Title : Crystal structure of a lipid
G protein-coupled
receptor
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
Output (sent_index, trigger,
protein,
sugar,
site):
Output(Part-Of) (sent_index,
protein,
site):
- 3. receptor, terminus
- 4. receptor, region
*Output_Site_Fusion* (sent_index,
protein,
sugar,
site):