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Literature summary for 2.7.10.1 extracted from

  • Varkondi, E.; Schaefer, E.; Boekoenyi, G.; Gyoekeres, T.; Oerfi, L.; Petak, I.; Pap, A.; Szokoloczi, O.; Keri, G.; Schwab, R.
    Comparison of ELISA-based tyrosine kinase assays for screening EGFR inhibitors (2005), J. Recept. Signal Transduct. Res., 25, 45-56.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of EGFR-TK in Spodoptera frugiperda Sf9 cells using the baculovirus infection system Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
gefitinib specific inhibition of EGFR-TK Homo sapiens
PD153035 specific inhibition of EGFR-TK, IC50 is 0.00329 mM with 1 U of purified EGFR-TK from A431 cells Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetics of wild-type EGFR-TK from A431 cells and recombinant EGFR-TK from Sf9 cells Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
EGFR-TK from A431 cells by affinity chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
A-431 cell
-
Homo sapiens
-
brain tumor cell overexpression of EGFR-TK Homo sapiens
-
breast cancer cell overexpression of EGFR-TK Homo sapiens
-
colonic cancer cell overexpression of EGFR-TK Homo sapiens
-
lung cancer cell overexpression of EGFR-TK Homo sapiens
-
ovarian cancer cell overexpression of EGFR-TK Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
development of a specific ELISA-based phosphotyrosine detection Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a [protein]-L-tyrosine
-
Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
?
ATP + [poly-(Glu,Tyr)1:4] synthetic substrate Homo sapiens ADP + [poly-(Glu,Tyr)1:4]-tyrosine phosphate
-
?

Synonyms

Synonyms Comment Organism
EGFR tyrosine kinase
-
Homo sapiens
EGFR-TK
-
Homo sapiens
epidermal growth factor receptor tyrosine kinase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00329
-
specific inhibition of EGFR-TK, IC50 is 0.00329 mM with 1 U of purified EGFR-TK from A431 cells Homo sapiens PD153035