Abstract: The present invention encompasses the recognition that reproducible and detectable changes in the level and or activity of Glucorticoid Receptor (GR) are associated with incidence and/or risk of Castration Resistant Prostrate Cancer (CRPC) and/or doubly resistant prostrate cancer, especially in individuals having prostrate cancer and on antiandrogen therapy, and provides for the use of GR inhibitors to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer. In some embodiments, GR inhibitors also have Androgen Receptors (AR) inhibitory activity and or administered in conjunction with AR Inhibitors. The present invention also provides technologies for identification and/or characterization of agents to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer; in some embodiments such agents alter level and/or activity of a GR. In some embodiments, provided agents show effects on a GR's activity of regulating transcription of one or more target genes.

Abstract: The present invention encompasses the recognition that reproducible and detectable changes in the level and or activity of Glucocorticoid Receptor (GR) are associated with incidence and/or risk of Castration Resistant Prostate Cancer (CRPC) and/or doubly resistant prostate cancer, specifically in individuals having prostate cancer and on antiandrogen therapy, and provides for the use of GR inhibitors to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer. In some embodiments, GR inhibitors also have Androgen Receptor (AR) inhibitory activity or are administered in conjunction with AR inhibitors. The present invention also provides technologies for identification and/or characterization of agents to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer; in some embodiments such agents alter level and/or activity of a GR. In some embodiments, provided agents show effects on a GR's activity of regulating transcription of one or more target genes.

Abstract: The present invention encompasses the recognition that reproducible and detectable changes in the level and or activity of Glucocorticoid Receptor (GR) are associated with incidence and/or risk of Castration Resistant Prostate Cancer (CRPC) and/or doubly resistant prostate cancer, specifically in individuals having prostate cancer and on antiandrogen therapy, and provides for the use of GR inhibitors to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer. In some embodiments, GR inhibitors also have Androgen Receptor (AR) inhibitory activity or are administered in conjunction with AR inhibitors. The present invention also provides technologies for identification and/or characterization of agents to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer; in some embodiments such agents alter level and/or activity of a GR. In some embodiments, provided agents show effects on a GR's activity of regulating transcription of one or more target genes.

Abstract: Provided herein are [18F]-labeled compounds having a chemical structure: R1 is 18F, 1-piperazinyl-4-CH2CH2—18F or 1-piperazinyl-4-CH2CH2OCH2CH2—18F, R2 is CH3 or 18F and R3 is Cl or 18F, such that only one of R1, R2 and R3 comprise an 18F. Also provided are methods for in vivo imaging using the [18F]-labeled compounds, particularly methods of imaging utilizing positron emission tomography. These methods are effective for diagnosing a pathophysiological condition susceptible to treatment with kinase inhibitor(s) in a subject, or for determining whether a cancer in a subject that is susceptible to being treated with a kinase inhibitor has developed resistance or increased sensitivity to the same and for maximizing tumor response to akinase inhibitor with minimal toxicity to the subject.