1h9u
From Proteopedia
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THE STRUCTURE OF THE HUMAN RETINOID-X-RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH THE SPECIFIC SYNTHETIC AGONIST LG100268
Overview
Ligands that specifically target retinoid-X receptors (RXRs) are emerging, as potentially powerful therapies for cancer, diabetes, and the lowering, of circulatory cholesterol. To date, RXR has only been crystallized in the, absence of ligand or with the promiscuous ligand 9-cis retinoic acid, which also activates retinoic acid receptors. Here we present the, structure of hRXRbeta in complex with the RXR-specific agonist LG100268, (LG268). The structure clearly reveals why LG268 is specific for the RXR, ligand binding pocket and will not activate retinoic acid receptors., Intriguingly, in the crystals, the C-terminal "activation" helix, (AF-2/helix H12) is trapped in a novel position not seen in other nuclear, receptor structures such that it does not cap the ligand binding cavity., ... [(full description)]
About this Structure
1H9U is a [Single protein] structure of sequence from [Homo sapiens] with NI, CL and LG2 as [ligands]. Full crystallographic information is available from [OCA].
Reference
The structural basis for the specificity of retinoid-X receptor-selective agonists: new insights into the role of helix H12., Love JD, Gooch JT, Benko S, Li C, Nagy L, Chatterjee VK, Evans RM, Schwabe JW, J Biol Chem. 2002 Mar 29;277(13):11385-91. Epub 2002 Jan 8. PMID:11782480
Page seeded by OCA on Mon Oct 29 21:52:34 2007
Categories: Homo sapiens | Single protein | Gooch, J.T. | Love, J.D. | Schwabe, J.W.R. | CL | LG2 | NI | Nuclear receptor | Rxr | Transcription factor
