'Crystal' Clear? Lysophospholipid Receptor Structure Insights and Controversies

Overview

Journal Trends Pharmacol Sci

Specialty Pharmacology

Date 2018 Oct 23

PMID 30343728

Citations 19

Authors

Victoria A Blaho

Jerold Chun

Affiliations

Soon will be listed here.

Abstract

Lysophospholipids (LPLs), particularly sphingosine 1-phosphate (S1P) and lysophosphatidic acid (LPA), are bioactive lipid modulators of cellular homeostasis and pathology. The discovery and characterization of five S1P- and six LPA-specific G protein-coupled receptors (GPCRs), S1P and LPA, have expanded their known involvement in all mammalian physiological systems. Resolution of the S1P, LPA, and LPA crystal structures has fueled the growing interest in these receptors and their ligands as targets for pharmacological manipulation. In this review, we have attempted to provide an integrated overview of the three crystallized LPL GPCRs with biochemical and physiological structure-function data. Finally, we provide a novel discussion of how chaperones for LPLs may be considered when extrapolating crystallographic and computational data toward understanding actual biological interactions and phenotypes.

Citing Articles

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