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Literature summary for 2.7.10.2 extracted from

  • Szigligeti, P.; Neumeier, L.; Duke, E.; Chougnet, C.; Takimoto, K.; Lee, S.M.; Filipovich, A.H.; Conforti, L.
    Signalling during hypoxia in human T lymphocytes - critical role of the src protein tyrosine kinase p56Lck in the O2 sensitivity of Kv1.3 channels (2006), J. Physiol., 573, 357-370.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
EPQYEEIPIYL a src kinase activating peptide, binds to the SH2 domain of the src-kinase and activates it, activation of endogenous src-PTKs does not inhibit Kv1.3 channels in T lymphocytes, overview Homo sapiens
additional information activation of Lck by prolonged hypoxia leading to increased phosphorylation of Kv1.3 channels Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
delivery of active Lck into L929 cells and overexpression of GFP-tagged Y505FLck do not decrease recombinant Kv1.3 currents, on the contrary, activation of endogenous src kinases increase wild-type Kv1.3 currents in T lymphocytes, overview Homo sapiens

Protein Variants

Protein Variants Comment Organism
Y505F constitutively active Lck mutant, effect on recombinant Kv1.3 current amplitude and O2 sensitivity, overexpressing LckY505F decreased Kv1.3 current from 2.5±0.3 nA to 2.2±0.2 nA, overview Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine i.e. PP2, abolishes the hypoxia-induced inhibition of Kv1.3 channels in primaryhumanT lymphocytes Homo sapiens
Hg2+ at PO2 of about 20 mM Homo sapiens
additional information no inhibition by 4-amino-7-phenylpyrazolo[3,4-d] pyrimidine, i.e. PP3 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens the Src protein tyrosine kinase p56Lck plays a critical role in the O2 sensitivity of Kv1.3 channels and in signalling during hypoxia in T lymphocytes, overview ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
J.CaM1.6 cell
-
Homo sapiens
-
T-lymphocyte primary, CD4+ and CD3+ lymphocytes Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the Src protein tyrosine kinase p56Lck plays a critical role in the O2 sensitivity of Kv1.3 channels and in signalling during hypoxia in T lymphocytes, overview Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
Lck
-
Homo sapiens
p56lck
-
Homo sapiens
src protein tyrosine kinase p56Lck
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens