title: Structural biology of the S1P1 receptor.
abstract: The sphingosine 1 phosphate receptor family has been studied widely since the initial discovery of its first member, endothelium differentiation gene 1. Since this initial discovery, the family has been renamed and the primary member of the family, the S1P1 receptor, has been targeted for a variety of disease indications and successfully drugged for the treatment of patients with relapsing multiple sclerosis. Recently, the three-dimensional structure of the S1P1 receptor has been determined by X-ray crystallography and the specifics of the sphingosine 1 phosphate ligand binding pocket mapped. Key structural features for the S1P1 receptor will be reviewed and the potential binding modes of additional pharmacologically active agents against the receptor will be analyzed in an effort to better understand the structural basis of important receptor-ligand interactions.
authors.affiliation: Receptos, Inc., 10853 Road To The Cure, Suite 205, San Diego, CA, 92121, USA, mhanson@receptos.com.
authors.forename: Michael A
authors.initials: MA
authors.lastname: Hanson
authors.forename: Robert
authors.initials: R
authors.lastname: Peach
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001665:Binding Sites; D006801:Humans; D008246:Lysophospholipids / Q000737:chemistry / Q000378:metabolism; D008969:Molecular Sequence Data; D017434:Protein Structure, Tertiary; D049349:Receptors, Lysosphingolipid / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism; D013110:Sphingosine / Q000031:analogs & derivatives / Q000737:chemistry / Q000378:metabolism
chemical_list: D008246:Lysophospholipids; D049349:Receptors, Lysosphingolipid; C060506:sphingosine 1-phosphate; D013110:Sphingosine