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Effects of a novel antitumor depsipeptide, FR901228, on human breast cancer cells
Breast Cancer Research and Treatment (1998)
  • G Rajgolikar
  • K K Chan
  • Hwa-Chain Robert Wang, University of Tennessee, Knoxville
Human breast cancer MCF7 and MDA-MB231 cells were used to investigate the biological and molecular activities of a novel naturally occurring agent, FR901228 (FR), that possesses a potent antitumor activity against human and murine tumor cells. Investigation of the cytotoxicity of FR and induction of internucleosomal DNA degradation in FR-treated cultures revealed that FR induced apoptotic-like cell death of MCF7 and MDA-MB231 cells. In FR-treated apoptotic cultures, flow cytometry revealed that there was a significant decrease of cells in S phase of the cell cycle. In FR-treated cells there was an increased expression of p21Cip1 and phosphorylation of Bcl-2 as determined by Western immunoblotting, and a novel cytoplasmic kinase of 33 kDa, p33 kinase, as determined by the in-gel kinase assay using myelin basic protein (MBP) as a substrate. Increased expression of p21CiP1, phosphorylation of Bcl-2, and activation of p33 MBP kinase may play part of the key mechanism for FR-induced apoptosis.
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G Rajgolikar, K K Chan and Hwa-Chain Robert Wang. "Effects of a novel antitumor depsipeptide, FR901228, on human breast cancer cells" Breast Cancer Research and Treatment Vol. 51 Iss. 1 (1998)
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