Table 1.
Representative Chemogenetic Technologies
| Name | Protein(s) | Ligand | Reference |
|---|---|---|---|
| Representative kinases | |||
| Allele-specific kinase inhibitors | v-I388G | Compound 3g | Liu et al., 1998 |
| Analogue-sensitive kinases | v-Src (I338G, v-Src-as1), c-Fyn (T339G, c-Fyn-as1), c-Abl (T315A, c-Abl-as2), CAMK IIα (F89G, CAMK IIα-as1) and CDK2 (F80G, CDK2-as1) | K252a and PPI analogues | Bishop et al., 1998 |
| Rapamycin-insensitive TOR complex 2 | TORC2 V2227L | BEZ235 | Bishop et al., 2000 |
| ATP-binding pocket mutations in EphB1, EphB2 and EphB3 | Ephb1T697G, Ephb2T699A, and Ephb3T706A | PP1 analogues | Soskis et al., 2012 |
| ATP-binding pocket mutations of TrkA, TrkB and TrkC | TrkAF592A, TrkBF616A, and TrkCF617A | 1NMPP1 and 1NaPP1 | Chen et al., 2005 |
| Representative Enzymes | |||
| Metalloenzymes | Achiral biotinylated rhodium-diphosphine complexes | Collot et al., 2003 | |
| Engineered transaminases | Chemically conjugating a pyridoxamine moiety within the large cavity of intestinal fatty acid binding protein | Enhanced activity | Häring and Distefano, 2001 |
| Representative GPCRs | |||
| Allele-specific GPCRs | β2-adrenergic receptor, D113S | 1-(3′,4′-dihydroxyphenyl)-3-methyl-L-butanone (L-185,870) | Strader et al., 1991 |
| RASSL-Gi (receptors activated solely by synthetic ligands) | κ-opioid chimeric receptor | Spiradoline | Coward et al., 1998 |
| Engineered GPCRs | 5-HT2A serotonin receptor F340→L340 | Ketanserin analogues | Westkaemper et al., 1999 |
| Gi-DREADD | M2- and M4 mutant muscarinic receptors | Clozapine-N-Oxide | Armbruster and Roth, 2005; Armbruster et al., 2007 |
| Gq-DREADD | M1, M3, and M5- mutant muscarinic receptors | Clozapine-N-oxide | Armbruster and Roth, 2005; Armbruster et al., 2007 |
| Gs-DREADD | Chimeric M3-frog Adrenergic receptor | Clozapine-N-oxide | Guettier et al., 2009 |
| Arrestin-DREADD | M3Dq R165L | Clozapine-N-oxide | Nakajima and Wess, 2012 |
| Axonally-targeted silencing | hM4D-neurexin variant | Clozapine-N-oxide | Stachniak et al., 2014 |
| KORD | κ-opioid receptor D138N mutant | Salvinorin B | Vardy et al., 2015 |
| Representative Channels | |||
| GluCl | Insect Glutmate chloride channel; Y182F mutation | Ivermectin | Lerchner et al., 2007 |
| TrpV1 | TrpV1 in TrpV1 KO mice | capsaicin | Arenkiel et al., 2008 |
| PSAM | Chimeric channels PSAMQ79G,L141S | PSEM9S | Magnus et al., 2011 |
| PSEM | PSAM-GlyR fusions | PSEM89S; PSSEM22S | Magnus et al., 2011 |