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Items: 30


BET bromodomain inhibitor birabresib in mantle cell lymphoma: in vivo activity and identification of novel combinations to overcome adaptive resistance.

Tarantelli C, Bernasconi E, Gaudio E, Cascione L, Restelli V, Arribas AJ, Spriano F, Rinaldi A, Mensah AA, Kwee I, Ponzoni M M.D, Zucca E, Carrassa L, Riveiro ME, Rezai K, Stathis A, Cvitkovic E, Bertoni F.

ESMO Open. 2018 Sep 26;3(6):e000387. doi: 10.1136/esmoopen-2018-000387. eCollection 2018.


Bromodomain and extra-terminal domain inhibition modulates the expression of pathologically relevant microRNAs in diffuse large B-cell lymphoma.

Mensah AA, Cascione L, Gaudio E, Tarantelli C, Bomben R, Bernasconi E, Zito D, Lampis A, Hahne JC, Rinaldi A, Stathis A, Zucca E, Kwee I, Gattei V, Valeri N, Riveiro ME, Bertoni F.

Haematologica. 2018 Aug 3. pii: haematol.2018.191684. doi: 10.3324/haematol.2018.191684. [Epub ahead of print]


The bromodomain inhibitor OTX015 (MK-8628) exerts anti-tumor activity in triple-negative breast cancer models as single agent and in combination with everolimus.

Vázquez R, Riveiro ME, Astorgues-Xerri L, Odore E, Rezai K, Erba E, Panini N, Rinaldi A, Kwee I, Beltrame L, Bekradda M, Cvitkovic E, Bertoni F, Frapolli R, D'Incalci M.

Oncotarget. 2017 Jan 31;8(5):7598-7613. doi: 10.18632/oncotarget.13814.


OTX015 (MK-8628), a novel BET inhibitor, exhibits antitumor activity in non-small cell and small cell lung cancer models harboring different oncogenic mutations.

Riveiro ME, Astorgues-Xerri L, Vazquez R, Frapolli R, Kwee I, Rinaldi A, Odore E, Rezai K, Bekradda M, Inghirami G, D'Incalci M, Noel K, Cvitkovic E, Raymond E, Bertoni F.

Oncotarget. 2016 Dec 20;7(51):84675-84687. doi: 10.18632/oncotarget.13181.


Therapeutic efficacy of the bromodomain inhibitor OTX015/MK-8628 in ALK-positive anaplastic large cell lymphoma: an alternative modality to overcome resistant phenotypes.

Boi M, Todaro M, Vurchio V, Yang SN, Moon J, Kwee I, Rinaldi A, Pan H, Crescenzo R, Cheng M, Cerchietti L, Elemento O, Riveiro ME, Cvitkovic E, Bertoni F, Inghirami G; AIRC 5xMille Consortium ‘Genetics-Driven Targeted Management of Lymphoid Malignancies’.

Oncotarget. 2016 Nov 29;7(48):79637-79653. doi: 10.18632/oncotarget.12876.


Promising in vivo efficacy of the BET bromodomain inhibitor OTX015/MK-8628 in malignant pleural mesothelioma xenografts.

Vázquez R, Licandro SA, Astorgues-Xerri L, Lettera E, Panini N, Romano M, Erba E, Ubezio P, Bello E, Libener R, Orecchia S, Grosso F, Riveiro ME, Cvitkovic E, Bekradda M, D'Incalci M, Frapolli R.

Int J Cancer. 2017 Jan 1;140(1):197-207. doi: 10.1002/ijc.30412. Epub 2016 Sep 19.


Everolimus affects vasculogenic mimicry in renal carcinoma resistant to sunitinib.

Serova M, Tijeras-Raballand A, Dos Santos C, Martinet M, Neuzillet C, Lopez A, Mitchell DC, Bryan BA, Gapihan G, Janin A, Bousquet G, Riveiro ME, Bieche I, Faivre S, Raymond E, de Gramont A.

Oncotarget. 2016 Jun 21;7(25):38467-86. doi: 10.18632/oncotarget.9542.


OTX015 (MK-8628), a novel BET inhibitor, displays in vitro and in vivo antitumor effects alone and in combination with conventional therapies in glioblastoma models.

Berenguer-Daizé C, Astorgues-Xerri L, Odore E, Cayol M, Cvitkovic E, Noel K, Bekradda M, MacKenzie S, Rezai K, Lokiec F, Riveiro ME, Ouafik L.

Int J Cancer. 2016 Nov 1;139(9):2047-55. doi: 10.1002/ijc.30256. Epub 2016 Jul 30.


Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition.

Henssen A, Althoff K, Odersky A, Beckers A, Koche R, Speleman F, Schäfers S, Bell E, Nortmeyer M, Westermann F, De Preter K, Florin A, Heukamp L, Spruessel A, Astrahanseff K, Lindner S, Sadowski N, Schramm A, Astorgues-Xerri L, Riveiro ME, Eggert A, Cvitkovic E, Schulte JH.

Clin Cancer Res. 2016 May 15;22(10):2470-81. doi: 10.1158/1078-0432.CCR-15-1449. Epub 2015 Dec 2.


Phase I Population Pharmacokinetic Assessment of the Oral Bromodomain Inhibitor OTX015 in Patients with Haematologic Malignancies.

Odore E, Lokiec F, Cvitkovic E, Bekradda M, Herait P, Bourdel F, Kahatt C, Raffoux E, Stathis A, Thieblemont C, Quesnel B, Cunningham D, Riveiro ME, Rezaï K.

Clin Pharmacokinet. 2016 Mar;55(3):397-405. doi: 10.1007/s40262-015-0327-6.


BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells.

Coudé MM, Braun T, Berrou J, Dupont M, Bertrand S, Masse A, Raffoux E, Itzykson R, Delord M, Riveiro ME, Herait P, Baruchel A, Dombret H, Gardin C.

Oncotarget. 2015 Jul 10;6(19):17698-712.


The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs.

Boi M, Gaudio E, Bonetti P, Kwee I, Bernasconi E, Tarantelli C, Rinaldi A, Testoni M, Cascione L, Ponzoni M, Mensah AA, Stathis A, Stussi G, Riveiro ME, Herait P, Inghirami G, Cvitkovic E, Zucca E, Bertoni F.

Clin Cancer Res. 2015 Apr 1;21(7):1628-38. doi: 10.1158/1078-0432.CCR-14-1561. Epub 2015 Jan 26.


Fsn0503h antibody-mediated blockade of cathepsin S as a potential therapeutic strategy for the treatment of solid tumors.

Vázquez R, Astorgues-Xerri L, Bekradda M, Gormley J, Buick R, Kerr P, Cvitkovic E, Raymond E, D'Incalci M, Frapolli R, Riveiro ME.

Biochimie. 2015 Jan;108:101-7. doi: 10.1016/j.biochi.2014.10.025. Epub 2014 Nov 5.


Insights on the CXCL12-CXCR4 axis in hepatocellular carcinoma carcinogenesis.

Ghanem I, Riveiro ME, Paradis V, Faivre S, de Parga PM, Raymond E.

Am J Transl Res. 2014 Jul 18;6(4):340-52. eCollection 2014. Review.


OTX008, a selective small-molecule inhibitor of galectin-1, downregulates cancer cell proliferation, invasion and tumour angiogenesis.

Astorgues-Xerri L, Riveiro ME, Tijeras-Raballand A, Serova M, Rabinovich GA, Bieche I, Vidaud M, de Gramont A, Martinet M, Cvitkovic E, Faivre S, Raymond E.

Eur J Cancer. 2014 Sep;50(14):2463-77. doi: 10.1016/j.ejca.2014.06.015. Epub 2014 Jul 16.


Unraveling galectin-1 as a novel therapeutic target for cancer.

Astorgues-Xerri L, Riveiro ME, Tijeras-Raballand A, Serova M, Neuzillet C, Albert S, Raymond E, Faivre S.

Cancer Treat Rev. 2014 Mar;40(2):307-19. doi: 10.1016/j.ctrv.2013.07.007. Epub 2013 Aug 1. Review.


Pharmacodynamic study of the 7,8-dihydroxy-4-methylcoumarin-induced selective cytotoxicity toward U-937 leukemic cells versus mature monocytes: cytoplasmic p21(Cip1/WAF1) as resistance factor.

Vázquez R, Riveiro ME, Mondillo C, Perazzo JC, Vermeulen M, Baldi A, Davio C, Shayo C.

Biochem Pharmacol. 2013 Jul 15;86(2):210-21. doi: 10.1016/j.bcp.2013.04.021. Epub 2013 May 9.


Predictive factors of sensitivity to elisidepsin, a novel Kahalalide F-derived marine compound.

Serova M, de Gramont A, Bieche I, Riveiro ME, Galmarini CM, Aracil M, Jimeno J, Faivre S, Raymond E.

Mar Drugs. 2013 Mar 20;11(3):944-59. doi: 10.3390/md11030944.


