Lysophosphatidic acid (LPA, 1-radyl-2-hydroxy-sn-glycero-3-phosphate) is the prototype
member of a family of lipid mediators and second messengers. LPA and its naturally
occurring analogues interact with G protein-coupled receptors on the cell surface
and a nuclear hormone receptor within the cell. In addition, there are several enzymes
that utilize LPA as a substrate or generate it as a product and are under its regulatory
control. LPA is present in biological fluids, and attempts have been made to link
changes in its concentration and molecular composition to specific disease conditions.
Through their many targets, members of the LPA family regulate cell survival, apoptosis,
motility, shape, differentiation, gene transcription, malignant transformation and
more. The present review depicts arbitrary aspects of the physiological and pathophysiological
actions of LPA and attempts to link them with select targets. Many of us are now convinced
that therapies targeting LPA biosynthesis and signalling are feasible for the treatment
of devastating human diseases such as cancer, fibrosis and degenerative conditions.
However, successful targeting of the pathways associated with this pleiotropic lipid
will depend on the future development of as yet undeveloped pharmacons.