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Literature summary extracted from

  • Olesen, U.; Petersen, J.; Garten, A.; Kiess, W.; Yoshino, J.; Imai, S.; Christensen, M.; Fristrup, P.; Thougaard, A.; Björkling, F.; Jensen, P.; Nielsen, S.; Sehested, M.
    Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase (2010), BMC Cancer, 10, 677.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.2.12 expressed in Escherichia coli Rosetta 2 (DE3) Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.4.2.12 DELTA D93 naturally occuring mutation in CHS-828 or APO866 resistant cell lines, about 20% of wild type aczivity Homo sapiens
2.4.2.12 H191R activity reduced by about 50% Homo sapiens
2.4.2.12 H191R/K342R naturally occuring mutation in APO866 resistant cell line Homo sapiens
2.4.2.12 H191R/K342R/Q388R naturally occuring mutation in TP201565 resistant cell line Homo sapiens
2.4.2.12 K342R naturally occuring mutation, activity reduced by about 50% Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.12 CHS-828 competitive inhibitor Homo sapiens
2.4.2.12 FK-866
-
 Homo sapiens
2.4.2.12 TP201565 competitive inhibitor Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.12 Homo sapiens P43490
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.4.2.12 immobilized metal ion affinity chromatography (Ni2+) Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.2.12 HCT-116 cell
-
 Homo sapiens
-
2.4.2.12 HEK-293T cell
-
 Homo sapiens
-
2.4.2.12 NYH cell
-
 Homo sapiens
-
2.4.2.12 PC-3 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.12 nicotinamide + 5-phosphoribosyl 1-diphosphate
-
 Homo sapiens nicotinamide mononucleotide + diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.2.12 nicotinamide phosphoribosyltransferase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.12 0.00011
-
 wild type protein, pH 8.5, 37°C Homo sapiens FK-866
2.4.2.12 0.008585
-
 H191R mutant protein, pH 8.5, 37°C Homo sapiens FK-866