Literature summary for 2.7.11.1 extracted from

Anand, V.S.; Reichling, L.J.; Lipinski, K.; Stochaj, W.; Duan, W.; Kelleher, K.; Pungaliya, P.; Brown, E.L.; Reinhart, P.H.; Somberg, R.; Hirst, W.D.; Riddle, S.M.; Braithwaite, S.P.
Investigation of leucine-rich repeat kinase 2: enzymological properties and novel assays (2009), FEBS J., 276, 466-478.

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Cloned(Commentary)

Cloned (Comment)	Organism
expressed in baculovirus-infected insect cells	Homo sapiens

Protein Variants

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

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 [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 [Da]	Molecular Weight Maximum [Da]	Comment	Organism
204000	-	SDS-PAGE	Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
phosphoprotein	LRRK2 undergoes weak autophosphorylation	Homo sapiens

Purification (Commentary)

Purification (Comment)	Organism
FLAG immunoaffinity column chromatography	Homo sapiens

Substrates and Products (Substrate)

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

Synonyms	Comment	Organism
leucine-rich repeat kinase 2	-	Homo sapiens
LRRK2	-	Homo sapiens

IC50 Value

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

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Release 2023.1 (January 2023)