Viziteu Elena, Grandmougin Camille, Goldschmidt Hartmut, Seckinger Anja, Hose Dirk, Klein Bernard, Moreaux Jerome
Institute of Human Genetics, CNRS-UPR1142, Montpellier F-34396, France.
Medizinische Klinik und Poliklinik V, Universitätsklinikum Heidelberg, Heidelberg, Germany.
Br J Cancer. 2016 Mar 1;114(5):519-23. doi: 10.1038/bjc.2016.20. Epub 2016 Feb 11.
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.
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.
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.
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.
多发性骨髓瘤（MM）是一种无法治愈的克隆性浆细胞恶性肿瘤。MM中HIF-1α的组成性表达表明，抑制HIF-1α介导的转录是MM中一个有趣的靶点。
由于p300是缺氧诱导转录的关键共激活因子，破坏HIF-1α/p300复合物以靶向HIF活性似乎是一种有吸引力的策略。
我们报道了chetomin，一种HIF-1α/p300相互作用的抑制剂，在人骨髓瘤细胞系和患者的原发性MM细胞中表现出抗肿瘤活性。
我们的数据表明，chetomin在MM中可能具有临床价值，特别是对于那些具有高EP300/HIF-1α表达和不良预后特征的患者。
