Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.4.2.12 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)

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

Protein Variants

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

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P43490
-
-

Purification (Commentary)

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
nicotinamide phosphoribosyltransferase
-
Homo sapiens

IC50 Value

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