title: Chetomin, targeting HIF-1α/p300 complex, exhibits antitumour activity in multiple myeloma.
abstract: BACKGROUND
  Multiple myeloma (MM) is an incurable clonal plasma cell malignancy. The constitutive expression of HIF-1α in MM suggests that inhibition of HIF-1α-mediated transcription represents an interesting target in MM.
  
  
  METHODS
  As p300 is a crucial co-activator of hypoxia-inducible transcription, disrupting the complex HIF-1α/p300 to target HIF activity appears to be an attractive strategy.
  
  
  RESULTS
  We reported that chetomin, an inhibitor of HIF-1α/p300 interaction, exhibits antitumour activity in human myeloma cell lines and primary MM cells from patients.
  
  
  CONCLUSIONS
  Our data suggest that chetomin may be of clinical value in MM and especially for patients characterised by a high EP300/HIF-1α expression and a poor prognosis.
authors: Institute of Human Genetics, CNRS-UPR1142, Montpellier F-34396, France.
authors: Elena
authors: E
authors: Viziteu
authors: Institute of Human Genetics, CNRS-UPR1142, Montpellier F-34396, France.
authors: Camille
authors: C
authors: Grandmougin
authors: Medizinische Klinik und Poliklinik V, Universitätsklinikum Heidelberg, Heidelberg, Germany.|Nationales Centrum für Tumorerkrankungen, Heidelberg, Germany.
authors: Hartmut
authors: H
authors: Goldschmidt
authors: Medizinische Klinik und Poliklinik V, Universitätsklinikum Heidelberg, Heidelberg, Germany.|Nationales Centrum für Tumorerkrankungen, Heidelberg, Germany.
authors: Anja
authors: A
authors: Seckinger
authors: Medizinische Klinik und Poliklinik V, Universitätsklinikum Heidelberg, Heidelberg, Germany.|Nationales Centrum für Tumorerkrankungen, Heidelberg, Germany.
authors: Dirk
authors: D
authors: Hose
authors: Institute of Human Genetics, CNRS-UPR1142, Montpellier F-34396, France.|Department of Biological Haematology, CHU Montpellier, Montpellier, France.|University of Montpellier 1, UFR de Médecine, Montpellier, France.
authors: Bernard
authors: B
authors: Klein
authors: Institute of Human Genetics, CNRS-UPR1142, Montpellier F-34396, France.|Department of Biological Haematology, CHU Montpellier, Montpellier, France.|University of Montpellier 1, UFR de Médecine, Montpellier, France.
authors: Jerome
authors: J
authors: Moreaux
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D004220:Disulfides / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D050881:E1A-Associated p300 Protein / Q000235:genetics*; D020869:Gene Expression Profiling; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects*; D006801:Humans; D051795:Hypoxia-Inducible Factor 1, alpha Subunit / Q000235:genetics*; D026121:Indole Alkaloids / Q000494:pharmacology*; D058990:Molecular Targeted Therapy; D009101:Multiple Myeloma / Q000188:drug therapy* / Q000235:genetics; D011379:Prognosis
chemical_list: D004220:Disulfides; C497442:HIF1A protein, human; D051795:Hypoxia-Inducible Factor 1, alpha Subunit; D026121:Indole Alkaloids; C001598:chetomin; D050881:E1A-Associated p300 Protein; C494360:EP300 protein, human