Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Tóm tắt
Từ khóa
Tài liệu tham khảo
Asangani, 2014, Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer, Nature, 510, 278, 10.1038/nature13229
Baratta, 2015, An in-tumor genetic screen reveals that the BET bromodomain protein, BRD4, is a potential therapeutic target in ovarian carcinoma, Proc. Natl. Acad. Sci. USA, 112, 232, 10.1073/pnas.1422165112
Belkina, 2012, BET domain co-regulators in obesity, inflammation and cancer, Nat. Rev. Cancer, 12, 465, 10.1038/nrc3256
Boi, 2015, The BET bromodomain inhibitor OTX015 affects pathogenetic pathways in pre-clinical B-cell tumor models and synergizes with targeted drugs, Clin. Cancer Res., 21, 1628, 10.1158/1078-0432.CCR-14-1561
Bolden, 2014, Inducible in vivo silencing of Brd4 identifies potential toxicities of sustained BET protein inhibition, Cell Rep., 8, 1919, 10.1016/j.celrep.2014.08.025
Buckley, 2014, Small-molecule control of intracellular protein levels through modulation of the ubiquitin proteasome system, Angew. Chem. Int. Ed. Engl., 53, 2312, 10.1002/anie.201307761
Burnett, 2011, Current progress of siRNA/shRNA therapeutics in clinical trials, Biotechnol. J., 6, 1130, 10.1002/biot.201100054
Ceribelli, 2014, Blockade of oncogenic IkappaB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors, Proc. Natl. Acad. Sci. USA, 111, 11365, 10.1073/pnas.1411701111
Chapuy, 2013, Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma, Cancer Cell, 24, 777, 10.1016/j.ccr.2013.11.003
Delmore, 2011, BET bromodomain inhibition as a therapeutic strategy to target c-Myc, Cell, 146, 904, 10.1016/j.cell.2011.08.017
Fernandez, 2014, Transformation resistance in a premature aging disorder identifies a tumor-protective function of BRD4, Cell Rep., 9, 248, 10.1016/j.celrep.2014.08.069
Filippakopoulos, 2010, Selective inhibition of BET bromodomains, Nature, 468, 1067, 10.1038/nature09504
Fischer, 2014, Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide, Nature, 512, 49, 10.1038/nature13527
French, 2008, BRD-NUT oncoproteins: a family of closely related nuclear proteins that block epithelial differentiation and maintain the growth of carcinoma cells, Oncogene, 27, 2237, 10.1038/sj.onc.1210852
Gabay, 2014, MYC activation is a hallmark of cancer initiation and maintenance, Cold Spring Harbor Perspect. Med., 4, 10.1101/cshperspect.a014241
Ge, 2007, Process for the preparation of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione compounds, US Pat. Appl.
Hoelder, 2012, Discovery of small molecule cancer drugs: successes, challenges and opportunities, Mol. Oncol., 6, 155, 10.1016/j.molonc.2012.02.004
Howell, 2004, The use of selective estrogen receptor modulators and selective estrogen receptor down-regulators in breast cancer, Best Pract. Res. Clin. Endocrinol. Metab., 18, 47, 10.1016/j.beem.2003.08.002
Ito, 2010, Identification of a primary target of thalidomide teratogenicity, Science, 327, 1345, 10.1126/science.1177319
Johnson, 2010, Strategies for discovering and derisking covalent, irreversible enzyme inhibitors, Future Med. Chem., 2, 949, 10.4155/fmc.10.21
Klapproth, 2010, Advances in the understanding of MYC-induced lymphomagenesis, Br. J. Haematol., 149, 484, 10.1111/j.1365-2141.2010.08159.x
Loosveld, 2014, Therapeutic targeting of c-Myc in T-cell acute lymphoblastic leukemia, T-ALL, Oncotarget, 5, 3168, 10.18632/oncotarget.1873
Lopez-Girona, 2012, Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide, Leukemia, 26, 2326, 10.1038/leu.2012.119
Loven, 2013, Selective inhibition of tumor oncogenes by disruption of super-enhancers, Cell, 153, 320, 10.1016/j.cell.2013.03.036
Lu, 2014, The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins, Science, 343, 305, 10.1126/science.1244917
Mertz, 2011, Targeting MYC dependence in cancer by inhibiting BET bromodomains, Proc. Natl. Acad. Sci. USA, 108, 16669, 10.1073/pnas.1108190108
Noel, 2014, Development of the BET bromodomain inhibitor OTX015, Mol. Cancer Ther., 12, C244, 10.1158/1535-7163.TARG-13-C244
Puissant, 2013, Targeting MYCN in neuroblastoma by BET bromodomain inhibition, Cancer Discov., 3, 308, 10.1158/2159-8290.CD-12-0418
Raina, 2010, Chemical inducers of targeted protein degradation, J. Biol. Chem., 285, 11057, 10.1074/jbc.R109.078105
Sakamoto, 2001, Protacs: chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation, Proc. Natl. Acad. Sci. USA, 98, 8554, 10.1073/pnas.141230798
Sakamoto, 2003, Development of Protacs to target cancer-promoting proteins for ubiquitination and degradation, Mol. Cell Proteomics, 2, 1350, 10.1074/mcp.T300009-MCP200
Schneekloth, 2005, Chemical approaches to controlling intracellular protein degradation, Chembiochem, 6, 40, 10.1002/cbic.200400274
Schneekloth, 2004, Chemical genetic control of protein levels: selective in vivo targeted degradation, J. Am. Chem. Soc., 126, 3748, 10.1021/ja039025z
Shao, 2014, BET protein inhibitor JQ1 attenuates Myc-amplified MCC tumor growth in vivo, Cancer Res., 74, 7090, 10.1158/0008-5472.CAN-14-0305
Shi, 2014, The mechanisms behind the therapeutic activity of BET bromodomain inhibition, Mol. Cell, 54, 728, 10.1016/j.molcel.2014.05.016
Shimamura, 2013, Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer, Clin. Cancer Res., 19, 6183, 10.1158/1078-0432.CCR-12-3904
Sueoka, 1998, Preparation and formulation of thienotriazolodiazepine derivatives for the treatment of inflammatory intestinal diseases, venous insufficiency, and venous ulcer, PCT Int. Appl.
Wyce, 2013, Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer, Oncotarget, 4, 2419, 10.18632/oncotarget.1572