3V2W: Crystal Structure Of A Lipid G Protein-coupled Receptor At 3.35a

Citation:
Abstract
The lyso-phospholipid sphingosine 1-phosphate modulates lymphocyte trafficking, endothelial development and integrity, heart rate, and vascular tone and maturation by activating G protein-coupled sphingosine 1-phosphate receptors. Here, we present the crystal structure of the sphingosine 1-phosphate receptor 1 fused to T4-lysozyme (S1P(1)-T4L) in complex with an antagonist sphingolipid mimic. Extracellular access to the binding pocket is occluded by the amino terminus and extracellular loops of the receptor. Access is gained by ligands entering laterally between helices I and VII within the transmembrane region of the receptor. This structure, along with mutagenesis, agonist structure-activity relationship data, and modeling, provides a detailed view of the molecular recognition and requirement for hydrophobic volume that activates S1P(1), resulting in the modulation of immune and stromal cell responses.
PDB ID: 3V2WDownload
MMDB ID: 97307
PDB Deposition Date: 2011/12/12
Updated in MMDB: 2017/06
Experimental Method:
x-ray diffraction
Resolution: 3.35  Å
Similar Structures:
Biological Unit for 3V2W: monomeric; determined by software (PISA)
Molecular Components in 3V2W
Label Count Molecule
Protein (1 molecule)
1
Sphingosine 1-phosphate Receptor 1, Lysozyme Chimera
Molecule annotation
Chemicals (2 molecules)
1
1
2
1
* Click molecule labels to explore molecular sequence information.

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