Literature DB >> 28868353

Dual epigenetic modifiers for cancer therapy.

Edurne San José-Enériz1, Obdulia Rabal2, Xabier Agirre1, Julen Oyarzabal2, Felipe Prosper1,3.   

Abstract

Epigenetic drug discovery is an emerging strategy for the treatment of cancer and other pathologies. Here, we discuss our recent discovery of first-in-class dual reversible inhibitors of the histone methyltransferase activity of G9a/EHMT2 and DNA methyltransferases showing in vivo efficacy in human tumors. Current and future investigation lines are presented.

Entities:  

Keywords:  Cancer; DNMT; G9a; drug discovery; epigenetic

Year:  2017        PMID： 28868353      PMCID： PMC5540207          DOI： 10.1080/23723556.2017.1342748

Source DB:  PubMed          Journal:  Mol Cell Oncol        ISSN： 2372-3556


  8 in total

1.  Probing the epigenome.

Authors:  Andrea Huston; Cheryl H Arrowsmith; Stefan Knapp; Matthieu Schapira
Journal:  Nat Chem Biol       Date:  2015-08       Impact factor: 15.040

Review 2.  Inhibitors of Protein Methyltransferases and Demethylases.

Authors:  H Ümit Kaniskan; Michael L Martini; Jian Jin
Journal:  Chem Rev       Date:  2017-03-24       Impact factor: 60.622

3.  Target watch: Drugging the epigenome.

Authors:  Samia Burridge
Journal:  Nat Rev Drug Discov       Date:  2013-02       Impact factor: 84.694

4.  Epigenetic silencing of the tumor suppressor microRNA Hsa-miR-124a regulates CDK6 expression and confers a poor prognosis in acute lymphoblastic leukemia.

Authors:  Xabier Agirre; Amaia Vilas-Zornoza; Antonio Jiménez-Velasco; José Ignacio Martin-Subero; Lucia Cordeu; Leire Gárate; Edurne San José-Eneriz; Gloria Abizanda; Paula Rodríguez-Otero; Puri Fortes; José Rifón; Eva Bandrés; María José Calasanz; Vanesa Martín; Anabel Heiniger; Antonio Torres; Reiner Siebert; José Román-Gomez; Felipe Prósper
Journal:  Cancer Res       Date:  2009-05-12       Impact factor: 12.701

Review 5.  DNA methyltransferase inhibitors in cancer: From pharmacology to translational studies.

Authors:  Dany Pechalrieu; Chantal Etievant; Paola B Arimondo
Journal:  Biochem Pharmacol       Date:  2016-12-09       Impact factor: 5.858

Review 6.  DNA methylation profiling in the clinic: applications and challenges.

Authors:  Holger Heyn; Manel Esteller
Journal:  Nat Rev Genet       Date:  2012-09-04       Impact factor: 53.242

7.  Whole-epigenome analysis in multiple myeloma reveals DNA hypermethylation of B cell-specific enhancers.

Authors:  Xabier Agirre; Giancarlo Castellano; Marien Pascual; Simon Heath; Marta Kulis; Victor Segura; Anke Bergmann; Anna Esteve; Angelika Merkel; Emanuele Raineri; Lidia Agueda; Julie Blanc; David Richardson; Laura Clarke; Avik Datta; Nuria Russiñol; Ana C Queirós; Renée Beekman; Juan R Rodríguez-Madoz; Edurne San José-Enériz; Fang Fang; Norma C Gutiérrez; José M García-Verdugo; Michael I Robson; Eric C Schirmer; Elisabeth Guruceaga; Joost H A Martens; Marta Gut; Maria J Calasanz; Paul Flicek; Reiner Siebert; Elías Campo; Jesús F San Miguel; Ari Melnick; Hendrik G Stunnenberg; Ivo G Gut; Felipe Prosper; José I Martín-Subero
Journal:  Genome Res       Date:  2015-02-02       Impact factor: 9.043

8.  Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies.

Authors:  Edurne San José-Enériz; Xabier Agirre; Obdulia Rabal; Amaia Vilas-Zornoza; Juan A Sanchez-Arias; Estibaliz Miranda; Ana Ugarte; Sergio Roa; Bruno Paiva; Ander Estella-Hermoso de Mendoza; Rosa María Alvarez; Noelia Casares; Victor Segura; José I Martín-Subero; François-Xavier Ogi; Pierre Soule; Clara M Santiveri; Ramón Campos-Olivas; Giancarlo Castellano; Maite Garcia Fernandez de Barrena; Juan Roberto Rodriguez-Madoz; Maria José García-Barchino; Juan Jose Lasarte; Matias A Avila; Jose Angel Martinez-Climent; Julen Oyarzabal; Felipe Prosper
Journal:  Nat Commun       Date:  2017-05-26       Impact factor: 14.919
  8 in total
  1 in total

Review 1.  The timeline of epigenetic drug discovery: from reality to dreams.

Authors:  A Ganesan; Paola B Arimondo; Marianne G Rots; Carmen Jeronimo; María Berdasco
Journal:  Clin Epigenetics       Date:  2019-12-02       Impact factor: 6.551
  1 in total

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