title: Bromodomain and extraterminal protein inhibitors in pediatrics: A review of the literature.
abstract: The last few years have seen the identification of pharmacologic approaches to target bromodomain and extraterminal (BET) proteins for cancer treatment. These proteins have an essential role in gene transcription regulation by binding acetylated lysine residues on histone tails, activating gene transcription. BET inhibitors have been tested in preclinical models including pediatric malignancies and several adult clinical trials are ongoing. Since the development of new drugs in pediatric cancer has long lagged behind programs for adults, the aim of this review is to show the importance of these therapies in pediatric malignancies to support their development in pediatric oncology/hematology.
authors.affiliation: Département d'Oncologie Pédiatrique, Adolescents et Jeunes Adultes de l'Institut Curie, Paris, France.
authors.forename: Irene
authors.initials: I
authors.lastname: Jiménez
authors.affiliation: Service d'hémato-immunologie de l'Hôpital Universitaire Robert Debré, Paris, France.|Institut Universitaire d'Hématologie, Centre Hayem, Hôpital Saint-Louis, Paris, France.|Professor of Pediatrics, Université Paris-Diderot, Paris, France.
authors.forename: André
authors.initials: A
authors.lastname: Baruchel
authors.affiliation: Département d'Oncologie Pédiatrique, Adolescents et Jeunes Adultes de l'Institut Curie, Paris, France.|Professor of Pediatrics, Sorbonne Paris Cité, Université Paris-Descartes, Paris, France.
authors.forename: François
authors.initials: F
authors.lastname: Doz
authors.affiliation: Department of Pediatric Oncology/Hematology, Charité-Universitätsmedizin Berlin, Berlin, Germany.
authors.forename: Johannes
authors.initials: J
authors.lastname: Schulte
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use; D001932:Brain Neoplasms / Q000188:drug therapy*; D018797:Cell Cycle Proteins; D002648:Child; D002675:Child, Preschool; D019337:Hematologic Neoplasms / Q000188:drug therapy*; D006801:Humans; D009447:Neuroblastoma / Q000188:drug therapy*; D009687:Nuclear Proteins / Q000037:antagonists & inhibitors*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D016601:RNA-Binding Proteins / Q000037:antagonists & inhibitors*; D014157:Transcription Factors / Q000037:antagonists & inhibitors*; D015533:Transcriptional Activation / Q000187:drug effects; D000092468:Bromodomain Containing Proteins
chemical_list: D000970:Antineoplastic Agents; D018797:Cell Cycle Proteins; D009687:Nuclear Proteins; D017346:Protein Serine-Threonine Kinases; D016601:RNA-Binding Proteins; D014157:Transcription Factors; C098415:BRD2 protein, human; D000092468:Bromodomain Containing Proteins; C109106:BRD3 protein, human; C441289:BRD4 protein, human; C109570:BRDT protein, human
keywords: BET inhibitors; bromodomain; epigenetics; pediatrics