Table 4.
hSERT variants | Effect on SERT Activity (versus wild type) | ||||
---|---|---|---|---|---|
Basal | PKG- activation | P38 MAPK-activation | PKC-activation | Surface expression | |
hSERT-WT | 100% | Stimulation | Stimulation | Inhibition | 100% |
Thr4Ala1 | Higher | Insensitive | Insensitive | More-sensitive | Similar to WT |
Gly56Ala1,3*# | Higher | Insensitive | Insensitive | More-sensitive | Similar to WT |
Lys201Asn2 | Higher | NT | NT | NT | Similar to WT |
Glu215Lys1 | Similar to WT | Insensitive | Insensitive | Similar to WT | Similar to WT |
Leu255Met1 | Similar to WT | Similar to WT | Similar to WT | Similar to WT | Similar to WT |
Ser293Phe1 | Higher | Similar to WT | Similar to WT | Similar to WT | Similar to WT |
Pro339Leu1 | Lower | Similar to WT | Similar to WT | Similar to WT | Lower |
Leu362Met1 | Higher | Similar to WT | Similar to WT | Similar to WT | Similar to WT |
Ile425Val11, 4 | Higher | Insensitive | NT | Similar to WT | Similar/higher to WT |
Ile425Leu3 | Higher | Less-sensitive | Less-sensitive | < = Less-sensitive | Higher |
Phe465Leu3* | Higher | Less-sensitive | Less-sensitive | < = Less-sensitive | Higher |
Leu550Val3 | Higher | Less-sensitive | Less-sensitive | < = Less-sensitive | Higher |
Lys605Asn1 | Similar to WT | Insensitive | Insensitive | More-sensitive | Similar to WT |
Pro621Ser1 | Similar to WT | Insensitive | Insensitive | More-sensitive | Similar to WT |
NT: Not tested; < = comparable or slightly reduced sensitivity in comparison with WT;
Less sensitive to PP2 inhibition with calyculin and fostriecin in comparison with WT;
exhibits elevated basal phosphorylation.