Literature summary for 2.7.10.2 extracted from

Williams, N.K.; Lucet, I.S.; Klinken, S.P.; Ingley, E.; Rossjohn, J.
Crystal structures of the Lyn protein tyrosine kinase domain in its apo- and inhibitor-bound state (2009), J. Biol. Chem., 284, 284-291.

Search for more literature for 2.7.10.2

Activating Compound

Activating Compound	Comment	Organism	Structure
additional information	phosphorylation of Tyr397 in Lyn results in activation of the enzyme	Mus musculus

Application

Application	Comment	Organism
medicine	Lyn kinase inhibitors are becoming an increasingly important class of chemotherapeutic agents	Mus musculus

Cloned(Commentary)

Cloned (Comment)	Organism
the murine Lyn kinase domain, amino acids 239-512, is subcloned into the baculovirus expression vector pFastBacHTA generating a His6-tagged fusion resulting in a 5 amino acid N-terminal extension to the Lyn kinase domain after tobacco etch virus cleavage	Mus musculus

Crystallization (Commentary)

Crystallization (Comment)	Organism
the crystal structures of the kinase domain of Lyn are determined in complex with three different inhibitors, AMP-PNP, 4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine and dasatinib, as well as the non-liganded form of the enzyme, at 2.5 to 2.7 A resolution	Mus musculus

Inhibitors

Inhibitors	Comment	Organism	Structure
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine	PP2, AG-1897	Mus musculus
AMP-PNP	-	Mus musculus
dasatinib	-	Mus musculus
additional information	phosphorylation of Tyr508 in Lyn inhibits activity of the enzyme	Mus musculus
SU6656	-	Mus musculus

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
membrane	-	Mus musculus	16020	-

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	-	Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + [protein]-L-tyrosine	Mus musculus	-	ADP + [protein]-L-tyrosine phosphate	-	?

Organism

Organism	UniProt	Comment	Textmining
Mus musculus	-	-	-

Purification (Commentary)

Purification (Comment)	Organism
using nickel-chelating resin, a HiTrap Q column and gel filtration	Mus musculus

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + Cbp	murine Csk binding protein, Cbp, amino acids 74-474, substrate used in kinase activity assay	Mus musculus	? + ADP	-	?
ATP + [protein]-L-tyrosine	-	Mus musculus	ADP + [protein]-L-tyrosine phosphate	-	?

Synonyms

Synonyms	Comment	Organism
Lyn protein tyrosine kinase	-	Mus musculus

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
30	-	kinase assay	Mus musculus

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.4	-	kinase assay	Mus musculus

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Mus musculus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000009	-	substrate Csk binding protein, Cbp	Mus musculus	4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
0.000011	-	substrate Csk binding protein, Cbp	Mus musculus	dasatinib
0.000035	-	substrate Csk binding protein, Cbp	Mus musculus	SU6656

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Release 2023.1 (January 2023)