European journal of pharmacology, 2008-09, Vol.591 (1), p.102-105
2008
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- Autor(en) / Beteiligte
- Titel
- Evaluation of Polo-like Kinase 1 inhibition on the G2/M checkpoint in Acute Myelocytic Leukaemia
- Ist Teil von
- European journal of pharmacology, 2008-09, Vol.591 (1), p.102-105
- Ort / Verlag
- Amsterdam: Elsevier B.V
- Erscheinungsjahr
- 2008
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Polo-Kinase 1 (PLK1) is a key cell cycle regulator that is necessary for checkpoint recovery after DNA damage-induced G2 arrest. We have examined the effects of PLK inhibition in Acute Myelocytic Leukaemia (AML) cells, whose resistance to genotoxic agents is thought to be associated with checkpoint reinforcement. We report that in U937 AML cells, PLK1 participates in checkpoint recovery, and that inhibition of PLK by the GW843682X compound results in mitotic accumulation and apoptosis. We also found that when challenged with VP-16, inhibition of PLK1 prevented U937 cells from checkpoint exit. Finally, we found that treatment with GW843682X slightly reduced genotoxic-induced inhibition of colony formation efficiency of primary leukaemia cells (CFU-L) from AML patients.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0014-2999, 1879-0712eISSN: 1879-0712, 0014-2999DOI: 10.1016/j.ejphar.2008.06.062Titel-ID: cdi_hal_primary_oai_HAL_hal_00317521v1
- Format
- –
- Schlagworte
- AML (Acute Myelocytic Leukaemia), Antineoplastic Agents, Phytogenic - pharmacology, Benzimidazoles - pharmacology, Biological and medical sciences, Cell cycle, Cell Cycle Proteins - antagonists & inhibitors, Cell Cycle Proteins - metabolism, Cell Division - drug effects, Cellular Biology, Etoposide - pharmacology, G2 Phase - drug effects, G2/M checkpoint, Humans, Leukemia, Myeloid, Acute - metabolism, Life Sciences, Medical sciences, Mitosis - drug effects, Pharmacology. Drug treatments, PLK1 (Polo-Kinase 1), Polo-Like Kinase 1, Protein Serine-Threonine Kinases - antagonists & inhibitors, Protein Serine-Threonine Kinases - metabolism, Proto-Oncogene Proteins - antagonists & inhibitors, Proto-Oncogene Proteins - metabolism, Thiophenes - pharmacology, U937 Cells