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Literature summary for 2.4.1.150 extracted from

  • Rao, C.V.; Janakiram, N.B.; Madka, V.; Kumar, G.; Scott, E.J.; Pathuri, G.; Bryant, T.; Kutche, H.; Zhang, Y.; Biddick, L.; Gali, H.; Zhao, Y.D.; Lightfoot, S.; Mohammed, A.
    Small-molecule inhibition of GCNT3 disrupts mucin biosynthesis and malignant cellular behaviors in pancreatic cancer (2016), Cancer Res., 76, 1965-1974 .
    View publication on PubMed

Application

Application Comment Organism
pharmacology targeting mucin biosynthesis through GCNT3 may improve drug responsiveness Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
gene GCNT3, genotyping Mus musculus

Protein Variants

Protein Variants Comment Organism
additional information CRISPR-mediated knockout of GCNT3 in pancreatic cancer cells Homo sapiens
additional information CRISPR-mediated knockout of GCNT3 in pancreatic cancer cells. A significant increase in pancreas weight is observed in Kras mice compared with wild-type mice. Only 6% of the pancreata from Kras mice are free from PanIN lesions and PDAC, whereas 100% of pancreata are normal in wild-type mice Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
talniflumate inhibits GCNT3 and mucins in genetically engineered mice in vivo Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens O95395
-
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Mus musculus Q5JCT0
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Mus musculus C5BL/6 Q5JCT0
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-

Source Tissue

Source Tissue Comment Organism Textmining
BxPC-3 cell
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Homo sapiens
-
MiaPaCa-2 cell
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Homo sapiens
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PANC-1 cell
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Homo sapiens
-
pancreas
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Homo sapiens
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pancreas
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Mus musculus
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pancreatic cancer cell over 95% of human pancreatic cancers are associated with Kras mutations Homo sapiens
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pancreatic cancer cell pancreas tumor tissue transcriptome analysis Mus musculus
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Synonyms

Synonyms Comment Organism
core 2 beta-1,6-N-acetylglucosaminyltransferase
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Homo sapiens
core 2 beta-1,6-N-acetylglucosaminyltransferase
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Mus musculus
gcnt3
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Homo sapiens
gcnt3
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Mus musculus
More cf. EC 2.4.1.102 and 2.4.1.148 Homo sapiens
More cf. EC 2.4.1.102 and 2.4.1.148 Mus musculus

Expression

Organism Comment Expression
Mus musculus in mouse pancreatic cancer tumors, GCNT3 upregulation (103fold) is correlated with increased expression of mucins (5 to 87fold). Pancreata from 6-week-old Kras mice treated with talniflumate for 1 week show a significant decrease in GCNT3 and mucin expression in PanIN lesions. Further, GCNT3 protein expression is significantly decreased in the pancreas of talniflumate-treated Kras mice compared with untreated control mouse pancreas. mRNA expression of GCNT3 is also observed to be lower in pancreatic tissues from talniflumate-treated mice down
Homo sapiens talniflumate alone and in combination with low-dose gefitinib reduces GCNT3 expression, leading to the disrupted production of mucins in vivo and in vitro, in silico molecular docking studies. Talniflumate binds to GCNT3 with a docking affinity of -8.3 kcal/mol and deeper in the pocket of GCNT3. GALB1,3GALNAC's best docking affinity is -7.51 kcal/mol, achieved closer to the surface of GCNT3 down

General Information

General Information Comment Organism
malfunction in mouse pancreatic cancer tumors, GCNT3 upregulation is correlated with increased expression of mucins. Aberrant GCNT3 expression is associated with increased mucin production, aggressive tumorigenesis, and reduced survival. CRISPR-mediated knockout of GCNT3 in pancreatic cancer cells reduced proliferation and spheroid formation Mus musculus
malfunction talniflumate alone and in combination with low-dose gefitinib reduces GCNT3 expression, leading to the disrupted production of mucins in vivo and in vitro. Aberrant GCNT3 expression is associated with increased mucin production, aggressive tumorigenesis, and reduced patient survival. CRISPR-mediated knockout of GCNT3 in pancreatic cancer cells reduced proliferation and spheroid formation Homo sapiens
physiological function core 2 beta-1,6-N-acetylglucosaminyltransferase (GCNT3) is a core mucin-synthesizing enzyme Mus musculus
physiological function core 2 beta-1,6-N-acetylglucosaminyltransferase (GCNT3) is a core mucin-synthesizing enzyme. Correlations between GCNT3 expression and pancreatic tumor progression, Kaplan-Meier analysis of patients' survival by GCNT3 expression level, overview Homo sapiens