EC-8042 · publications

Updated list of our EC-8042 publications…

26 Mithramycin delivery systems to develop effective therapies in sarcomas

Estupiñán Ó, Niza E, Bravo I, Rey V, Tornín J, Gallego B, Clemente-Casares P, Moris F, Ocaña A, Blanco-Lorenzo V, Rodríguez-Santamaría M, Vallina-Álvarez A, González MV, Rodríguez A, Hermida-Merino D, Alonso-Moreno C, Rodríguez R.
J Nanobiotechnology. 2021,19(1), 267. doi: 10.1186/s12951-021-01008-x. PMID: 34488783

25 Nano-Encapsulation of Mithramycin in Transfersomes and Polymeric Micelles for the Treatment of Sarcomas

Estupiñán Ó, Rendueles C, Suárez P, Rey V, Murillo D, Morís F, Gutiérrez G, Blanco-López MDC, Matos M, Rodríguez R.
J Clin Med. 2021 Mar 25;10(7):1358. doi: 10.3390/jcm10071358. PMID: 33806182

24 Mithramycin induces promoter reprogramming and differentiation of rhabdoid tumor

Chasse MH, Johnson BK, Boguslawski EA, Sorensen KM, Rosien JE, Kang MH, Reynolds CP, Heo L, Madaj ZB, Beddows I, Foxa GE, Kitchen-Goosen SM, Williams BO, Triche TJ Jr, Grohar PJ.
EMBO Mol Med. 2021 Feb 5;13(2):e12640. doi: 10.15252/emmm.202012640. PMID: 33332735

23 Mithramycin A and mithralog EC-8042 inhibit SETDB1 expression and its oncogenic activity in malignant melanoma

Federico A, Steinfass T, Larribère L, Novak D, Morís F, Núñez LE, Umansky V, Utikal J.
Mol Ther – Oncolytics 2020 Jun 4;18:83-99 doi: 10.1016/j.omto.2020.06.001. PMID: 32637583

22 CDK9 Blockade Exploits Context-dependent Transcriptional Changes to Improve Activity and Limit Toxicity of Mithramycin for Ewing Sarcoma

Flores G, Everett JH, Boguslawski EA, Oswald BM, Madaj ZB, Beddows I, Dikalov S, Adams M, Klumpp-Thomas CA, Kitchen-Goosen SM, Martin SE, Caplen NJ, Helman LJ, Grohar PJ.
Mol Cancer Ther. 2020 May;19(5):1183-1196. doi: 10.1158/1535-7163.MCT-19-0775. PMID:32127464

21 SOX2 Expression and Transcriptional Activity Identifies a Subpopulation of Cancer Stem Cells in Sarcoma with Prognostic Implications

Menéndez ST, Rey V, Martínez-Cruzado L, González MV, Morales-Molina A, Santos L, Blanco V, Alvarez C, Estupiñán O, Allonca E, Rodrigo JP, García-Castro J, García-Pedrero JM, Rodríguez R.
Cancers (Basel). 2020 Apr 13;12(4). pii: E964. doi: 10.3390/cancers12040964. PMID: 32295077

20 The mithralog EC-7072 induces chronic lymphocytic leukemia cell death by targeting tonic B-cell receptor signaling pathway

Lorenzo-Herrero S, Sordo-Bahamonde C, Bretones G, Payer AR, González-Rodríguez AP, González-García E, Pérez-Escuredo J, Villa-Álvarez M, Núñez LE, Morís F, Gonzalez S, López-Soto A
Frontiers in immunology, 2019, 10, 2455. doi: 10.3389/fimmu.2019.02455. PMID: 31681329

19 The SRC Inhibitor Dasatinib Induces Stem Cell-Like Properties in Head and Neck Cancer Cells that are Effectively Counteracted by the Mithralog EC-8042

