Schroeder Frank C, Kau Tweeny R, Silver Pamela A, Clardy Jon
Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115, USA.
J Nat Prod. 2005 Apr;68(4):574-6. doi: 10.1021/np049624z.
A small collection of marine natural product extracts was screened for compounds that would compensate lost tumor suppressor functionality in PTEN-deficient cells. From the most active extract, the previously unreported bromotyrosine derivative, psammaplysene A (1), was identified. Psammaplysene A compensates for PTEN loss by relocalizing the transcription factor FOXO1a to the nucleus.
对一小批海洋天然产物提取物进行了筛选,以寻找能够补偿PTEN缺陷细胞中丧失的肿瘤抑制功能的化合物。从活性最强的提取物中,鉴定出了此前未报道的溴酪氨酸衍生物——沙海葵素A(1)。沙海葵素A通过将转录因子FOXO1a重新定位到细胞核来补偿PTEN的缺失。