Loading
PDBj
MenuPDBj@FacebookPDBj@X(formerly Twitter)PDBj@BlueSkyPDBj@YouTubewwPDB FoundationwwPDBDonate
RCSB PDBPDBeBMRBAdv. SearchSearch help

7LCI

PF 06882961 bound to the glucagon-like peptide-1 receptor (GLP-1R):Gs complex

Summary for 7LCI
Entry DOI10.2210/pdb7lci/pdb
Related6X1A
EMDB information23274
DescriptorGlucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... (6 entities in total)
Functional Keywordsgpcr, small molecule agonist, membrane protein
Biological sourceHomo sapiens (Human)
More
Total number of polymer chains4
Total formula weight146792.65
Authors
Belousoff, M.J.,Johnson, R.M.,Drulyte, I.,Yu, L.,Kotecha, A.,Danev, R.,Wootten, D.,Zhang, X.,Sexton, P.M. (deposition date: 2021-01-11, release date: 2021-01-20, Last modification date: 2025-06-04)
Primary citationZhang, X.,Johnson, R.M.,Drulyte, I.,Yu, L.,Kotecha, A.,Danev, R.,Wootten, D.,Sexton, P.M.,Belousoff, M.J.
Evolving cryo-EM structural approaches for GPCR drug discovery.
Structure, 29:963-, 2021
Cited by
PubMed Abstract: G protein-coupled receptors (GPCRs) are the largest class of cell surface drug targets. Advances in stabilization of GPCR:transducer complexes, together with improvements in cryoelectron microscopy (cryo-EM) have recently been applied to structure-assisted drug design for GPCR agonists. Nonetheless, limitations in the commercial application of these approaches, including the use of nanobody 35 (Nb35) to aid complex stabilization and the high cost of 300 kV imaging, have restricted broad application of cryo-EM in drug discovery. Here, using the PF 06882961-bound GLP-1R as exemplar, we validated the formation of stable complexes with a modified Gs protein in the absence of Nb35. In parallel, we compare 200 versus 300 kV image acquisition using a Falcon 4 or K3 direct electron detector. Moreover, the 200 kV Glacios-Falcon 4 yielded a 3.2 Å map with clear density for bound drug and multiple structurally ordered waters. Our work paves the way for broader commercial application of cryo-EM for GPCR drug discovery.
PubMed: 33957078
DOI: 10.1016/j.str.2021.04.008
PDB entries with the same primary citation
Experimental method
ELECTRON MICROSCOPY (2.9 Å)
Structure validation

243083

数据于2025-10-15公开中

PDB statisticsPDBj update infoContact PDBjnumon