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

被引：183

作者：

Cerezo, Michael ^{[1
,2
]}

Lehraiki, Abdelali ^{[1
,2
]}

Millet, Antoine ^{[3
]}

Rouaud, Florian ^{[1
,2
]}

Plaisant, Magali ^{[1
,2
]}

Jaune, Emilie ^{[1
,2
]}

Botton, Thomas ^{[1
,2
]}

Ronco, Cyril ^{[3
]}

Abbe, Patricia ^{[1
,2
]}

Amdouni, Hella ^{[3
]}

Passeron, Thierry ^{[1
,2
,4
]}

Hofman, Veronique ^{[2
,5
,6
,7
]}

Mograbi, Baharia ^{[2
,5
]}

Dabert-Gay, Anne-Sophie ^{[2
,8
]}

Debayle, Delphine ^{[2
,8
]}

Alcor, Damien ^{[1
,2
]}

Rabhi, Nabil ^{[9
]}

Annicotte, Jean-Sebastien ^{[9
]}

Heliot, Laurent ^{[10
]}

Gonzalez-Pisfil, Mariano ^{[10
]}

Robert, Caroline ^{[11
]}

Morera, Solange ^{[12
]}

Vigouroux, Armelle ^{[12
]}

Gual, Philippe ^{[13
]}

Ali, Maruf M. U. ^{[14
]}

Bertolotto, Corine ^{[1
,2
,4
]}

Hofman, Paul ^{[2
,5
,6
,7
]}

Ballotti, Robert ^{[1
,2
,4
]}

Benhida, Rachid ^{[3
]}

Rocchi, Stephane ^{[1
,2
,4
]}

机构：

[1] C3M, INSERM, U1065, Equipe Biol & Pathol Cellules Melanocytaire Pigme, Batiment ARCHIMED, F-06204 Nice 3, France

[2] Univ Nice Sophia Antipolis, UFR Med, F-06000 Nice, France

[3] Univ Nice Sophia Antipolis, UMR UNS CNRS 7272, Inst Chim Nice, Parc Valrose, F-06108 Nice 2, France

[4] CHU Nice, Hop Archet 2, Serv Dermatol, F-06204 Nice, France

[5] CNRS, UMR7284, INSERM, IRCAN,U1081, F-06107 Nice, France

[6] Hop Louis Pasteur, Lab Pathol Clin & Expt, F-06002 Nice, France

[7] Hop Louis Pasteur, Hosp Related Biobank BB 0033 00025, F-06002 Nice, France

[8] CNRS, UMR 7275, IPMC, F-06560 Valbonne, France

[9] Univ Lille, CNRS, Inst Pasteur Lille, UMR EGID 8199, F-59000 Lille, France

[10] Equipe Biophoton Cellulaire Fonct, Lab Phys Lasers Atomes & Mol PhLAM, GDR 2588, F-59658 Villeneuve Dascq, France

[11] Inst Gustave Roussy, Dept Dermatol, Canc Campus,114 Rue Edouard Vaillant, F-94805 Villejuif, France

[12] Univ Paris Saclay, Univ Paris Sud, CEA, CNRS,I2BC, F-91198 Gif Sur Yvette, France

[13] C3M, INSERM, U1065, Team 8, 151 Route St Antoine de Ginestiere, F-06204 Nice 3, France

[14] Univ London Imperial Coll Sci Technol & Med, Dept Life Sci, South Kensington Campus, London SW7 2AZ, England

来源：

CANCER CELL | 2016年 / 29卷 / 06期

关键词：

ENDOPLASMIC-RETICULUM STRESS; UNFOLDED PROTEIN RESPONSE; QUALITY-CONTROL; MELANOMA; CANCER; AUTOPHAGY; APOPTOSIS; CELLS; GRP78; MECHANISMS;

D O I：

10.1016/j.ccell.2016.04.013

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

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.

引用

页码：805 / 819

页数：15

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