2004
DOI: 10.1038/sj.bjc.6602214
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Inhibition of AKT survival pathway by a small molecule inhibitor in human endometrial cancer cells

Abstract: The PTEN (phosphatase and tensin homolog deleted on chromosome 10) tumour suppressor is mutated in 40–50% of human endometrial cancers. PTEN exerts its effects in part via inhibition of the antiapoptotic protein AKT. We demonstrate that two endometrial cancer cell lines that harbour PTEN mutations, Ishikawa and RL95-2, have high levels of phosphorylated AKT and high AKT kinase activity. Two additional endometrial cancer cell lines that express wild-type PTEN, Hec1A and KLE, have little phosphorylated AKT and m… Show more

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Cited by 71 publications
(57 citation statements)
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“…In addition, more potent AKT inhibitors, such as small-molecule inhibitor API-59CJ-OMe (9-methoxy-2-methylellipticinium acetate; ref. 53), are being developed.…”
Section: Discussionmentioning
confidence: 99%
“…In addition, more potent AKT inhibitors, such as small-molecule inhibitor API-59CJ-OMe (9-methoxy-2-methylellipticinium acetate; ref. 53), are being developed.…”
Section: Discussionmentioning
confidence: 99%
“…PD173074 had no effect on ERK1/2 or AKT activation in HEC1A cells. Due to the low level of phosphorylated AKT (Threonine 308) in HEC1A cells (13), the image shown here is an overexposure relative to the other pAKT blots presented. B, AN3CA cells were starved in 0.2% FBS overnight, pretreated with or without 1 Amol/L PD173074 for 1 h, and then stimulated with 1 nmol/L FGF7 and 10 Ag/mL heparin for 5 min.…”
Section: Discussionmentioning
confidence: 99%
“…It has also shown efficacy against ovarian carcinoma (Hu et al 2000). Also, more potent AKT inhibitors such as the small molecule inhibitor API-59CJ-OMe (9-methoxy-2-methylellipticinium acetate) (Jin et al 2004) are being developed.…”
Section: Discussionmentioning
confidence: 99%