7joz

Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist

spinqualitylabelsall models 7joz, resolution 3.80Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 7joz is a 5 chain structure with sequence from Escherichia virus T4, Homo sapiens and Lama glama. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 3.8Å Ligands: 1PE, VFP Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Publication Abstract from PubMed Dopamine D1 receptor (D1R) is an important drug target implicated in many psychiatric and neurological disorders. Selective agonism of D1R are sought to be the therapeutic strategy for these disorders. Most selective D1R agonists share a dopamine-like catechol moiety in their molecular structure, and their therapeutic potential is therefore limited by poor pharmacological properties in vivo. Recently, a class of non-catechol D1R selective agonists with a distinct scaffold and pharmacological properties were reported. Here, we report the crystal structure of D1R in complex with stimulatory G protein (Gs) and a non-catechol agonist Compound 1 at 3.8 A resolution. The structure reveals the ligand bound to D1R in an extended conformation, spanning from the orthosteric site to extracellular loop 2 (ECL2). Structural analysis reveals that the unique features of D1R ligand binding pocket explains the remarkable selectivity of this scaffold for D1R over other aminergic receptors, and sheds light on the mechanism for D1R activation by the non-catechol agonist. Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist.,Sun B, Feng D, Chu ML, Fish I, Lovera S, Sands ZA, Kelm S, Valade A, Wood M, Ceska T, Kobilka TS, Lebon F, Kobilka BK Nat Commun. 2021 Jun 3;12(1):3305. doi: 10.1038/s41467-021-23519-9. PMID:34083522 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Dopamine receptor 3D structures GTP-binding protein 3D structures Transducin 3D structures

Proteopedia Page Contributors and Editors (what is this?)

OCA