pha-680632 and Neoplasms

pha-680632 has been researched along with Neoplasms* in 2 studies

Reviews

1 review(s) available for pha-680632 and Neoplasms

ArticleYear
Discovery and development of aurora kinase inhibitors as anticancer agents.
    Journal of medicinal chemistry, 2009, May-14, Volume: 52, Issue:9

    Topics: Animals; Antineoplastic Agents; Aurora Kinases; Drug Discovery; Humans; Mitosis; Neoplasms; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases

2009

Other Studies

1 other study(ies) available for pha-680632 and Neoplasms

ArticleYear
Enhancement of radiation response by inhibition of Aurora-A kinase using siRNA or a selective Aurora kinase inhibitor PHA680632 in p53-deficient cancer cells.
    British journal of cancer, 2007, Dec-17, Volume: 97, Issue:12

    Overexpression of Aurora-A kinase has been correlated with cancer susceptibility and poor prognosis in several human cancers. In this study, we evaluated the effect of inhibition of Aurora-A kinase on cell cycle progression and tumour cell survival after exposure to ionising radiation (IR). Combined IR and Aurora-A inhibition by short interfering RNA (siRNA) or by PHA680632 (a selective Aurora kinase inhibitor with submicromolar activity against Aurora-A) prior to IR led to an enhancement of radiation-induced annexin V positive cells, micronuclei formation, and Brca1 foci formation only in cells with deficient p53. However, the drug brought about additive to sub-additive interaction with radiation with regard to in vitro clonogenic survival. Cell cycle analysis revealed a high >4N DNA content 24 h after PHA680632 exposure. DNA content >4N was reduced dramatically when cells were irradiated combined with PHA680632 simultaneously. In vivo xenografts (p53-/- HCT116) of a mice study showed enhanced tumour growth delay (TGD) after the PHA680632-IR combinatorial treatment compared with IR alone. These results demonstrate that PHA680632 in association with radiation leads to an additive effect in cancer cells, especially in the p53-deficient cells, but does not act as a radiosensitiser in vitro or in vivo.

    Topics: Aneugens; Animals; Aurora Kinase A; Aurora Kinases; Cell Survival; Genes, p53; HCT116 Cells; HT29 Cells; Humans; Mice; Mice, Nude; Neoplasms; Protein Serine-Threonine Kinases; Pyrazoles; Pyrroles; Radiation-Sensitizing Agents; RNA, Small Interfering; Xenograft Model Antitumor Assays

2007