Hermida-Prado F, Villaronga MA, Granda-Díaz R, Del-Río-Ibisate N, Santos L, Hermosilla MA, Oro P, Allonca E, Agorreta J, Garmendia I, Tornín J, Perez-Escuredo J, Fuente R, Montuenga LM, Morís F, Rodrigo JP, Rodríguez R, García-Pedrero JM.
J Clin Med. 2019 Aug 2;8(8). pii: E1157. doi: 10.3390/jcm8081157. PMID: 31382448

18 Transcriptional Reprogramming and Inhibition of Tumor-propagating Stem-like Cells by EC-8042 in ERG-positive Prostate Cancer

Shinde D, Albino D, Zoma M, Mutti A, Mapelli SN, Civenni G, Kokanovic A, Merulla J, Perez-Escuredo J, Costales P, Morís F, Catapano CV, Carbone GM
European Urology Oncology 2019, 2(4), 415-424. doi: 10.1016/j.euo.2018.08.024. PMID: 31277777

17 Factors Secreted by Cancer-Associated Fibroblasts that Sustain Cancer Stem Properties in Head and Neck Squamous Carcinoma Cells as Potential Therapeutic Targets

Álvarez-Teijeiro S, García-Inclán C, Villaronga MA, Casado P, Hermida-Prado F, Granda-Díaz R, Rodrigo JP, Calvo F, Del-Río-Ibisate N, Gandarillas A, Morís F, Hermsen M, Cutillas P, García-Pedrero JM.
Cancers (Basel). 2018 Sep 17;10(9). pii: E334. doi: 10.3390/cancers10090334

16 Inhibition of SP1 by the Mithramycin Analog EC-8042 Efficiently Targets Tumor Initiating Cells in Sarcoma

Tornin J, Martínez-Cruzado L, Santos L, Rodríguez A, Núñez L-E, Oro P, Hermosilla MA, Allonca E, Fernández-García MT, Astudillo A, Suárez C, Morís F, Rodríguez R.
Oncotarget 2016, May 24;7(21):30935-50. doi: 10.18632/oncotarget.8817 PMID: 27105533

15 ALDH1 expression and activity increase during tumor evolution in sarcoma cancer stem cell populations

Martínez-Cruzado L, Tornin J, Santos L, Rodríguez A, García-Castro J, Morís F, Rodríguez R.
Sci. Rep. 2016, Jun 13;6:27878. doi: 10.1038/srep27878 PMID: 27292183

14 Identification of mithramycin analogs with improved targeting of the EWS-FLI1 transcription factor

Osgood CL, Maloney N, Kidd CG, Kitchen-Goosen S, Segars E, Gebregiorgis M, Woldemichael GM, He M, Sankar S, Lessnick SL, Kang MH, Smith MA, Turner L, Madaj ZB, Winn ME, Núñez LE, González-Sabín J, Helman LJ, Morís F, Grohar PJ.
Clinical Cancer Res. 2016, 22(16):4105-18. doi: 10.1158/1078-0432 PMID: 26979396

13 Pleiotropic anti-angiogenic and anti-oncogenic activities of the novel mithralog demycarosyl-3D-ß-D-digitoxosyl-mithramycin SK (EC-8042)

Fernández-Guizán A, Acebes-Huerta A, Huergo-Zapico L, López-Soto A, Núñez L-E, Morís F, González S.
PLoS ONE, 2015, Nov 4;10(11):e0140786. doi:10.1371/journal.pone.0140786. PMID: 26536461

12 Expanding the Chemical Diversity of the Antitumoral Compound Mithramycin by Combinatorial Biosynthesis and Biocatalysis: The Quest for Mithralogs with Improved Therapeutic Window

Méndez C, González-Sabín J, Morís F, Salas JA.
Planta Med. 2015 81(15), 1326-1338. doi: 10.1055/s-0035-1557876. PMID: 26393942

