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Ref Type | Journal Article | ||||||||||||
PMID | (8913270) | ||||||||||||
Authors | Qiao L, Koutsos M, Tsai LL, Kozoni V, Guzman J, Shiff SJ, Rigas B | ||||||||||||
Title | Staurosporine inhibits the proliferation, alters the cell cycle distribution and induces apoptosis in HT-29 human colon adenocarcinoma cells. | ||||||||||||
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Abstract Text | Staurosporine (ST), a potent inhibitor of protein kinase C (PKC), was evaluated for its effect on the proliferation of HT-29 colon adenocarcinoma cells; PKC is associated with increased colon cell proliferation. ST inhibited cell proliferation in a time- and concentration-dependent manner by up to 90%. It also blocked the G2/M phase of the cell cycle and induced classical apoptosis (sub-diploid peak on flow cytometry, DNA ladder, and typical morphological changes). The kinetics of these changes suggest that low ST concentrations (2-20 nM) may act via a different mechanism from higher (100-1000 nM) ones. The role of ST, which is currently evaluated as an antitumor agent, in colon cancer requires further evaluation. |
Molecular Profile | Treatment Approach |
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Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
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Therapy Name | Drugs | Efficacy Evidence | Clinical Trials |
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Staurosporine | Staurosporine | 0 | 0 |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
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Staurosporine | CGP-39360|AM-2282 | PAK1 Inhibitor 11 PKC Inhibitor (Pan) 11 | Staurosporine (CGP-39360) is an alkaloid pan-protein kinase C (PKC) inhibitor, with activity against several additional protein kinases, including PAK1 (PMID: 32863957), which may result in increased apoptosis and decreased tumor cell growth (PMID: 3457562, PMID: 8529658, PMID: 8913270). |
Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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