Towards selective lysophospholipid GPCR modulators

Archbold, Julia K., Martin, Jennifer L. and Sweet, Matthew J. (2014) Towards selective lysophospholipid GPCR modulators. Trends in Pharmacological Sciences, 35 5: 219-226. doi:10.1016/

Author Archbold, Julia K.
Martin, Jennifer L.
Sweet, Matthew J.
Title Towards selective lysophospholipid GPCR modulators
Journal name Trends in Pharmacological Sciences   Check publisher's open access policy
ISSN 1873-3735
Publication date 2014-05-01
Year available 2014
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1016/
Open Access Status Not yet assessed
Volume 35
Issue 5
Start page 219
End page 226
Total pages 8
Place of publication Kidlington, Oxford, United Kingdom
Publisher Elsevier
Language eng
Subject 3004 Pharmacology
3005 Toxicology
Abstract G-protein-coupled receptors (GPCRs) that recognize the lysophospholipids (LPLs) are grouped into two phylogenetically distinct families: the endothelial differentiation gene (Edg) and non-Edg GPCRs. Owing to their more recent identification, and hindered by a lack of selective pharmacological tools, our understanding of the functions and signaling pathways of the non-Edg GPCRs is still in its infancy. Targeting the non-conserved allosteric binding sites of the LPL GPCRs shows particular promise for the development of selective modulators by structure-based drug design. However, only one Edg GPCR (S1PR1) structure has been determined to date, and it has low sequence identity with the non-Edg GPCRs (<20%). Thus, a representative structure of a non-Edg GPCR remains a pressing objective for selective structure-based drug design. Obtaining selective modulators targeting the non-Edg receptors would help to unravel the biology behind these novel GPCRs and potentially will support therapeutic treatment of diseases such as cancer, inflammation, and neuropsychiatric disorders.
Keyword Endothelial-derived growth factor (Edg)
G-protein-coupled receptors (GPCRs)
GPCR structure
Lysophosphatidic acid (LPA)
Q-Index Code C1
Q-Index Status Confirmed Code
Grant ID APP606728
Institutional Status UQ

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: Official 2015 Collection
Institute for Molecular Bioscience - Publications
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