October 2022 "Protease activated receptors (PARs) are among the first receptors shown to transactivate other receptors: noticeably, these interactions are not limited to members of the same family, but involve receptors as diverse as receptor kinases, prostanoid receptors, purinergic receptors and ionic channels the evidence for PAR interactions with members of their own family, as well as with other types of receptors pathological relevance of these interactions, since this additional level of molecular cross-talk between receptors

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

influence predominantly arises via engagement with the principal two G-protein-coupled cannabinoid receptors Earlier publications have indicated that expression of CB1 receptor mRNA and protein has been recognized The part played by CB1 receptor activation or inhibition with respect to these functions and relevant This can be deduced from the qRT-PCR assays; triggering CB1 receptors amplifies both NR4A1 and NR4A3 The impact of ACEA is inhibited by the selective CB1 receptor antagonist, rimonabant.

< GPCR News < GPCRs in Oncology and Immunology Signaling by Neutrophil G Protein-Coupled Receptors that Neutrophils, which express many receptors that are members of the large family of G protein-coupled receptors The receptors have signaling and functional similarities, although there are also important differences transactivation in the regulation of inflammatory reactions." transactivation Source Contribute to the GPCR News Coming soon Become a Contributor Classified GPCR

< GPCRs in Oncology and Immunology The Effect of Cancer-Associated Mutations on Ligand Binding and Receptor Function - A Case for the 5-HT2C Receptor Published date October 29, 2024 Abstract "The serotonin 5- HT2C receptor is a G protein-coupled receptor (GPCR) mainly expressed in the central nervous system. In this study, we aimed to investigate the effects of cancer patient-derived 5-HT2C receptor mutations on ligand binding and receptor functionality.

Sponsors GPCR Retreat Program < Back to schedule Atypical Structure and Function of Typical Chemokine Receptors of the principal efforts of our laboratory is to understand the physiological consequences of NMDA receptor The NMDA receptor is a subtype of glutamate neurotransmitter receptor that regulates the formation and Our laboratory is interested in the role of NMDA receptors not only on neurons, but also on other cells Our laboratory has a long-standing interest in the way that NMDA receptors contribute to the symptoms