Lysophosphatidic acids (LPAs) are bioactive phospholipids implicated in a wide range of cellular activities They recognize two types of G protein-coupled receptors (LPARs): LPA1-3 receptors and LPA4-6 receptors In recent years, the LPA signaling pathway has captured an increasing amount of attention because of This article provides an extensive review on the current status of ligand development targeting LPA receptors to modulate LPA signaling and their therapeutic potential in various diseases.

all these situations, chemokines interact with seven-transmembrane chemokine-type G protein-coupled receptors (chemokine receptors, CKRs) and glycosaminoglycans (GAGs) to regulate the movement of leukocytes throughout In humans there are approximately 45 chemokines, 19 chemotactic or G-protein coupled chemokine receptors (CKRs) that signal via Gαi and 4 official atypical chemokine receptors (ACKRs) which engage in ligand CCR2 is an example of a dual-function receptor that directly regulates both cell migration and scavenging

The bioactive lysophospholipid sphingosine-1-phosphate (S1P) acts via five different subtypes of S1P receptors Several S1PR therapeutic drugs have been developed to treat these diseases; however, they lack receptor In this article, we describe a 2.2 Å resolution room temperature crystal structure of the human S1P5 receptor demonstrates a unique ligand-binding mode, involving an allosteric sub-pocket, which clarifies the receptor

Lysophosphatidic acid (LPA) is a lipid that activates G protein-coupled receptors (GPCRs), enhancing Our group previously reported that LPA induces production of CCN1 protein in human prostate cancer cell In these cells, the mitogenic activity of LPA is mediated by LPA Receptor 1 (LPAR1), a GPCR. There are multiple examples of the induction of CCN proteins by LPA, and by the related lipid mediator Specifically, CCNs secreted into the extracellular space can facilitate the activation of additional receptors

< GPCR News < GPCRs in Oncology and Immunology The path of GPR87: from a P2Y-like receptor to its role progression Published date December 6, 2024 Abstract "GPR87 is a G protein-coupled seven-transmembrane receptor first described as an orphan receptor in 2001. Despite its high structural homology to several extracellular nucleotide-activated P2Y receptors and Authors Katrin Sak Tags Carcinogenesis , GPR87 , LPA receptor , Metastasis , Orphan GPCR , P2Y receptor

Published date June 26, 2023 Abstract "The functional association between stimulation of G-protein coupled receptors We also observed PTX-dependent TNT biogenesis in response to lysophosphatidic acid (LPA), indicative TNT generation by either 5-oxo-ETE or LPA is partially dependent on the transactivation of the epidermal growth factor receptor (EGFR) and impaired by PI3K inhibition.