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

Michaël Cerezo; Abdelali Lehraiki; Antoine Millet; Florian Rouaud; Magali Plaisant; Emilie Jaune; Thomas Botton; Cyril Ronco; Patricia Abbe; Hella Amdouni; Thierry Passeron; Veronique Hofman; Baharia Mograbi; Anne Sophie Dabert-Gay; Delphine Debayle; Damien Alcor; Nabil Rabhi; Jean Sébastien Annicotte; Laurent Héliot; Mariano Gonzalez-Pisfil; Caroline Robert; Solange Moréra; Armelle Virougoux; Philippe Gual; Maruf M.U. Ali; Corine Bertolotto; Paul Hofman; Robert Ballotti; Rachid Benhida; Stéphane Rocchi

doi:10.1016/j.ccell.2016.04.013

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

Michaël Cerezo, Abdelali Lehraiki, Antoine Millet, Florian Rouaud, Magali Plaisant, Emilie Jaune, Thomas Botton, Cyril Ronco, Patricia Abbe, Hella Amdouni, Thierry Passeron, Veronique Hofman, Baharia Mograbi, Anne Sophie Dabert-Gay, Delphine Debayle, Damien Alcor, Nabil Rabhi, Jean Sébastien Annicotte, Laurent Héliot, Mariano Gonzalez-PisfilCaroline Robert, Solange Moréra, Armelle Virougoux, Philippe Gual, Maruf M.U. Ali, Corine Bertolotto, Paul Hofman, Robert Ballotti, Rachid Benhida, Stéphane Rocchi

Résultats de recherche: Contribution à un journal › Article › Revue par des pairs

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Résumé

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.

langue originale	Anglais
Pages (de - à)	805-819
Nombre de pages	15
journal	Cancer Cell
Volume	29
Numéro de publication	6
Les DOIs	https://doi.org/10.1016/j.ccell.2016.04.013
état	Publié - 13 juin 2016

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10.1016/j.ccell.2016.04.013

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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, A. S., Debayle, D., Alcor, D., Rabhi, N., Annicotte, J. S., Héliot, L., ... Rocchi, S. (2016). Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance. Cancer Cell, 29(6), 805-819. https://doi.org/10.1016/j.ccell.2016.04.013

@article{5b6cde2c54134099beb7c84984625438,

title = "Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance",

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.",

author = "Micha{\"e}l Cerezo and Abdelali Lehraiki and Antoine Millet and Florian Rouaud and Magali Plaisant and Emilie Jaune and Thomas Botton and Cyril Ronco and Patricia Abbe and Hella Amdouni and Thierry Passeron and Veronique Hofman and Baharia Mograbi and Dabert-Gay, {Anne Sophie} and Delphine Debayle and Damien Alcor and Nabil Rabhi and Annicotte, {Jean S{\'e}bastien} and Laurent H{\'e}liot and Mariano Gonzalez-Pisfil and Caroline Robert and Solange Mor{\'e}ra and Armelle Virougoux and Philippe Gual and Ali, {Maruf M.U.} and Corine Bertolotto and Paul Hofman and Robert Ballotti and Rachid Benhida and St{\'e}phane Rocchi",

note = "Publisher Copyright: {\textcopyright} 2016 Elsevier Inc.",

year = "2016",

month = jun,

day = "13",

doi = "10.1016/j.ccell.2016.04.013",

language = "English",

volume = "29",

pages = "805--819",

journal = "Cancer Cell",

issn = "1535-6108",

number = "6",

}

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, Virougoux, A, Gual, P, Ali, MMU, Bertolotto, C, Hofman, P, Ballotti, R, Benhida, R & Rocchi, S 2016, 'Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance', Cancer Cell, VOL. 29, Numéro 6, p. 805-819. https://doi.org/10.1016/j.ccell.2016.04.013

TY - JOUR

T1 - Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance

AU - Cerezo, Michaël

AU - Lehraiki, Abdelali

AU - Millet, Antoine

AU - Rouaud, Florian

AU - Plaisant, Magali

AU - Jaune, Emilie

AU - Botton, Thomas

AU - Ronco, Cyril

AU - Abbe, Patricia

AU - Amdouni, Hella

AU - Passeron, Thierry

AU - Hofman, Veronique

AU - Mograbi, Baharia

AU - Dabert-Gay, Anne Sophie

AU - Debayle, Delphine

AU - Alcor, Damien

AU - Rabhi, Nabil

AU - Annicotte, Jean Sébastien

AU - Héliot, Laurent

AU - Gonzalez-Pisfil, Mariano

AU - Robert, Caroline

AU - Moréra, Solange

AU - Virougoux, Armelle

AU - Gual, Philippe

AU - Ali, Maruf M.U.

AU - Bertolotto, Corine

AU - Hofman, Paul

AU - Ballotti, Robert

AU - Benhida, Rachid

AU - Rocchi, Stéphane

PY - 2016/6/13

Y1 - 2016/6/13

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=84969753139&partnerID=8YFLogxK

U2 - 10.1016/j.ccell.2016.04.013

DO - 10.1016/j.ccell.2016.04.013

M3 - Article

C2 - 27238082

AN - SCOPUS:84969753139

SN - 1535-6108

VL - 29

SP - 805

EP - 819

JO - Cancer Cell

JF - Cancer Cell

IS - 6

ER -