|Title||High-throughput assay for G(2) checkpoint inhibitors and identification of the structurally novel compound isogranulatimide|
|Publication Type||Journal Article|
|Year of Publication||1998|
|Authors||Roberge, 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|
|Type of Article||Article|
|Keywords||ANTITUMOR DRUG, BHK CELLS, CAFFEINE, CELL-CYCLE CHECKPOINTS, DNA-DAMAGE, HELA-CELLS, mitosis, P34(CDC2) KINASE, P53 FUNCTION, PREMATURE, PROTEIN KINASE-C|
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|