Cloned (Comment) | Organism |
---|---|
expressed in baculovirus-infected insect cells | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D1994A | kinase-dead mutant | Homo sapiens |
G2019S | the mutation results in a robust enhancement of LRRK2 activity with peptide LRRKtide as the substrate, the mutation also affects binding of ATP to LRRK2 with wild type binding being tighter | Homo sapiens |
I112V | the mutant shows increased activity compared to the wild type enzyme | Homo sapiens |
I2020T | the mutant shows reduced activity compared to the wild type enzyme | Homo sapiens |
R1441C | the mutant shows increased activity compared to the wild type enzyme | Homo sapiens |
Y1699C | the mutant shows increased activity compared to the wild type enzyme | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-{3-[4-(1-Methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl carbamimidothioate | - |
Homo sapiens | |
JAK3 inhibitor VI | - |
Homo sapiens | |
K252a | - |
Homo sapiens | |
staurosporine | - |
Homo sapiens | |
Su-11248 | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.057 | - |
ATP | wild type enzyme | Homo sapiens | |
0.134 | - |
ATP | mutant enzyme G2019S | Homo sapiens |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
204000 | - |
SDS-PAGE | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + peptide LRRKtide | Homo sapiens | high activity towards the peptidic substrate LRRKtide | ADP + phosphorylated peptide LRRKtide | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | LRRK2 undergoes weak autophosphorylation | Homo sapiens |
Purification (Comment) | Organism |
---|---|
FLAG immunoaffinity column chromatography | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + peptide LRRKtide | high activity towards the peptidic substrate LRRKtide | Homo sapiens | ADP + phosphorylated peptide LRRKtide | - |
? |
Synonyms | Comment | Organism |
---|---|---|
leucine-rich repeat kinase 2 | - |
Homo sapiens |
LRRK2 | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000018 | - |
mutant enzyme G2019S | Homo sapiens | staurosporine | |
0.000002 | - |
wild type enzyme | Homo sapiens | staurosporine | |
0.0000028 | - |
mutant enzyme G2019S | Homo sapiens | K252a | |
0.0000036 | - |
wild type enzyme | Homo sapiens | K252a | |
0.000015 | - |
wild type enzyme | Homo sapiens | Su-11248 | |
0.000022 | - |
wild type enzyme | Homo sapiens | JAK3 inhibitor VI | |
0.000026 | - |
mutant enzyme G2019S | Homo sapiens | Su-11248 | |
0.00004 | - |
mutant enzyme G2019S | Homo sapiens | JAK3 inhibitor VI | |
0.001922 | - |
mutant enzyme G2019S | Homo sapiens | 3-{3-[4-(1-Methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl carbamimidothioate | |
0.002671 | - |
wild type enzyme | Homo sapiens | 3-{3-[4-(1-Methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl carbamimidothioate |