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Literature summary for 2.4.1.122 extracted from

  • Lin, M.C.; Chien, P.H.; Wu, H.Y.; Chen, S.T.; Juan, H.F.; Lou, P.J.; Huang, M.C.
    C1GALT1 predicts poor prognosis and is a potential therapeutic target in head and neck cancer (2018), Oncogene, 37, 5780-5793 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.4.1.122

Application

Application Comment Organism
diagnostics C1GALT1 predicts poor prognosis and is a potential therapeutic target in head and neck cancer Homo sapiens
medicine C1GALT1 predicts poor prognosis and is a potential therapeutic target in head and neck cancer Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
itraconazole itraconazole is a C1GALT1 inhibitor that directly binds C1GALT1 and promotes its proteasomal degradation, leading to significant blockade of C1GALT1-mediated effects in HNSCC cells in vitro and in vivo Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
UDP-alpha-D-galactose + N-acetyl-alpha-D-galactosaminyl-epidermal growth factor receptor Homo sapiens
-
 UDP + beta-D-galactosyl-(1->3)-N-acetyl-alpha-D-galactosaminyl-epidermal growth factor receptor
-
 ?
UDP-alpha-D-galactose + N-acetyl-alpha-D-galactosaminyl-R Homo sapiens
-
 UDP + beta-D-galactosyl-(1->3)-N-acetyl-alpha-D-galactosaminyl-R
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NS00
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
additional information itraconazole is a C1GALT1 inhibitor that directly binds C1GALT1 and promotes its proteasomal degradation, leading to significant blockade of C1GALT1-mediated effects in HNSCC cells in vitro and in vivo Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
head and neck squamous cell carcinoma cell C1GALT1 expression is upregulated in HNSCC tumors Homo sapiens
-
additional information C1GALT1 is overexpressed in various human malignancies Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-alpha-D-galactose + N-acetyl-alpha-D-galactosaminyl-epidermal growth factor receptor
-
 Homo sapiens UDP + beta-D-galactosyl-(1->3)-N-acetyl-alpha-D-galactosaminyl-epidermal growth factor receptor
-
 ?
UDP-alpha-D-galactose + N-acetyl-alpha-D-galactosaminyl-R
-
 Homo sapiens UDP + beta-D-galactosyl-(1->3)-N-acetyl-alpha-D-galactosaminyl-R
-
 ?

Synonyms

Synonyms Comment Organism
C1GALT1
-
 Homo sapiens
core 1 beta1,3-galactosyltransferase
-
 Homo sapiens

General Information

General Information Comment Organism
malfunction core 1 beta1,3-galactosyltransferase (C1GALT1) expression is upregulated in HNSCC tumors and is associated with adverse clinicopathologic features. Moreover, high C1GALT1 expression predicts poor disease-free and overall survivals. C1GALT1 overexpression enhances HNSCC cell viability, migration, and invasion, which can be reversed by erlotinib. Silencing of C1GALT1 suppresses the malignant behavior both in vitro and in vivo. Blocking O-glycan elongation on epidermal growth factor receptor (EGFR) by C1GALT1 knockdown decreases EGF-EGFR binding affinity and inhibits EGFR signaling, thereby suppressing malignant phenotypes. C1GALT1 knockout also decreases the EGFR signaling in SAS cells as shown in two independent clones. C1GALT1 overexpression in SAS cells increases EGF-induced phosphorylation of EGFR at Y1068. By contrast, C1GALT1 knockdown decreases the EGFR signaling in OEC-M1 and FaDu cells. Decreased C1GALT1 causes accumulation of Tn antigens, which is detected by vicia villosa agglutinin (VVA) lectin Homo sapiens
additional information C1GALT1 is overexpressed in various human malignancies Homo sapiens
physiological function core 1 beta1,3-galactosyltransferase (C1GALT1) controls the crucial step of GalNAc-type O-glycosylation. C1GALT1 regulates phosphorylation, EGF-binding affinity, and O-glycosylation of EGFR to enhance malignant phenotypes in HNSCC cells. Itraconazole blocks C1GALT1-mediated malignant phenotypes and EGFR activity, overview. C1GALT1 transfers galactose to Tn antigen to form T antigen Homo sapiens