G protein coupling datasets deposited in GproteinDb
In addition to the subtype-level couplings, GproteinDb includes family-level couplings from the Guide to Pharmacology database (1). Biosensors are described in the Biosensors page.
| Lab | Biosensor | Parameter | Year | Ref | #Rec |
#wt Gprots tested |
Gs | Gi/o | Gq/11 | G12/13 |
Year added |
Note | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| GsS | GsL | Golf | Gi1 | Gi2 | Gi3 | GoA | GoB | Gz | Ggust | Gq | G11 | G14 | G15 | G12 | G13 | |||||||||
| Bouvier | EMTA / GEMTA | log(Emax/EC50) | 2022 | (2) | 100 | 12 | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | 2022 | |||||
| Inoue | NanoBiT-G | log(Emax/EC50) | 2019 | (3) | 8 | 8 | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | 2024 | |||||||||
| Inoue | TGFα-shedding | log(Emax/EC50) | 2019 | (3) | 150 | 1* | ✓ | 2022 | *Only Gq is wt/used |
|||||||||||||||
| Lambert | RGB-GDP | Efficacy | - | Unp | 14 | 6 | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | 2024 | Adhesions | ||||||||||
| Lambert | RGB-GDP | Econst., Efficacy | - | Unp | 8 | 4 | ✓ | ✓ | ✓ | ✓ | 2024 | |||||||||||||
| Lambert | RGB-GDP | Econst., Efficacy | 2019 | (4) | 16 | 4 | ✓ | ✓ | ✓ | ✓ | 2024 | |||||||||||||
| Lambert | RGB-GDP | Econst., Efficacy | 2020 | (5) | 3 | 4 | ✓ | ✓ | ✓ | ✓ | 2024 | |||||||||||||
| Lambert | RGB-GDP | Econst. | 2021 | (6) | 49 | 5 | ✓ | ✓ | ✓ | ✓ | ✓ | 2024 | Orphans | |||||||||||
| Martemyanov | FReeβγ-Nluc | Activation rate (s-1) | 2023 | (7) | 117 | 5 | ✓ | ✓ | ✓ | ✓ | ✓ | 2024 | ||||||||||||
| Roth | TRUPATH | log(Emax/EC50) | 2020 | (8) | 4 | 15 | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | ✓ | 2022 | ||
References
1. Harding, S.D., Armstrong, J.F., Faccenda, E., Southan, C., Alexander, S.P.H., Davenport, A.P., Pawson, A.J., Spedding, M., Davies, J.A. and Nc, I. (2022) The IUPHAR/BPS guide to PHARMACOLOGY in 2022: curating pharmacology for COVID-19, malaria and antibacterials. Nucleic Acids Res., 50, D1282-D1294.
2. Avet, C., Mancini, A., Breton, B., Le Gouill, C., Hauser, A.S., Normand, C., Kobayashi, H., Gross, F., Hogue, M., Lukasheva, V. et al. (2022) Effector membrane translocation biosensors reveal G protein and betaarrestin coupling profiles of 100 therapeutically relevant GPCRs. Elife, 11, 2020.2004.2020.052027.
3. Inoue, A., Raimondi, F., Kadji, F.M.N., Singh, G., Kishi, T., Uwamizu, A., Ono, Y., Shinjo, Y., Ishida, S., Arang, N. et al. (2019) Illuminating G-Protein-Coupling Selectivity of GPCRs. Cell, 177, 1933-1947 e1925.
4. Okashah, N., Wan, Q., Ghosh, S., Sandhu, M., Inoue, A., Vaidehi, N. and Lambert, N.A. (2019) Variable G protein determinants of GPCR coupling selectivity. Proceedings of the National Academy of Sciences, 116, 12054-12059.
5. Okashah, N., Wright, S.C., Kawakami, K., Mathiasen, S., Zhou, J., Lu, S., Javitch, J.A., Inoue, A., Bouvier, M. and Lambert, N.A. (2020) Agonist-induced formation of unproductive receptor-G12 complexes. Proceedings of the National Academy of Sciences of the United States of America, 117, 21723-21730.
6. Lu, S., Jang, W., Inoue, A. and Lambert, N.A. (2021) Constitutive G protein coupling profiles of understudied orphan GPCRs. PLoS One, 16, e0247743.
7. Masuho, I., Kise, R., Gainza, P., Von Moo, E., Li, X., Tany, R., Wakasugi-Masuho, H., Correia, B.E. and Martemyanov, K.A. (2023) Rules and mechanisms governing G protein coupling selectivity of GPCRs. Cell reports, 42, 113173.
8. Olsen, R.H.J., DiBerto, J.F., English, J.G., Glaudin, A.M., Krumm, B.E., Slocum, S.T., Che, T., Gavin, A.C., McCorvy, J.D., Roth, B.L. and Strachan, R.T. (2020) TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome. Nat. Chem. Biol., 16, 841-849.