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Literature summary extracted from

  • Gargala, G.; Baishanbo, A.; Favennec, L.; Francois, A.; Ballet, J.J.; Rossignol, J.F.
    Inhibitory activities of epidermal growth factor receptor tyrosine kinase-targeted dihydroxyisoflavone and trihydroxydeoxybenzoin derivatives on Sarcocystis neurona, Neospora caninum, and Cryptosporidium parvum development (2005), Antimicrob. Agents Chemother., 49, 4628-4634.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.7.10.1 drug development the enzyme is a target for development of anticoccidial agents such as genistein analogues Cryptosporidium parvum
2.7.10.1 drug development the enzyme is a target for development of anticoccidial agents such as genistein analogues Neospora caninum
2.7.10.1 drug development the enzyme is a target for development of anticoccidial agents such as genistein analogues Sarcocystis neurona

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.10.1 2,4,6-trihydroxydeoxybenzoin derivatives diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview Cryptosporidium parvum
2.7.10.1 2,4,6-trihydroxydeoxybenzoin derivatives diverse derivatives, analysis of inhibitory effect on EGFR tyrosine kinase activity, overview Homo sapiens
2.7.10.1 2,4,6-trihydroxydeoxybenzoin derivatives diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview Neospora caninum
2.7.10.1 2,4,6-trihydroxydeoxybenzoin derivatives diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview Sarcocystis neurona
2.7.10.1 5,7-dihydroxyisoflavone derivatives diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview Cryptosporidium parvum
2.7.10.1 5,7-dihydroxyisoflavone derivatives diverse derivatives, analysis of inhibitory effect on EGFR tyrosine kinase activity, overview Homo sapiens
2.7.10.1 5,7-dihydroxyisoflavone derivatives diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview Neospora caninum
2.7.10.1 5,7-dihydroxyisoflavone derivatives diverse derivatives, analysis of inhibitory effect on parasite infection of host cells BM and HCT-8, IC50 values, overview Sarcocystis neurona
2.7.10.1 genistein
-
 Cryptosporidium parvum
2.7.10.1 genistein
-
 Neospora caninum
2.7.10.1 genistein
-
 Sarcocystis neurona
2.7.10.1 RM-6427 inhibits parasite infection of host cells BM and HCT-8 Cryptosporidium parvum
2.7.10.1 RM-6427 inhibits parasite infection of host cells BM and HCT-8 Neospora caninum
2.7.10.1 RM-6427 inhibits parasite infection of host cells BM and HCT-8 Sarcocystis neurona
2.7.10.1 RM-6428 inhibits parasite infection of host cells BM and HCT-8 Cryptosporidium parvum
2.7.10.1 RM-6428 inhibits parasite infection of host cells BM and HCT-8 Neospora caninum
2.7.10.1 RM-6428 inhibits parasite infection of host cells BM and HCT-8 Sarcocystis neurona

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.10.1 cell membrane
-
 Homo sapiens
-
-
2.7.10.1 plasma membrane
-
 Cryptosporidium parvum 5886
-
2.7.10.1 plasma membrane
-
 Meriones unguiculatus 5886
-
2.7.10.1 plasma membrane
-
 Neospora caninum 5886
-
2.7.10.1 plasma membrane
-
 Sarcocystis neurona 5886
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.10.1 ATP + a [protein]-L-tyrosine Homo sapiens
-
 ADP + a [protein]-L-tyrosine phosphate
-
 ?
2.7.10.1 ATP + a [protein]-L-tyrosine Meriones unguiculatus
-
 ADP + a [protein]-L-tyrosine phosphate
-
 ?
2.7.10.1 additional information Cryptosporidium parvum EGF-like peptides bind as ligands to the extracellular domain of host cell EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade ?
-
 ?
2.7.10.1 additional information Sarcocystis neurona EGF-like peptides bind as ligands to the extracellular domain of host cell EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade ?
-
 ?
2.7.10.1 additional information Meriones unguiculatus EGF-like peptides on the surface of coccidial parasites Sarcocystis neurona, Neospora caninum, and Cryptosporidium parvum bind as ligands to the extracellular domain of the gerbils' host cells' EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.10.1 Cryptosporidium parvum
-
 grown in bovine BM and HCT-8 cells, parasite contains membrane proteins with EGF-like extracellular domains
-
2.7.10.1 Homo sapiens
-
-
-
2.7.10.1 Meriones unguiculatus
-
 Mongolian gerbil
-
2.7.10.1 Neospora caninum
-
 grown in bovine BM and HCT-8 cells, parasite contains membrane proteins with EGF-like extracellular domains
-
2.7.10.1 Sarcocystis neurona
-
 grown in bovine BM and HCT-8 cells, parasite contains membrane proteins with EGF-like extracellular domains
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.10.1 A-431 cell
-
 Homo sapiens
-
2.7.10.1 merozoite
-
 Cryptosporidium parvum
-
2.7.10.1 merozoite
-
 Neospora caninum
-
2.7.10.1 merozoite
-
 Sarcocystis neurona
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.10.1 ATP + a [protein]-L-tyrosine
-
 Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?
2.7.10.1 ATP + a [protein]-L-tyrosine
-
 Meriones unguiculatus ADP + a [protein]-L-tyrosine phosphate
-
 ?
2.7.10.1 ATP + poly(Glu-Ala-Tyr)
-
 Homo sapiens ADP + poly(Glu-Ala-Tyr)-L-tyrosine phosphate
-
 ?
2.7.10.1 additional information EGF-like peptides bind as ligands to the extracellular domain of host cell EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade Cryptosporidium parvum ?
-
 ?
2.7.10.1 additional information EGF-like peptides bind as ligands to the extracellular domain of host cell EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade Neospora caninum ?
-
 ?
2.7.10.1 additional information EGF-like peptides bind as ligands to the extracellular domain of host cell EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade Sarcocystis neurona ?
-
 ?
2.7.10.1 additional information EGF-like peptides on the surface of coccidial parasites Sarcocystis neurona, Neospora caninum, and Cryptosporidium parvum bind as ligands to the extracellular domain of the gerbils' host cells' EGFR leading to an activation of the intracellular tyrosine kinase domain which initiates downstream signaling pathways, e.g. the mitogen-activated protein kinase cascade Meriones unguiculatus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.10.1 EGF TK
-
 Homo sapiens
2.7.10.1 EGFR protein tyrosine kinase
-
 Homo sapiens
2.7.10.1 EGFR protein tyrosine kinase
-
 Meriones unguiculatus
2.7.10.1 EGFR PTK
-
 Meriones unguiculatus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.10.1 37
-
 in vivo inhibition assay at Cryptosporidium parvum
2.7.10.1 37
-
 in vivo inhibition assay at Neospora caninum
2.7.10.1 37
-
 in vivo inhibition assay at Sarcocystis neurona

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.10.1 ATP
-
 Homo sapiens
2.7.10.1 ATP
-
 Meriones unguiculatus