Benchmarking effects of mTOR, PI3K, and dual PI3K/mTOR inhibitors in hepatocellular and renal cell carcinoma models developing resistance to sunitinib and sorafenib.

Serova M, de Gramont A, Tijeras-Raballand A, Dos Santos C, Riveiro ME, Slimane K, Faivre S, Raymond E.

Cancer Chemother Pharmacol. 2013 May;71(5):1297-307. doi: 10.1007/s00280-013-2129-6. Epub 2013 Mar 12.


Focus on the role of the CXCL12/CXCR4 chemokine axis in head and neck squamous cell carcinoma.

Albert S, Riveiro ME, Halimi C, Hourseau M, Couvelard A, Serova M, Barry B, Raymond E, Faivre S.

Head Neck. 2013 Dec;35(12):1819-28. doi: 10.1002/hed.23217. Epub 2013 Mar 6. Review.


Structure-anti-leukemic activity relationship study of ortho-dihydroxycoumarins in U-937 cells: key role of the δ-lactone ring in determining differentiation-inducing potency and selective pro-apoptotic action.

Vázquez R, Riveiro ME, Vermeulen M, Alonso E, Mondillo C, Facorro G, Piehl L, Gómez N, Moglioni A, Fernández N, Baldi A, Shayo C, Davio C.

Bioorg Med Chem. 2012 Sep 15;20(18):5537-49. doi: 10.1016/j.bmc.2012.07.043. Epub 2012 Aug 2.


Prognostic value of the chemokine receptor CXCR4 and epithelial-to-mesenchymal transition in patients with squamous cell carcinoma of the mobile tongue.

Albert S, Hourseau M, Halimi C, Serova M, Descatoire V, Barry B, Couvelard A, Riveiro ME, Tijeras-Raballand A, de Gramont A, Raymond E, Faivre S.

Oral Oncol. 2012 Dec;48(12):1263-71. doi: 10.1016/j.oraloncology.2012.06.010. Epub 2012 Jul 7.


Toddaculin, a natural coumarin from Toddalia asiatica, induces differentiation and apoptosis in U-937 leukemic cells.

Vázquez R, Riveiro ME, Vermeulen M, Mondillo C, Coombes PH, Crouch NR, Ismail F, Mulholland DA, Baldi A, Shayo C, Davio C.

Phytomedicine. 2012 Jun 15;19(8-9):737-46. doi: 10.1016/j.phymed.2012.03.008. Epub 2012 Apr 25.


Coumarins: old compounds with novel promising therapeutic perspectives.

Riveiro ME, De Kimpe N, Moglioni A, Vázquez R, Monczor F, Shayo C, Davio C.

Curr Med Chem. 2010;17(13):1325-38. Review.


Toward establishing structure-activity relationships for oxygenated coumarins as differentiation inducers of promonocytic leukemic cells.

Riveiro ME, Maes D, Vázquez R, Vermeulen M, Mangelinckx S, Jacobs J, Debenedetti S, Shayo C, De Kimpe N, Davio C.

Bioorg Med Chem. 2009 Sep 15;17(18):6547-59. doi: 10.1016/j.bmc.2009.08.002. Epub 2009 Aug 8.


Structural insights into hydroxycoumarin-induced apoptosis in U-937 cells.

Riveiro ME, Moglioni A, Vazquez R, Gomez N, Facorro G, Piehl L, de Celis ER, Shayo C, Davio C.

Bioorg Med Chem. 2008 Mar 1;16(5):2665-75. Epub 2007 Nov 19.


Biochemical mechanisms underlying the pro-apoptotic activity of 7,8-dihydroxy-4-methylcoumarin in human leukemic cells.

Riveiro ME, Vazquez R, Moglioni A, Gomez N, Baldi A, Davio C, Shayo C.

Biochem Pharmacol. 2008 Feb 1;75(3):725-36. Epub 2007 Oct 5.


Induction of cell differentiation in human leukemia U-937 cells by 5-oxygenated-6,7-methylenedioxycoumarins from Pterocaulon polystachyum.

Riveiro ME, Shayo C, Monczor F, Fernández N, Baldi A, De Kimpe N, Rossi J, Debenedetti S, Davio C.

Cancer Lett. 2004 Jul 16;210(2):179-88.


The time-course of cyclic AMP signaling is critical for leukemia U-937 cell differentiation.

Shayo C, Legnazzi BL, Monczor F, Fernández N, Riveiro ME, Baldi A, Davio C.

Biochem Biophys Res Commun. 2004 Feb 13;314(3):798-804.


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