Cancer Research · 2010 · 144 citations · 42 references
Life SciencesMolecular BiologyOncologyCell SignalingMolecular OncologySignal TransductionAndrogen Deprivation TherapyAndrogen PhysiologyAndrogen TherapyProstate CancerProtein Kinase CascadesSteroid Hormone SignalingAmp-activated Protein Kinase InteractionAndrogen Action In ProstateAndrogen Receptor ExpressionAndrogen Receptor RegulationAndrogen ReceptorsKinase Activation MechanismsProstate Cancer RecurrenceTissue Microarray Analysis
While patients with advanced prostate cancer initially respond favorably to androgen ablation therapy, most experience a relapse of the disease within 1-2 years. Although hormone-refractory disease is unresponsive to androgen-deprivation, androgen receptor (AR)-regulated signaling pathways remain active and are necessary for cancer progression. Thus, both AR itself and the processes downstream of the receptor remain viable targets for therapeutic intervention. Microarray analysis of multiple clinical cohorts showed that the serine/threonine kinase Ca2+/calmodulin-dependent protein kinase kinase β (CaMKKβ) is both highly expressed in the prostate and further elevated in prostate cancers. Using cellular models of prostate cancer, we have determined that androgens (a) directly increase the expression of a CaMKKβ splice variant and (b) increase functional CaMKKβ protein levels as determined by the phosphorylation of both CaMKI and AMP-activated protein kinase (AMPK), two of CaMKKβ's primary substrates. Importantly, inhibition of the CaMKKβ-AMPK, but not CaMKI, signaling axis in prostate cancer cells by pharmacological inhibitors or siRNA-mediated knockdown blocks androgen-mediated migration and invasion. Conversely, overexpression of CaMKKβ alone leads to both increased AMPK phosphorylation and cell migration. Given the key roles of CaMKKβ and AMPK in the biology of prostate cancer cells, we propose that these enzymes are potential therapeutic targets in prostate cancer.
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Integrative Genomic Profiling of Human Prostate Cancer
Barry S. Taylor, Nikolaus Schultz, Haley Hieronymus et al. · Cancer Cell · 2010 · 3.8K citations · Full text
Molecular determinants of resistance to antiandrogen therapy
Charlie D. Chen, Derek S. Welsbie, Chris Tran et al. · Nature Medicine · 2003 · 2.3K citations
Medicine, Endocrinology, Urology +17