- Institution: Stanford Univ Med Ctr Lane Med Lib/Periodical Dept/Rm L109
- Sign In as Member / Individual
REGULATORs OF G PROTEIN SIGNALING & DRUGS OF ABUSE
Table 1.
Mammalian RGS Proteins
| RGS family | Domains present | RGS1 | G protein specificity | References to Drugs of Abuse2 |
|---|---|---|---|---|
| 1Alternative names are given in parentheses. | ||||
| 2RGS-insensitive mutants of Gαo are used in references 26, 87, and 88. | ||||
| 3RGS3 is much larger than other members of the R4 family and has multiple splice variants, some of which include a PDZ domain. | ||||
| 4RGS12 has a splice variant with N-terminal PDZ and PTB domains and interacts with N-type calcium channels. | ||||
| 5Rho GEF RH domains have GAP activity toward Gα12, Gα13, and Gαq, but their primary function appears to be as effectors, not inhibitors, of signaling. | ||||
| 6GRK2 and GRK3 only. | ||||
| Abbreviations: D-AKAP2, dual-specificity A-kinase-anchoring protein 2; GAIP, Gα-interacting protein; GEF, guanine-nucleotide-exchange factor; GRK, G-protein receptor kinase; LARG, leukaemia-associated RhoGEF; PDZ, PSD95/Dlg/Z0-1 domain; RGS, regulator of G-protein signaling; R9AP, R9-associated protein; R7PB, R7 binding protein; SNX, sorting nexin. | ||||
| Classical RGS – known Gα binding, GAP activity, and functional inhibition | ||||
| RZ | Cysteine-string | RGS19 (GAIP) | Gi Gz Gq | |
| RGS17 (RGS Z2) | Gi Gz Gq | |||
| RGS20 RGS Z1) | Gi, Gz | 86 | ||
| R4 | N-terminal amphipathic sequence | RGS1 | Gi Gq | |
| RGS4 | Gi Gq | 69,78,79,80, 29, 95, 86 | ||
| RGS2 | Gq»Gi | 34,68,69,70,85,86 | ||
| RGS33 | Gi Gq | 68,70,86 | ||
| RGS5 | Gi Gq | 68,70 | ||
| RGS8 | Gi Gq | |||
| RGS13 | ND | |||
| RGS16 | Gi Gq | |||
| RGS18 | Gi Gq | 86 | ||
| RGS21 | Gi Gq | |||
| R7 | GGL–(Gβ5) DEP–(R9AP, R7BP) | RGS9 | Go | 29,68,69,82,86 |
| RGS7 | Goα > Giα2 > Giα1 | |||
| RGS11 | Go | 86 | ||
| RGS6 | Go | 86 | ||
| R12 | GoLoco–(Gα-GDP) RBD–(rap) PDZ | RGS124 | Gi | |
| RGS14 | Gi | |||
| RGS10 | Gi | |||
| RGS Homology – Gα binding | ||||
| RhoGEF5 | DH/PH–(Rho exchange factor activity) | p115RhoGEF | G12, G13 | |
| LARG G12 | G12, Gq | |||
| PDZRhoGEF | G13 | |||
| GRK | GRK (receptor kinase) PH+ (βγbinding)6 | GRK2 | Gq | |
| GRK3 | Gq | |||
| GRK1 | ND | |||
| GRK4 | ND | |||
| GRK5 | ND | |||
| GRK6 | ND | |||
| GRK7 | ND | |||
| RGS Homology (RH) – Gα actions unknown | ||||
| Axin | RH domain binds APC (β-catenin, GSK-3, Wnt signaling) | Axin | ND | |
| Axil | ND | |||
| AKAP | AKAP PDZ | D-AKAP2 | ND | |
| SNX | PX | SNX13 | ? Gs | |
| SNX14 | ? Gs | |||
| SNX25 | ? Gs | |||
