G protein-coupled receptors (GPCRs) are cell-surface receptors mediating the responses of 2/3rds of human hormones1 and 1/3rd of drugs2. Each GPCR can bind several transducers, G proteins, GPCR kinases (GRKs) and arrestins leading to distinct intracellular signaling networks and functional outcomes.
- 423 Human proteins
- 42,617 Species orthologs
- 69,602 Genetic variants
- 974 Drugs
- 174 Drug targets
- 411 Disease indications
- 213,447 Ligands
- 531 Endogenous ligands
- 468,052 Ligand bioactivities
- 34,650 Ligand site mutations
- 43,446 Ligand interactions
- 988 GPCRs structures
- 844 GPCRs structure models
- 2,924 Generic residues
- 765 Refined structures
Latest releaseMarch 9, 2023
- 195 new structures added (up until December 2022)
- New automated structure segment annotation based on DSSP and custom rules
- New interaction calculation process using RDKit for higher precision and accuracy
- Van der Waals interactions added
- Class C activation state reverted to author based annotation instead of degree active calculation
- New API calls for ligand data
- Hydrogen atoms removed from AlphaFold models
- GPCR - G protein interface interactions figures are now downloadable
- Structure annotation fixes
- Minor bug and performance fixes
GPCRdb in 2023: State-specific structure models using AlphaFold2 and expansion of ligand resources.
Pándy-Szekeres, G., Caroli, J., Mamyrbekov, A., Kermani, A.A., Keserű, G.M., Kooistra, A.J. and Gloriam, D.E.
Nucleic Acids Research, 2023
GPCRdb in 2021: integrating GPCR sequence, structure and function.
Kooistra AJ, Mordalski S, Pandy-Szekeres G, Esguerra M, Mamyrbekov A, Munk C, Keseru GM, Gloriam DE
Nucleic acids research, 2021, 49:D335-D343
Structure of the class D GPCR Ste2 dimer coupled to two G proteins.
Velazhahan V, Ma N, Pandy-Szekeres G, Kooistra AJ, Lee Y, Gloriam DE, Vaidehi N, Tate CG
Nature, 2021, 589:148-153
An online GPCR structure analysis platform.
Kooistra AJ, Munk C, Hauser AS, Gloriam DE
Nature structural & molecular biology, 2021, 28:875-878
Combinatorial expression of GPCR isoforms affects signalling and drug responses.
Marti-Solano M, Crilly SE, Malinverni D, Munk C, Harris M, Pearce A, Quon T, Mackenzie AE, Wang X, Peng J, Tobin AB, Ladds G, Milligan G, Gloriam DE, Puthenveedu MA, Babu MM
Nature, 2020, 587:650-656
An online resource for GPCR structure determination and analysis.
Munk C, Mutt E, Isberg V, Nikolajsen LF, Bibbe JM, Flock T, Hanson MA, Stevens RC, Deupi X, Gloriam DE
Nature methods, 2019, 16:151-162