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Hormone-Dependent Coactivator Binding to a Hydrophobic Cleft on Nuclear Receptors

Science  12 Jun 1998:
Vol. 280, Issue 5370, pp. 1747-1749
DOI: 10.1126/science.280.5370.1747

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Abstract

The ligand-binding domain of nuclear receptors contains a transcriptional activation function (AF-2) that mediates hormone-dependent binding of coactivator proteins. Scanning surface mutagenesis on the human thyroid hormone receptor was performed to define the site that binds the coactivators, glucocorticoid receptor–interacting protein 1 (GRIP1) and steroid receptor coactivator 1 (SRC-1). The residues involved encircle a small surface that contains a hydrophobic cleft. Ligand activation of transcription involves formation of this surface by folding the carboxyl-terminal α helix against a scaffold of three other helices. These features may represent general ones for nuclear receptors.

  • * To whom correspondence should be addressed. E-mail: west{at}socrates.ucsf.edu (B.L.W.) or kushner{at}itsa.ucsf.edu(P.J.K.)

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