8e9x

CryoEM structure of miniGo-coupled hM4Di in complex with DCZ

spinqualitylabelsall models 8e9x, resolution 2.70Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 8e9x is a 5 chain structure with sequence from Homo sapiens and Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: Electron Microscopy, Resolution 2.7Å Ligands: WEC Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function GBB1_HUMAN Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction. Publication Abstract from PubMed Designer receptors exclusively activated by designer drugs (DREADDs) represent a powerful chemogenetic technology for the remote control of neuronal activity and cellular signalling(1-4). The muscarinic receptor-based DREADDs are the most widely used chemogenetic tools in neuroscience research. The G(q)-coupled DREADD (hM3Dq) is used to enhance neuronal activity, whereas the G(i/o)-coupled DREADD (hM4Di) is utilized to inhibit neuronal activity(5). Here we report four DREADD-related cryogenic electron microscopy high-resolution structures: a hM3Dq-miniG(q) complex and a hM4Di-miniG(o) complex bound to deschloroclozapine; a hM3Dq-miniG(q) complex bound to clozapine-N-oxide; and a hM3R-miniG(q) complex bound to iperoxo. Complemented with mutagenesis, functional and computational simulation data, our structures reveal key details of the recognition of DREADD chemogenetic actuators and the molecular basis for activation. These findings should accelerate the structure-guided discovery of next-generation chemogenetic tools. Molecular basis for selective activation of DREADD-based chemogenetics.,Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL Nature. 2022 Dec;612(7939):354-362. doi: 10.1038/s41586-022-05489-0. Epub 2022 , Nov 30. PMID:36450989 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Muscarinic acetylcholine receptor Transducin 3D structures

Proteopedia Page Contributors and Editors (what is this?)

OCA