Chemical approaches to the lysophospholipid receptors.
Both ligand-based and GPCR privileged scaffold chemical tools have recently emerged to provide new insights into the function and physiology of the GPCR lysophospholipid receptors both in vitro and in vivo. Both rational, design-based approaches as well as hybrid approaches where high throughput screening has been coupled to an understanding of critical molecular interactions have been productive in advancing understanding of physiology and potential therapeutics in this field. It is now feasible to identify reasonably potent and selective small molecules that provide chemical proof-of-concept in vivo directly from high throughput screening. These developments, coupled with the availability of receptor knock-out mice, presage rapid progress in the field.
Rosen
Hugh
H
Department of Immunology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA. hrosen@scripps.edu
D000818:Animals; D019204:GTP-Binding Proteins / Q000737:chemistry; D006801:Humans; D008024:Ligands; D008246:Lysophospholipids / Q000737:chemistry / Q000378:metabolism; D011485:Protein Binding; D043562:Receptors, G-Protein-Coupled / Q000145:classification / Q000378:metabolism; D049312:Receptors, Lysophospholipid / Q000737:chemistry*; D013110:Sphingosine / Q000031:analogs & derivatives / Q000737:chemistry
D008024:Ligands; D008246:Lysophospholipids; D043562:Receptors, G-Protein-Coupled; D049312:Receptors, Lysophospholipid; C060506:sphingosine 1-phosphate; D019204:GTP-Binding Proteins; D013110:Sphingosine; C032881:lysophosphatidic acid