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Abstract:

Crystal structures of the glucocorticoid receptor (GR) ligand binding domain in complex with various agonists and antagonists give us an insight on how ligands are recognized by the receptor and how their structure can affect the behavior of the GR. Interestingly, these structural data show how the GR can adapt its binding pocket to accommodate molecules that differ substantially from the natural ligands without loss of function. (Figure Presented) © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.

Registro:

Documento: Artículo
Título:Structure of the glucocorticoid receptor, a flexible protein that can adapt to different ligands
Autor:Veleiro, A.S.; Alvarez, L.D.; Eduardo, S.L.; Burton, G.
Filiación:Departamento de Química Orgánica and UMYMFOR (CONICET-UBA), Universidad de Buenos Aires, Ciudad Universitaria, C1428EGA Buenos Aires, Argentina
Palabras clave:Glucocorticoids; Hormones; Nuclear receptors; Protein structures; Steroids; aldosterone; deacylcortivazol; deoxycorticosterone; dexamethasone; dimer; fluticasone furoate; fluticasone propionate; glucocorticoid; glucocorticoid receptor; glucocorticoid receptor antagonist; hydrocortisone; ligand; mifepristone; nuclear receptor coactivator 2; steroid; unclassified drug; agonist; amino terminal sequence; antiinflammatory activity; apoptosis; asthma; autoimmune disease; binding site; carboxy terminal sequence; conformation; crystal structure; dermatitis; diabetes mellitus; drug mechanism; drug receptor binding; gene mutation; hydrophilicity; hydrophobicity; hypertension; immunoregulation; immunosuppressive treatment; leukemia; ligand binding; lymphoma; molecular interaction; molecular recognition; myeloma; obesity; osteoporosis; priority journal; protein binding; protein motif; protein protein interaction; protein structure; rheumatoid arthritis; short survey; Binding Sites; Computer Simulation; Crystallography, X-Ray; Ligands; Protein Structure, Tertiary; Receptors, Glucocorticoid
Año:2010
Volumen:5
Número:5
Página de inicio:649
Página de fin:659
DOI: http://dx.doi.org/10.1002/cmdc.201000014
Título revista:ChemMedChem
Título revista abreviado:ChemMedChem
ISSN:18607179
CAS:aldosterone, 52-39-1, 6251-69-0; deoxycorticosterone, 64-85-7; dexamethasone, 50-02-2; fluticasone furoate, 397864-44-7; fluticasone propionate, 80474-14-2; hydrocortisone, 50-23-7; mifepristone, 84371-65-3; Ligands; Receptors, Glucocorticoid
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_18607179_v5_n5_p649_Veleiro

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Citas:

---------- APA ----------
Veleiro, A.S., Alvarez, L.D., Eduardo, S.L. & Burton, G. (2010) . Structure of the glucocorticoid receptor, a flexible protein that can adapt to different ligands. ChemMedChem, 5(5), 649-659.
http://dx.doi.org/10.1002/cmdc.201000014
---------- CHICAGO ----------
Veleiro, A.S., Alvarez, L.D., Eduardo, S.L., Burton, G. "Structure of the glucocorticoid receptor, a flexible protein that can adapt to different ligands" . ChemMedChem 5, no. 5 (2010) : 649-659.
http://dx.doi.org/10.1002/cmdc.201000014
---------- MLA ----------
Veleiro, A.S., Alvarez, L.D., Eduardo, S.L., Burton, G. "Structure of the glucocorticoid receptor, a flexible protein that can adapt to different ligands" . ChemMedChem, vol. 5, no. 5, 2010, pp. 649-659.
http://dx.doi.org/10.1002/cmdc.201000014
---------- VANCOUVER ----------
Veleiro, A.S., Alvarez, L.D., Eduardo, S.L., Burton, G. Structure of the glucocorticoid receptor, a flexible protein that can adapt to different ligands. ChemMedChem. 2010;5(5):649-659.
http://dx.doi.org/10.1002/cmdc.201000014