Page 8 - 81_03
P. 8

BET inhibitors. The odd compound (+)-JQ1                    15. Shao Q, Kannan A, Lin Z, Stack BC, Suen JY, Gao L.
                                                                 BET protein inhibitor JQ1 attenuates Myc-amplified
     Knapp S. Targeting bromodomains: epigenetic readers         MCC tumor growth in vivo. Cancer Res 2014; 74:
     of lysine acetylation. Nature Rev Drug Discov 2014;         7090-7102.
     13: 337-56. (b) Gallenkamp D, Gelato K A, Haendler
     B, Weinmann H. Bromodomains and Their                  16. Baker EK, Taylos S, Gupte A, et al. BET inhibitors
     Pharmacological Inhibitors. ChemMedChem 2014; 9:            induce apoptosis through a MYC independent
     438-64. (c) Sánchez R, Meslamani J, Zhou MM. The            mechanism and synergise with CDK inhibitors to kill
     bromodomain: from epigenome reader to druggable             osteosarcoma cells. Scientific Reports 2015; 5: Article
     target. Biochim Biophys Acta 2014; 1839: 676-85.            number 10120.

3. Para una revisión de derivados de diazepina inhibidores  17. Wen S-M, Quan Ch-Y, Jiang N, Shang ZQ, Niu YJ.
     de bromodominios ver: Smith SG, Sánchez R, Zhou             What is the next generation therapeutic strategy for
     MM. Privileged diazepine compounds and their                castration-resistant prostate cáncer. Asian J Androl
     emergence as bromodomain inhibitors. Chem Biol              2015; 17: 223-24.
     2014; 21: 573-83.
                                                            18. a) Mirguet O, Gosmini R, Toum J, et al. Discovery of
4. Avendaño C, Menéndez JC. Peptidomimetics in cancer            epigenetic regulator I-BET762: lead optimization to
     chemotherapy. Clin Transl Oncol 2007; 9: 563-70.            afford a clinical candidate inhibitor of the BET
                                                                 bromodomains. J Med Chem 2013; 56: 7501-15. b)
5. Chung CW, Coste H, White JH, et al. Discovery and             Zhao Y, Yang Ch-Y, Wang S. The Making of
     characterization of small molecule inhibitors of the        I-BET762, a BET Bromodomain Inhibitor Now in
     BET family bromodomains. J Med Chem 2011; 54:               Clinical Development. J Med Chem 2013; 56: 7498-
     3827-38.                                                    7500.

6. Adachi K, Hikawa H, Hamada M, et al. inventors;          19. Boi M, Gaudio E, Bonetti P, et al. The BET
     Mitsubishi Tanabe Pharma Corporation, assignee.             Bromodomain Inhibitor OTX015 Affects
     Thienotriazolodiazepine compound and a medicinal            Pathogenetic Pathways in Preclinical B-cell Tumor
     use thereof. WO 2006129623 A1. 2006. Sept.                  Models and Synergizes with Targeted Drugs. Clin
                                                                 Cancer Res 2015; 21:1628-38.
7. Miyoshi S, Ooike S, Iwata K, Hikawa K, Sugahara K,
     inventors; Mitsubishi Tanabe Pharma Corporation,       20. Dawson MA, Prinjha RK, Dittmann A, et al. Inhibition
     assignee. Antitumor agent. International patent             of BET recruitment to chromatin as an effective
     PCT/JP2008/073864. 2009. Sept.                              treatment for MLL-fusion leukaemia. Nature 2011;
                                                                 478: 529-33.
8. Filippakopoulos P, Qi PJ, Picaud S, et al. Selective
     inhibition of BET bromodomains. Nature 2010; 468:      21. Hewings DS, Wang M, Philpott M, et al. 3,5-
     1067-73.                                                    Dimethylisoxazoles Act As Acetyl-lysine-mimetic
                                                                 Bromodomain Ligands. J Med Chem 2011; 54: 6761-
9. Maxmen A. Cancer research: Open ambition. Nature              70.
     News & Comment 2012; 488: 148-50.
                                                            22. Hewings DS, Fedorov O, Filippakopoulos P, et al.
10. Zuber J, Vakoc C. RNAi screen identifies BRD4 as a           Optimization of 3,5-dimethylisoxazole derivatives as
     therapeutic target in acute myeloid leukaemia. Nature       potent bromodomain ligands. J Med Chem 2013; 56:
     2011; 478: 524-28.                                          3217-27.

11. Delmore JE, Issa GC, Lemieux ME, et al. BET             23. a) Nicodeme E, Jeffrey KL, Schaefer U. Suppression
     bromodomain inhibition as a therapeutic strategy to         of inflammation by a synthetic histone mimic. Nature
     target c-Myc. Cell 2011; 146: 904-17.                       2010; 468: 1119-23. b) Toniolo PA, Liu S, Yeh JE, et
                                                                 al. Inhibiting STAT5 by the BET bromodomain
12. Los inhibidores del proteasoma aumentan los niveles          inhibitor JQ1 disrupts human dendritic cell
     de proteínas reguladoras, lo que conduce a la muerte        maturation. J Immunol 2015; 194: 3180-90.
     celular por distintos mecanismos.
                                                            24. Para una revisión reciente ver: Kogan P, Wald M. Urol
13. Floyd SR, Pacold ME, Huang Q, et al. The                     Clin N Am 2014; 41: 145-61.
     bromodomain protein BRD4 insulates chromatin from
     DNA damage signalling. Nature 2013; 498: 246-50.       25. Matzuk MM, McKeown MR, Filippakopoulos P, et al.
                                                                 Small-Molecule Inhibition of BRDT for Male
14. a) Raza SS, Knab M, Chow Ch, et al. Development of           Contraception. Cell 2012; 150: 673-84.
     resistance to BET bromodomain inhibitor JQ1 and
     demonstration of epithelial-mesenchymal transition in  26. Palermo RD, Webb HM, West MJ. RNA Polymerase
     pancreatic cancer cells. J Clin Oncol 2014; 32 suppl,       II Stalling Promotes Nucleosome Occlusion and
     e15263. b) Kumar K, Raza SS, Knab LM, et al. GLI2-          pTEFb Recruitment to Drive Immortalization by
     dependent c-MYC upregulation mediates resistance of         Epstein-Barr Virus. PLoS Pathog 2011, 7: e1002334.
     pancreatic cancer cells to the BET bromodomain
     inhibitor JQ1. Scientific Reports 2015; 5: Article     27. Banerjee C, Archin N, Michaels D, et al. BET
     number 9489. c) García PL, Miller AL, Kreitzburg            bromodomain inhibition as a novel strategy for
     KM, et al. The BET bromodomain inhibitor JQ1                reactivation of HIV-1. Journal of Leukocyte Biology
     suppresses growth of pancreatic ductal                      2012; 92: 1147-54.
     adenocarcinoma in patient-derived xenograft models.
     Oncogene 2015; doi:10.1038/onc.2015.126.                                                                                 219

     @Real Academia Nacional de Farmacia. Spain
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