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Literature summary for 2.7.10.1 extracted from

  • Mudduluru, G.; Allgayer, H.
    The human receptor tyrosine kinase Axl gene - promoter characterization and regulation of constitutive expression by Sp1, Sp3 and CpG methylation (2008), Biosci. Rep., 28, 161-176.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
5-aza-2'-deoxycytidine demethylation by 5-aza-2'-deoxycytidine upregulates Axl and Sp3 expression in low-Axl-expressing Colo206f/WiDr cells, but not in high-Axl-expressing Rko cells Homo sapiens
additional information exogenous expression of Sp1/Sp3 increases Axl promoter activity Drosophila sp. (in: flies)
additional information two sites (Sp a and Sp b) proximal to the translation start site are indispensable for Axl promoter activity, whereas mutation of three additional upstream motifs (Sp c, Sp d and Sp e) is of additional relevance Homo sapiens

Application

Application Comment Organism
medicine Axl gene expression in cancer cells is constitutively driven by Sp1/Sp3 bound to five core promoter motifs, and is restricted by methylation within/around Sp-binding sites Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information mutation of all motifs abolishes binding of Sp1 and Sp3 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
mithramycin inhibits binding of Sp factors to GC-rich sites, dramatically reduces Axl promoter activity and Axl, Sp1 and Sp3 expression Homo sapiens
siRNA use of Sp1/Sp3 siRNAs significantly reducs Axl promoter activity and protein levels in Rko and HeLa cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Drosophila sp. (in: flies)
-
-
-
Homo sapiens P30530
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HCT-116 cell
-
Homo sapiens
-
HeLa cell
-
Homo sapiens
-
additional information Colo-206F/WiDr cell Homo sapiens
-
additional information SCHNEIDER SL2-cell Drosophila sp. (in: flies)
-
RKO cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
Axl
-
Drosophila sp. (in: flies)
Axl
-
Homo sapiens
receptor tyrosine kinase
-
Drosophila sp. (in: flies)
receptor tyrosine kinase
-
Homo sapiens