Abstract
Sphingosine 1-phosphate and lysophosphatidic acid are two phospholipid growth factors whose importance in physiology and pathophysiology is becoming more and more apparent. Structure-activity relationships for agonism and antagonism at the thirteen known cell-surface and one intracellular receptor are described. Particular emphasis is placed on ligands having different selectivity than the parent molecules. Structural insights regarding agonist and antagonist recognition by the receptors from both computational modeling studies and crystallography are also discussed.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
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Review
MeSH terms
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Animals
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Humans
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Ligands
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PPAR gamma / metabolism
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Protein Binding
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Receptors, G-Protein-Coupled / metabolism
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Receptors, Lysophosphatidic Acid / agonists*
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Receptors, Lysophosphatidic Acid / antagonists & inhibitors*
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Receptors, Lysosphingolipid / agonists*
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Receptors, Lysosphingolipid / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Ligands
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PPAR gamma
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Receptors, G-Protein-Coupled
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Receptors, Lysophosphatidic Acid
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Receptors, Lysosphingolipid