Accession Number : ADA620319


Title :   Targeting Prostate Cancer with Bifunctional Modulators of the Androgen Receptor


Descriptive Note : Annual rept. 30 Sep 2013-29 Sep 2014


Corporate Author : MICHIGAN UNIV ANN ARBOR


Personal Author(s) : Mapp, Anna K ; Sturlis, Steven ; Carolan, James ; van Dyke, Aaron


Full Text : https://apps.dtic.mil/dtic/tr/fulltext/u2/a620319.pdf


Report Date : Oct 2014


Pagination or Media Count : 18


Abstract : The overall goal of this research project is to develop and implement a conceptually innovative strategy for down-regulating androgen receptor: the creation of bifunctional molecules that simultaneously bind to the androgen receptor and to bromodomain proteins Brd4. In this way, genes that are typically regulated by androgen receptor and glucocorticoid receptor will be extrinsically controlled. In this final year of funding, we completed the functional characterization of agonist and antagonist-based bi-functional recruiters. Importantly, we have a suite of recruiters that show context specificity. In the extension period of the work, we are completing RNAseq experiments to gain a complete understanding of the context specificity of this exciting class of molecules.


Descriptors :   *ANDROGENS , *PROSTATE CANCER , *RECEPTOR SITES(PHYSIOLOGY) , ADRENAL CORTEX HORMONES , CELLS(BIOLOGY) , CLINICAL MEDICINE , CORTICOSTEROID AGENTS , DIAGNOSIS(MEDICINE) , ENDOCRINOLOGY , EPITHELIUM , EXPERIMENTAL DATA , GENE EXPRESSION , MODULATORS , MOLECULAR DYNAMICS , PATHOGENESIS , PROTEINS , RIBONUCLEIC ACIDS , SENSE ORGANS , TARGETING , TRANSCRIPTION(GENETICS)


Subject Categories : Biochemistry
      Genetic Engineering and Molecular Biology
      Anatomy and Physiology
      Medicine and Medical Research


Distribution Statement : APPROVED FOR PUBLIC RELEASE