2lbd

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==Overview==
==Overview==
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The 2.0-A crystal structure of the ligand-binding domain (LBD) of the, human retinoic acid receptor (RAR)-gamma bound to all-trans retinoic acid, reveals the ligand-binding interactions and suggests an electrostatic, guidance mechanism. The overall fold is similar to that of the human, RXR-alpha apo-LBD, except for the carboxy-terminal part which folds back, towards the LBD core, contributing to the hydrophobic ligand pocket and, 'sealing' its entry site. We propose a 'mouse trap' mechanism whereby a, ligand-induced conformational transition repositions the amphipathic, alpha-helix of the AF-2 activating domain and forms a transcriptionally, active receptor.
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The 2.0-A crystal structure of the ligand-binding domain (LBD) of the human retinoic acid receptor (RAR)-gamma bound to all-trans retinoic acid reveals the ligand-binding interactions and suggests an electrostatic guidance mechanism. The overall fold is similar to that of the human RXR-alpha apo-LBD, except for the carboxy-terminal part which folds back towards the LBD core, contributing to the hydrophobic ligand pocket and 'sealing' its entry site. We propose a 'mouse trap' mechanism whereby a ligand-induced conformational transition repositions the amphipathic alpha-helix of the AF-2 activating domain and forms a transcriptionally active receptor.
==About this Structure==
==About this Structure==
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Moras, D.]]
[[Category: Moras, D.]]
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[[Category: Renaud, J.P.]]
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[[Category: Renaud, J P.]]
[[Category: Rochel, N.]]
[[Category: Rochel, N.]]
[[Category: Ruff, M.]]
[[Category: Ruff, M.]]
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[[Category: SPINE, Structural.Proteomics.in.Europe.]]
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[[Category: SPINE, Structural Proteomics in Europe.]]
[[Category: REA]]
[[Category: REA]]
[[Category: active conformation]]
[[Category: active conformation]]
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[[Category: transcription regulation]]
[[Category: transcription regulation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 17:37:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:06:59 2008''

Revision as of 16:07, 21 February 2008


2lbd, resolution 2.06Å

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LIGAND-BINDING DOMAIN OF THE HUMAN RETINOIC ACID RECEPTOR GAMMA BOUND TO ALL-TRANS RETINOIC ACID

Overview

The 2.0-A crystal structure of the ligand-binding domain (LBD) of the human retinoic acid receptor (RAR)-gamma bound to all-trans retinoic acid reveals the ligand-binding interactions and suggests an electrostatic guidance mechanism. The overall fold is similar to that of the human RXR-alpha apo-LBD, except for the carboxy-terminal part which folds back towards the LBD core, contributing to the hydrophobic ligand pocket and 'sealing' its entry site. We propose a 'mouse trap' mechanism whereby a ligand-induced conformational transition repositions the amphipathic alpha-helix of the AF-2 activating domain and forms a transcriptionally active receptor.

About this Structure

2LBD is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.

Reference

Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid., Renaud JP, Rochel N, Ruff M, Vivat V, Chambon P, Gronemeyer H, Moras D, Nature. 1995 Dec 14;378(6558):681-9. PMID:7501014

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