publication . Article . Other literature type . 2011

Helix 11 Dynamics is Critical for Constitutive Androstane Receptor Activity

Wright, Edward; Busby, Scott A.; Wisecarver, Sarah; Vincent, Jeremy; Griffin, Patrick R.; Fernandez, Elias J.;
Open Access English
  • Published: 12 Jan 2011 Journal: Structure, volume 19, issue 1, pages 37-44 (issn: 0969-2126, Copyright policy)
  • Publisher: Elsevier BV
Abstract
The constitutive androstane receptor (CAR) transactivation can occur in the absence of exogenous ligand and this activity is enhanced by agonists TCPOBOP and meclizine. We use biophysical and cell-based assays to show that increased activity of CAR(TCPOBOP) relative to CAR(meclizine) corresponds to a higher affinity of CAR(TCPOBOP) for the steroid receptor coactivator-1. Additionally, steady-state fluorescence spectra suggest conformational differences between CAR(TCPOBOP):RXR and CAR(meclizine):RXR. Hydrogen/deuterium exchange (HDX) data indicate that the CAR activation function 2 (AF-2) is more stable in CAR(TCPOBOP):RXR and CAR(meclizine):RXR than in CAR:RXR....
Subjects
mesheuropmc: human activitiesbody regionsembryonic structureslipids (amino acids, peptides, and proteins)hormones, hormone substitutes, and hormone antagonists
free text keywords: Molecular Biology, Structural Biology, Article
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publication . Article . Other literature type . 2011

Helix 11 Dynamics is Critical for Constitutive Androstane Receptor Activity

Wright, Edward; Busby, Scott A.; Wisecarver, Sarah; Vincent, Jeremy; Griffin, Patrick R.; Fernandez, Elias J.;