Laurent Héliot  8 , Mariano Gonzalez-Pisfil  8 , Caroline Robert  9 , Solange Moréra  10 , Armelle Vigouroux  10 , Philippe Gual  11 , Maruf M U Ali  12 , Corine Bertolotto  3 , Paul Hofman  4 , Robert Ballotti  3 , Rachid Benhida  13 , Stéphane Rocchi  14
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Free article

Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance

Michaël Cerezo et al. Cancer Cell. .
Free article

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  • Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance.
    Cerezo M, Lehraiki A, Millet A, Rouaud F, Plaisant M, Jaune E, Botton T, Ronco C, Abbe P, Amdouni H, Passeron T, Hofman V, Mograbi B, Dabert-Gay AS, Debayle D, Alcor D, Rabhi N, Annicotte JS, Héliot L, Gonzalez-Pisfil M, Robert C, Moréra S, Vigouroux A, Gual P, Ali MMU, Bertolotto C, Hofman P, Ballotti R, Benhida R, Rocchi S. Cerezo M, et al. Cancer Cell. 2016 Jul 11;30(1):183. doi: 10.1016/j.ccell.2016.06.007. Epub 2016 Jul 11. Cancer Cell. 2016. PMID: 27479035 No abstract available.

Abstract

We have discovered and developed a series of molecules (thiazole benzenesulfonamides). HA15, the lead compound of this series, displayed anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors. Our molecule displayed activity against other liquid and solid tumors. HA15 also exhibited strong efficacy in xenograft mouse models with melanoma cells either sensitive or resistant to BRAF inhibitors. Transcriptomic, proteomic, and biochemical studies identified the chaperone BiP/GRP78/HSPA5 as the specific target of HA15 and demonstrated that the interaction increases ER stress, leading to melanoma cell death by concomitant induction of autophagic and apoptotic mechanisms.

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