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Abstract:

The large FK506-binding protein FKBP52 has been characterized as an important positive regulator of androgen, glucocorticoid and progesterone receptor signaling pathways. FKBP52 associates with receptor-Hsp90 complexes and is proposed to have roles in both receptor hormone binding and receptor subcellular localization. Data from biochemical and cellular studies have been corroborated in whole animal models as fkbp52-deficient male and female mice display characteristics of androgen, glucocorticoid and/or progesterone insensitivity. FKBP52 receptor specificity and the specific phenotypes displayed by the fkbp52-deficient mice have firmly established FKBP52 as a promising target for the treatment of a variety of hormone-dependent diseases. Recent studies demonstrated that the FKBP52 FK1 domain and the proline-rich loop within this domain are functionally important for FKBP52 regulation of receptor function. Based on these data, efforts are currently underway to target the FKBP52 FK1 domain and the proline-rich loop with small molecule inhibitors. © 2011 Elsevier Ltd. All rights reserved.

Registro:

Documento: Artículo
Título:Regulation of steroid hormone receptor function by the 52-kDa FK506-binding protein (FKBP52)
Autor:Sivils, J.C.; Storer, C.L.; Galigniana, M.D.; Cox, M.B.
Filiación:Border Biomedical Research Center, Department of Biological Sciences, University of Texas at El Paso, El Paso, TX, United States
Instituto de Biología y Medicina Experimental (IBYME)-CONICET, Departamento de Química Biológica, Universidad de Buenos Aires, Buenos Aires, Argentina
Palabras clave:androgen receptor; dynein adenosine triphosphatase; estrogen receptor; fk 506 binding protein; fk 506 binding protein 52; geldanamycin; glucocorticoid receptor; heat shock protein 90; karyopherin alpha; karyopherin beta; peptidylprolyl isomerase; progesterone receptor; steroid receptor; tacrolimus; unclassified drug; article; breast tumor; cellular distribution; complex formation; cytoplasm; endometriosis; female infertility; hormone binding; human; nonhuman; nuclear localization signal; nuclear pore complex; oxidative stress; priority journal; prostate cancer; protein degradation; protein phosphorylation; protein protein interaction; Animals; Drug Delivery Systems; Drug Design; Female; Humans; Male; Mice; Receptors, Androgen; Receptors, Glucocorticoid; Receptors, Progesterone; Signal Transduction; Tacrolimus Binding Proteins
Año:2011
Volumen:11
Número:4
Página de inicio:314
Página de fin:319
DOI: http://dx.doi.org/10.1016/j.coph.2011.03.010
Título revista:Current Opinion in Pharmacology
Título revista abreviado:Curr. Opin. Pharmacol.
ISSN:14714892
CODEN:COPUB
CAS:geldanamycin, 30562-34-6; karyopherin alpha, 236096-11-0; peptidylprolyl isomerase, 95076-93-0; tacrolimus, 104987-11-3; Receptors, Androgen; Receptors, Glucocorticoid; Receptors, Progesterone; Tacrolimus Binding Proteins, 5.2.1.-; tacrolimus binding protein 4, 5.2.1.-
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14714892_v11_n4_p314_Sivils

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Citas:

---------- APA ----------
Sivils, J.C., Storer, C.L., Galigniana, M.D. & Cox, M.B. (2011) . Regulation of steroid hormone receptor function by the 52-kDa FK506-binding protein (FKBP52). Current Opinion in Pharmacology, 11(4), 314-319.
http://dx.doi.org/10.1016/j.coph.2011.03.010
---------- CHICAGO ----------
Sivils, J.C., Storer, C.L., Galigniana, M.D., Cox, M.B. "Regulation of steroid hormone receptor function by the 52-kDa FK506-binding protein (FKBP52)" . Current Opinion in Pharmacology 11, no. 4 (2011) : 314-319.
http://dx.doi.org/10.1016/j.coph.2011.03.010
---------- MLA ----------
Sivils, J.C., Storer, C.L., Galigniana, M.D., Cox, M.B. "Regulation of steroid hormone receptor function by the 52-kDa FK506-binding protein (FKBP52)" . Current Opinion in Pharmacology, vol. 11, no. 4, 2011, pp. 314-319.
http://dx.doi.org/10.1016/j.coph.2011.03.010
---------- VANCOUVER ----------
Sivils, J.C., Storer, C.L., Galigniana, M.D., Cox, M.B. Regulation of steroid hormone receptor function by the 52-kDa FK506-binding protein (FKBP52). Curr. Opin. Pharmacol. 2011;11(4):314-319.
http://dx.doi.org/10.1016/j.coph.2011.03.010