October 2022 Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the the iterative optimization of a chemical series culminating in the discovery of the selective CXCR3 antagonist

October 2022 GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches thiophene modification at the C8 position in the common adenine scaffold converted an A2AAR agonist into an antagonist We synthesized and characterized a novel A2AAR antagonist, 2 (LJ-4517), with Ki = 18.3 nM. This approach can expand the repertoire of adenosine receptor antagonists that can be designed based

August 2022 "Chemokines, a subgroup of cytokines along with their receptors, are involved in various biologic processes and regulation of a wide range of immune responses in different physiologic and pathologic states such as tissue repair, infection, and inflammation. C-X-C motif chemokine receptor 4 (CXCR4), a G-protein-coupled receptor (GPCR), has one identified natural ligand termed stromal-derived factor-1(SDF-1 or CXCL12). Evidence demonstrated that the ligation of SDF-1 to CXCR4 initiates several intracellular signaling pathways, regulating cell proliferation, survival, chemotaxis, migration, angiogenesis, adhesion, as well as bone marrow (BM)-resident cells homing and mobilization. Additionally, CXCR4 is expressed by tumor cells in blood malignancies and solid tumors." Read more at the source #DrGPCR #GPCR #IndustryNews

News < GPCRs in Oncology and Immunology Expanding role of CXCR2 and therapeutic potential of CXCR2 antagonists To date, many small-molecule CXCR2 antagonists have entered clinical trials, showing favorable safety pathways, biological functions, structure-activity relationships and clinical significance of CXCR2 antagonists According to the latest development and recent clinical progress of CXCR2 small molecule antagonists, we speculated that CXCR2 can be used as a biomarker and a new target for diabetes and that CXCR2 antagonists

The course will focus on the methods used to quantify GPCR ligand activity (agonists, antagonists, modulators October 10th: Drug Affinity: Measurement of Antagonism (Binding and Function) / Classifying Antagonists

-induced calcium signaling and migration were increased in LPAR1 knockout cells, and LPA1-selective antagonists cell migration toward CXCL12 and alkyl-OMPT was only achieved in the presence of both CXCR4 and LPA1 antagonists inflammatory diseases associated with these receptors, simultaneously raising concerns about the use of LPA1 antagonists