11 Antitumoral activity of the mithralog EC-8042 in triple negative breast cancer linked to cell cycle arrest in G2

Pandiella A, Morís F, Ocaña A, Núñez LE, Montero JC.
Oncotarget 2015, 6(32), 32856-67. doi: 10.18632/oncotarget.5942. PMID: 26439989

10 Cytotoxic effects of mithramycin DIG-MSK can depend on the rise of autophagy

Vizcaíno C, Rodríguez-Sánchez MA, Núñez LE, Morís F, Portugal J.
Toxicol. in vitro. 2015 Oct;29(7):1537-44. doi: 10.1016/j.tiv.2015.06.008. PMID: 26079942

9 Genome-wide modulation of gene transcription in ovarian carcinoma cells by a new mithramycin analogue

Vizcaíno C, Núñez LE, Morís F, Portugal J.
PLoS One. 2014 Aug 11;9(8):e104687. doi: 10.1371/journal.pone.0104687. PMID: 25110883

8 The activity of a novel mithramycin analog is related to its binding to DNA, cellular accumulation, and inhibition of Sp1-driven gene transcription

Fernández-Guizán A, Mansilla S, Barceló F, Vizcaíno C, Núñez LE, Morís F, González S, Portugal J.
Chem. Biol. Interact. 2014 Jun 4;219C:123-132. doi: 10.1016/j.cbi.2014.05.019. PMID: 24907531

7 Exploring Novel Opportunities for Aureolic Acids as Anticancer Drugs

González-Sabín J, Morís F.
Biochem. & Pharmacol. 2013, 2:e140. doi: 10.4172/2167-0501.1000e140

6 Novel mithramycins abrogate the involvement of protein factors in the transcription of cell cycle control genes

Vizcaíno C, Mansilla S, Núñez LE, Méndez C, Salas JA, Morís F, Portugal J.
Biochem. Pharmacol. 2012 Nov1;84(9):1133-42. doi: 10.1016/j.bcp.2012.08.003. PMID: 22981341

5 Modulation of the activity of Sp transcription factors by mithramycin analogues as a new strategy for treatment of metastatic prostate cancer

Malek A, Núñez LE, Magistri M, Brambilla L, Jovic S, Carbone GM, Morís F, Catapano CV.
PLoS One. 2012;7(4):e35130. doi: 10.1371/journal.pone.0035130. PMID:22545098

4 Lipase-catalyzed preparation of chromomycin A₃ analogues and biological evaluation for anticancer activity

González-Sabín J, Núñez LE, Menéndez N, Braña AF, Méndez C, Salas JA, Gotor V, Morís F.
Bioorg. Med. Chem. Lett. 2012 Jul 1;22(13):4310-3. doi: 10.1016/j.bmcl.2012.05.015. PMID: 22647722

3 Regioselective Enzymatic Acylation of Aureolic Acids to Obtain Novel Analogues with Improved Antitumor Activity

González-Sabín J, Núñez LE , Braña AF, Méndez C, Salas JA, Gotor V, Morís F.
Adv. Synth. Catal. 2012, 354, 1500 – 1508. doi: 10.1002/adsc.201100944

2 A novel mithramycin analogue with high antitumor activity and less toxicity generated by combinatorial biosynthesis

Núñez LE, Nybo SE, González-Sabín J, Pérez M, Menéndez N, Braña AF, Shaaban KA, He M, Morís F, Salas JA, Rohr J, Méndez C.
Med. Chem. 2012 Jun 28;55(12):5813-25. doi: 10.1021/jm300234t. PMID: 22578073

1 The chromomycin CmmA acetyltransferase: a membrane-bound enzyme as a tool for increasing structural diversity of the antitumour mithramycin

García B, González-Sabín J, Menéndez N, Braña AF, Núñez LE, Morís F, Salas JA, Méndez C.
Microb. Biotechnol. 2011 Mar;4(2):226-38. doi: 10.1111/j.1751-7915.2010.00229.x. PMID: 21342468