September 2022 "Chemerin is the product of the RARRES2 gene which is secreted as a precursor of 143 amino acids. That precursor is inactive, but proteases from the coagulation and fibrinolytic cascades, as well as from inflammatory reactions, process the C-terminus of chemerin to first activate it and then subsequently inactivate it. Chemerin can signal via two G protein-coupled receptors, chem1 and chem2, as well as be bound to a third non-signaling receptor, CCRL2. Chemerin is produced by the liver and secreted into the circulation as a precursor, but it is also expressed in some tissues where it can be activated locally. This review discusses the specific tissue expression of the components of the chemerin system, and the role of different proteases in regulating the activation and inactivation of chemerin. Methods of identifying and determining the levels of different chemerin forms in both mass and activity assays are reviewed. The levels of chemerin in circulation are correlated with certain disease conditions, such as patients with obesity or diabetes, leading to the possibility of using chemerin as a biomarker." Read more at the source #DrGPCR #GPCR #IndustryNews

Significantly, we show that GRKs generate distinct phosphorylation barcodes in intracellular loop 2 ( regulate recruitment of the scaffolding protein β-arrestin 2 (βarr2) to APH1A and γ-secretase-mediated Aβ generation the molecular and structural determinants of the APH1A-βarr2 interaction that critically regulate Aβ generation

March 2022 "Explicyte grants Domain Therapeutics exclusivity on data related to GPCR implicated in immunoresistance, to develop first-in class innovative cancer therapies. Strasbourg and Bordeaux, France, March 10, 2022 – Domain Therapeutics, a biopharmaceutical company specializing in the discovery and development of new drugs targeting G Protein-Coupled Receptors (GPCRs) in immuno-oncology (IO), and Explicyte, an expert in the field of IO and innovative target identification through multiparametric approaches, announce today the signing of a partnership agreement. The two companies will combine their expertise to identify GPCR targets and associated biomarkers to discover and develop breakthrough therapeutic programs for IO. Financial terms are not disclosed." Read more at the source #DrGPCR #GPCR #IndustryNews

Guenter Blobel , before starting my Ph.D. in 2009 at The Scripps Research Institute in La Jolla.

Guenter Blobel , before starting my Ph.D. in 2009 at The Scripps Research Institute in La Jolla.

allosteric modulators has gained attention as they have the potential to fine-tune cellular responses with greater