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Literature summary for 2.7.10.1 extracted from

  • Carey, K.D.; Garton, A.J.; Romero, M.S.; Kahler, J.; Thomson, S.; Ross, S.; Park, F.; Haley, J.D.; Gibson, N.; Sliwkowski, M.X.
    Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib (2006), Cancer Res., 66, 8163-8171.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in NR6 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
DELTA746-750 the in-frame deletion mutant is active but exhibits a higher KM for ATP and a lower Ki for erlotinib relative to the wild-type receptor Homo sapiens
L858R mutant is active but exhibits a higher KM for ATP and a lower Ki for erlotinib relative to the wild-type receptor Homo sapiens
L861Q comparable activity to the wild-type receptor Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
erlotinib
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0011
-
ATP mutant enzyme L861Q Homo sapiens
0.005
-
ATP wild type enzyme Homo sapiens
0.0109
-
ATP mutant enzyme L858R Homo sapiens
0.129
-
ATP deletion mutant enzyme DELTA746-750 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + poly(Glu:Tyr) Homo sapiens
-
ADP + poly(Glu:Tyr) phosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + poly(Glu:Tyr)
-
Homo sapiens ADP + poly(Glu:Tyr) phosphate
-
?

Synonyms

Synonyms Comment Organism
Egfr
-
Homo sapiens
epidermal growth factor receptor tyrosine kinase inhibitor
-
Homo sapiens
erlotinib
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000033
-
erlotinib deletion mutant enzyme DELTA746-750 Homo sapiens
0.00000625
-
erlotinib mutant enzyme L858R Homo sapiens
0.0000175
-
erlotinib wild type enzyme Homo sapiens
0.0000487
-
erlotinib mutant enzyme L861Q Homo sapiens