Wang, Lei published the artcileStructures of the Human PGD2 Receptor CRTH2 Reveal Novel Mechanisms for Ligand Recognition, Safety of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Molecular Cell (2018), 72(1), 48-59.e4, database is CAplus and MEDLINE.
The signaling of prostaglandin D2 (PGD2) through G-protein-coupled receptor (GPCR) CRTH2 is a major pathway in type 2 inflammation. Compelling evidence suggests the therapeutic benefits of blocking CRTH2 signaling in many inflammatory disorders. Currently, a number of CRTH2 antagonists are under clin. investigation, and one compound, fevipiprant, has advanced to phase 3 clin. trials for asthma. Here, we present the crystal structures of human CRTH2 with two antagonists, fevipiprant and CAY10471. The structures, together with docking and ligand-binding data, reveal a semi-occluded pocket covered by a well-structured amino terminus and different binding modes of chem. diverse CRTH2 antagonists. Structural anal. suggests a ligand entry port and a binding process that is facilitated by opposite charge attraction for PGD2, which differs significantly from the binding pose and binding environment of lysophospholipids and endocannabinoids, revealing a new mechanism for lipid recognition by GPCRs.
Molecular Cell published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C25H47NO8, Safety of [(2-Hexylcyclopentylidene)amino]thiourea.
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