从一种镰刀菌中分离并鉴定新型p53-MDM2拮抗剂氯伏菌素的结构

Isolation and structure elucidation of Chlorofusin, a novel p53-MDM2 antagonist from a Fusarium sp.

作者信息

Duncan S J, Grüschow S, Williams D H, McNicholas C, Purewal R, Hajek M, Gerlitz M, Martin S, Wrigley S K, Moore M

机构信息

Contribution from the Cambridge Centre for Molecular Recognition, University Chemical Laboratory, Lensfield Road, Cambridge CB2 1EW, UK.

出版信息

J Am Chem Soc. 2001 Jan 31;123(4):554-60. doi: 10.1021/ja002940p.

DOI:10.1021/ja002940p

PMID:11456567

Abstract

Wild-type p53 plays a crucial role in the prevention of cancer. Since dysfunction of p53 can be caused by increased levels of the protein MDM2, small molecules which antagonize the interaction between these two proteins have potential in cancer therapy. The discovery and structure determination of a fungal metabolite, chlorofusin, which antagonizes the p53/MDM2 interaction are reported.

摘要

野生型p53在预防癌症中起着至关重要的作用。由于p53功能失调可能由蛋白质MDM2水平升高引起，因此拮抗这两种蛋白质之间相互作用的小分子在癌症治疗中具有潜力。本文报道了一种拮抗p53/MDM2相互作用的真菌代谢产物氯福新的发现及结构测定。