4mqe | pdb_00004mqe

Crystal structure of the extracellular domain of human GABA(B) receptor in the apo form

spinqualitylabelsall models 4mqe, resolution 2.35Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4mqe is a 2 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: NAG, FUC, MAN Related: 4mqf, 4mr7, 4mr8, 4mr9, 4mrm, 4ms1, 4ms3, 4ms4 Gene: GABBR1, GPRC3A (HUMAN), GABBR2, GPR51, GPRC3B (HUMAN) Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed Human GABA(B) (gamma-aminobutyric acid class B) receptor is a G-protein-coupled receptor central to inhibitory neurotransmission in the brain. It functions as an obligatory heterodimer of the subunits GBR1 and GBR2. Here we present the crystal structures of a heterodimeric complex between the extracellular domains of GBR1 and GBR2 in the apo, agonist-bound and antagonist-bound forms. The apo and antagonist-bound structures represent the resting state of the receptor; the agonist-bound complex corresponds to the active state. Both subunits adopt an open conformation at rest, and only GBR1 closes on agonist-induced receptor activation. The agonists and antagonists are anchored in the interdomain crevice of GBR1 by an overlapping set of residues. An antagonist confines GBR1 to the open conformation of the inactive state, whereas an agonist induces its domain closure for activation. Our data reveal a unique activation mechanism for GABA(B) receptor that involves the formation of a novel heterodimer interface between subunits. Structural mechanism of ligand activation in human GABA(B) receptor.,Geng Y, Bush M, Mosyak L, Wang F, Fan QR Nature. 2013 Dec 12;504(7479):254-9. doi: 10.1038/nature12725. Epub 2013 Dec 4. PMID:24305054 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

Proteopedia Page Contributors and Editors (what is this?)

OCA