Analysis Affinity of Shingosine-1-Phosphate (S1P) and lysophosphatidic Acid (LPA) by KinExA (CAT#: STEM-MB-0024-CJ)

Introduction

Sphingosine-1-phosphate (S1P) and lysophosphatidic acid (LPA) are bioactive lysophospholipids that bind and signal through multiple G protein-coupled receptors (GPCRs). Many physiological processes, such as cell growth, differentiation, survival, motility, and angiogenesis, and pathophysiological processes, such as cancer, cardiovascular disease, multiple sclerosis, neuropathic pain, and fibrosis, involve S1P or LPA signaling. The S1P and LPA pathways are validated therapeutic targets; many drugs and pharmacological agents have been developed to modulate the activity of receptors and enzymes in these pathways. Many of these compounds block circulating S1P and LPA from binding and activating cognate membrane-bound receptors. In blood, LPA also exists bound to carrier proteins, primarily serum albumin. Total LPA in plasma comprises several distinct species, which contain esterified fatty acids with varying numbers of carbon atoms and cis double bonds capable of activating cognate GPCRs with varying potencies. Although albumin is the most abundant protein in human plasma and LPA is one of the first bioactive lipids identified, the stoichiometry and mechanism of interaction between these two molecules is poorly understood.