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Titolo:
Lessons to be learned from the androgen receptor
Autore:
Brinkmann, AO;
Indirizzi:
Erasmus Univ, Dept Endocrinol & Reprod, NL-3000 DR Rotterdam, Netherlands Erasmus Univ Rotterdam Netherlands NL-3000 DR DR Rotterdam, Netherlands
Titolo Testata:
EUROPEAN JOURNAL OF DERMATOLOGY
fascicolo: 4, volume: 11, anno: 2001,
pagine: 301 - 303
SICI:
1167-1122(200107/08)11:4<301:LTBLFT>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
TRANSCRIPTIONAL COACTIVATOR; GLUCOCORTICOID RECEPTOR; COMPLEMENTARY-DNA; NUCLEAR RECEPTORS; TERMINAL DOMAIN; LIGAND-BINDING; EXPRESSION; CDNA; ACTIVATION; CLONING;
Keywords:
androgen receptor; transcriptional activation; functional domains; phosphorylation;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Brinkmann, AO Erasmus Univ, Dept Endocrinol & Reprod, POB 1738, NL-3000 DRRotterdam, Netherlands Erasmus Univ POB 1738 Rotterdam Netherlands NL-3000 DR ands
Citazione:
A.O. Brinkmann, "Lessons to be learned from the androgen receptor", EUR J DERM, 11(4), 2001, pp. 301-303

Abstract

Androgen action is mediated by the androgen receptor, a ligand dependent transcription factor, belonging to the superfamily of nuclear receptors, Thetwo most important androgens are testosterone and 5 alpha -dihydrotestosterone and their tissue specific actions are mediated by the same androgen receptor protein. Binding of androgens by the androgen receptor results in two consecutive conformational changes, which are different from those induced by antiandrogens. The androgen receptor can use different transactivation domains (AF1 and AF5, respectively, in the NH2-terminal domain and AF2-AD in the COOH-terminal domain) depending on the "form" of the receptor protein. The AF2 functionis strongly dependent on the presence of nuclear receptor coactivators. Two AF functions are ligand dependent (AF-1 and AF2), whereas AF5 operates ina ligand independent way. The ligand dependency of AF-1 in the full lengthandrogen receptor and the switch to AF5 in the COOH-terminal truncated androgen receptor strongly suggests a functional inhibitory action of the ligand-binding domain on AF-1 in the absence of Ligand and on AF5 in the presence of ligand, In vivo experiments favour a ligand dependent functional interaction between the AF-2 AD core region in the ligand-binding domain with the NH2-terminal domain. This interaction might be either direct or indirect, requiring additional factors, and results in androgen receptor driven transcription activation. The androgen receptor protein can undergo two post-translational modifications during receptor activation. Firstly, upon synthesis the protein is rapidly phosphorylated to acquire hormone binding capacities and secondly, upon hormone binding an additional phosphorylation occurs during transformation to the DNA-binding transcription activation form.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 12:20:08