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Differential Presentation of Protein Interaction Surfaces on the Androgen Receptor Defines the Pharmacological Actions of Bound Ligands

  1. Author:
    Norris, J. D.
    Joseph, J. D.
    Sherk, A. B.
    Juzumiene, D.
    Turnbull, P. S.
    Rafferty, S. W.
    Cui, H. X.
    Anderson, E.
    Fan, D. J.
    Dye, D. A.
    Deng, X.
    Kazmin, D.
    Chang, C. Y.
    Willson, T. M.
    McDonnell, D. P.

  2. Author Address

    Norris, John David, Joseph, James David, Sherk, Andrea Barreto, Juzumiene, Dalia, Cui, Huaxia, Anderson, Erin, Fan, Daju, Dye, Delita Arnelle, Deng, Xiang, Kazmin, Dmitri, Chang, Ching-Yi, McDonnell, Donald Patrick] Duke Univ, Med Ctr, Dept Pharmacol & Canc Biol, Durham, NC 27710 USA. [Turnbull, Philip Stewart, Rafferty, Stephen William, Dye, Delita Arnelle, Willson, Timothy Mark] GlaxoSmithKline Inc, Res Triangle Pk, NC 27709 USA. [Deng, Xiang] NCI, Core Genotyping Facil, Adv Technol Program, SAIC Frederick Inc, Frederick, MD 21702 USA. [Juzumiene, Dalia] Affinergy Inc, Durham, NC 27713 USA.
    1. Year: 2009
  2. Journal: Chemistry & Biology
    1. 16
    2. 4
    3. Pages: 452-460
  4. Type of Article: Article
  1. Abstract:

    The pharmacological activity of different nuclear receptor ligands is reflected by their impact on receptor structure. Thus, we asked whether differential presentation of protein-protein interaction surfaces on the androgen receptor (AR), a surrogate assay of receptor conformation, could be used in a prospective manner to define the pharmacological activity of bound ligands. To this end, we identified over 150 proteins/polypeptides whose ability to interact with AR is influenced in a differential manner by ligand binding. The most discriminatory of these protein-AR interactions were used to develop a robust compound-profiling tool that enabled the separation of ligands into functionally distinguishable classes. Importantly, the ligands, within each class exhibited similar pharmacological activities, a result that highlights the relationship between receptor structure and activity and provides direction for the discovery of novel AR modulators.

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  2. DOI: 10.1016/j.chembiol.2009.01.016
  3. PMID: 19389631

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