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High-throughput assay for G(2) checkpoint inhibitors and identification of the structurally novel compound isogranulatimide

TitleHigh-throughput assay for G(2) checkpoint inhibitors and identification of the structurally novel compound isogranulatimide
Publication TypeJournal Article
Year of Publication1998
AuthorsRoberge, M, Berlinck, RGS, Xu, L, Anderson, HJ, Lim, LY, Curman, D, Stringer, CM, Friend, SH, Davies, P, Vincent, I, Haggarty, SJ, Kelly, MT, Britton, R, Piers, E, Andersen, RJ
JournalCancer Research
Volume58
Pagination5701-5706
Date PublishedDec
Type of ArticleArticle
ISBN Number0008-5472
KeywordsANTITUMOR DRUG, BHK CELLS, CAFFEINE, CELL-CYCLE CHECKPOINTS, DNA-DAMAGE, HELA-CELLS, mitosis, P34(CDC2) KINASE, P53 FUNCTION, PREMATURE, PROTEIN KINASE-C
Abstract

Treatment of cancer cells lacking p53 function with G(2) checkpoint inhibitors sensitizes them to the toxic effects of DNA damage and has been proposed as a strategy for cancer therapy. However, few inhibitors are known, and they have been found serendipitously, We report the development of a G(2) checkpoint inhibition assay that is suitable for high-throughput screening and its application to a screen of 1300 natural extracts. We present the isolation of a new G(2) checkpoint inhibitor, the structurally novel compound isogranulatimide. In combination with gamma-irradiation, isogranulatimide selectively kills MCF-7 cells lacking p53 function.

URL<Go to ISI>://000077499800017