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TUCAN/CARDINAL/CARD8 and apoptosis resistance in non-small cell lung cancer cells
Agnieszka Checinska1, Giuseppe Giaccone, Bas S J Hoogeland
1Department of Medical Oncology, VU University Medical Center, 1081 HV Amsterdam, The Netherlands. a.checinska@vumc.nl
Background:
Activation of caspase-9 in response to treatment with cytotoxic drugs is inhibited in NSCLC cells, which may contribute to the clinical resistance to chemotherapy shown in this type of tumor. The aim of the present study was to investigate the mechanism of caspase-9 inhibition, with a focus on a possible role of TUCAN as caspase-9 inhibitor and a determinant of chemosensitivity in NSCLC cells.
Methods:
Caspase-9 processing and activation were investigated by Western blot and by measuring the cleavage of the fluorogenic substrate LEHD-AFC. Proteins interaction assays, and RNA interference in combination with cell viability and apoptosis assays were used to investigate the involvement of TUCAN in inhibition of caspase-9 and chemosensitivity NSCLC.
Results:
Analysis of the components of the caspase-9 activation pathway in a panel of NSCLC and SCLC cells revealed no intrinsic defects. In fact, exogenously added cytochrome c and dATP triggered procaspase-9 cleavage and activation in lung cancer cell lysates, suggesting the presence of an inhibitor. The reported inhibitor of caspase-9, TUCAN, was exclusively expressed in NSCLC cells. However, interactions between TUCAN and procaspase-9 could not be demonstrated by any of the assays used. Furthermore, RNA interference-mediated down-regulation of TUCAN did not restore cisplatin-induced caspase-9 activation or affect cisplatin sensitivity in NSCLC cells.
Conclusion:
These results indicate that procaspase-9 is functional and can undergo activation and full processing in lung cancer cell extracts in the presence of additional cytochrome c/dATP. However, the inhibitory protein TUCAN does not play a role in inhibition of procaspase-9 and in determining the sensitivity to cisplatin in NSCLC.
Insights
TUCAN does not inhibit caspase-9 activation or affect chemotherapy sensitivity in non-small cell lung cancer (NSCLC). This finding clarifies the mechanism behind drug resistance in NSCLC, suggesting TUCAN is not a viable therapeutic target.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Non-small cell lung cancer (NSCLC) exhibits resistance to chemotherapy, potentially due to inhibited caspase-9 activation.
- Investigating the mechanism of caspase-9 inhibition is crucial for understanding and overcoming this clinical resistance.
Purpose of the Study:
- To investigate the mechanism of caspase-9 inhibition in NSCLC cells.
- To determine the role of TUCAN (a known caspase-9 inhibitor) in NSCLC chemosensitivity.
Main Methods:
- Western blot and fluorogenic substrate assays (LEHD-AFC) to assess caspase-9 processing and activation.
- Protein interaction assays, RNA interference, cell viability, and apoptosis assays to evaluate TUCAN's involvement.
Main Results:
- Lung cancer cell lysates showed functional caspase-9 activation upon addition of cytochrome c and dATP, indicating an inhibitor's presence.
- TUCAN, a reported caspase-9 inhibitor, was expressed in NSCLC cells, but direct interaction with procaspase-9 was not detected.
- Down-regulating TUCAN via RNA interference did not restore cisplatin-induced caspase-9 activation or alter NSCLC sensitivity to cisplatin.
Conclusions:
- Procaspase-9 is functional and activatable in lung cancer cell extracts with cytochrome c/dATP.
- The inhibitory protein TUCAN does not play a role in inhibiting procaspase-9 or determining cisplatin sensitivity in NSCLC.
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