7ddz | pdb_00007ddz

The Crystal Structure of Human Neuropeptide Y Y2 Receptor with JNJ-31020028

spinqualitylabelsall models 7ddz, resolution 2.80Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 7ddz is a 1 chain structure with sequence from Desulfovibrio vulgaris str. Hildenborough, Enterobacteria phage RB59 and Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.8Å Ligands: FMN, H46 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function NPY2R_HUMAN Receptor for neuropeptide Y and peptide YY. The rank order of affinity of this receptor for pancreatic polypeptides is PYY > NPY > PYY (3-36) > NPY (2-36) > [Ile-31, Gln-34] PP > [Leu-31, Pro-34] NPY > PP, [Pro-34] PYY and NPY free acid.FLAV_DESVH Low-potential electron donor to a number of redox enzymes. Publication Abstract from PubMed The human neuropeptide Y (NPY) Y(2) receptor (Y(2)R) plays essential roles in food intake, bone formation and mood regulation, and has been considered an important drug target for obesity and anxiety. However, development of drugs targeting Y(2)R remains challenging with no success in clinical application yet. Here, we report the crystal structure of Y(2)R bound to a selective antagonist JNJ-31020028 at 2.8 A resolution. The structure reveals molecular details of the ligand-binding mode of Y(2)R. Combined with mutagenesis studies, the Y(2)R structure provides insights into key factors that define antagonistic activity of diverse antagonists. Comparison with the previously determined antagonist-bound Y(1)R structures identified receptor-ligand interactions that play different roles in modulating receptor activation and mediating ligand selectivity. These findings deepen our understanding about molecular mechanisms of ligand recognition and subtype specificity of NPY receptors, and would enable structure-based drug design. Structural basis for ligand recognition of the neuropeptide Y Y(2) receptor.,Tang T, Hartig C, Chen Q, Zhao W, Kaiser A, Zhang X, Zhang H, Qu H, Yi C, Ma L, Han S, Zhao Q, Beck-Sickinger AG, Wu B Nat Commun. 2021 Feb 2;12(1):737. doi: 10.1038/s41467-021-21030-9. PMID:33531491 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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