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Literature summary for 2.7.1.33 extracted from

  • Leonardi, R.; Zhang, Y.M.; Yun, M.K.; Zhou, R.; Zeng, F.Y.; Lin, W.; Cui, J.; Chen, T.; Rock, C.O.; White, S.W.; Jackowski, S.
    Modulation of pantothenate kinase 3 activity by small molecules that interact with the substrate/allosteric regulatory domain (2010), Chem. Biol., 17, 892-902.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
cholesterol about 125% activity at 0.1 mM Homo sapiens
glyburide
-
Homo sapiens
glyburide isoform PanK1b is activated by glyburide Homo sapiens
additional information isoform PanK3 is not activated by 1,4-naphthoquinone and phenylmercuric acid Homo sapiens
O-oleoylcarnitine 140% activation at 0.1 mM Homo sapiens
O-palmitoylcarnitine 120% activation at 0.1 mM Homo sapiens
oleoylethanolamide 120% activation at 0.1 mM Homo sapiens
tamoxifen 140% activation at 0.1 mM Homo sapiens

Protein Variants

Protein Variants Comment Organism
A267F catalytically inactive Homo sapiens
A269F catalytically inactive Homo sapiens
R207A catalytically inactive Homo sapiens
S195V the mutant is insensitive to acetyl-CoA and has a KM defect for pantothenate Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1,4-phenylene-bis(1,2-ethanediyl)bis-isothiourea dihydrobromide
-
Homo sapiens
acetyl-CoA complete inhibition of isoform PanK3 at 0.008 mM Homo sapiens
ADP competitive inhibitor of isoform PanK3 with respect to ATP1 and a mixed-type inhibitor with respect to pantothenate Homo sapiens
chloranil
-
Homo sapiens
dehydroisoandrosterone about 30% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
Dehydroisoandrosterone sulfate about 8% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
ephedrine hydrochloride
-
Homo sapiens
estradiol about 80% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
Estradiol sulfate about 90% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
Estrone sulfate about 50% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
Fusidic acid
-
Homo sapiens
glipizide
-
Homo sapiens
glyburide
-
Homo sapiens
GW5074
-
Homo sapiens
Hexachlorophene
-
Homo sapiens
MCC-555 MCC-555 inhibits all three isoforms with a rank order of PanK3 > PanK2 > PanK1b; MCC-555 inhibits all three isoforms with a rank order of PanK3 > PanK2 > PanK1b Homo sapiens
additional information isoform PanK3 is not inhibited by estrone Homo sapiens
pioglitazone hydrochloride
-
Homo sapiens
pregnenolone sulfate about 10% residual activity at 0.1 mM (isoform PanK3); about 92% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
Psi-rhodomyrtoxin
-
Homo sapiens
Reactive blue 2
-
Homo sapiens
Ro 41-0960
-
Homo sapiens
rosiglitazone
-
Homo sapiens
tamoxifen
-
Homo sapiens
tolfenamic acid
-
Homo sapiens
tyrphostin AG 528
-
Homo sapiens
tyrphostin AG 808
-
Homo sapiens
WIN 62577
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.014
-
(R)-pantothenate isoform PanK3, at pH 7.5 and 37°C Homo sapiens
0.311
-
ATP isoform PanK3, at pH 7.5 and 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens Q9H999 isoform PanK3
-

Source Tissue

Source Tissue Comment Organism Textmining
HepG2/C3A cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + (R)-pantothenate
-
Homo sapiens ADP + (R)-4'-phosphopantothenate
-
?

Synonyms

Synonyms Comment Organism
PanK1b isoform Homo sapiens
PanK2 isoform Homo sapiens
PanK3 isoform Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Fusidic acid
0.0004
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens 1,4-phenylene-bis(1,2-ethanediyl)bis-isothiourea dihydrobromide
0.0007
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens WIN 62577
0.001
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens pioglitazone hydrochloride
0.0013
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Reactive blue 2
0.0016
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens ephedrine hydrochloride
0.0016
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Psi-rhodomyrtoxin
0.0017
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens rosiglitazone
0.0025
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens pregnenolone sulfate
0.003
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens tyrphostin AG 528
0.0035
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Dehydroisoandrosterone sulfate
0.0039
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Ro 41-0960
0.0052
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens glipizide
0.0059
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens chloranil
0.0068
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens glyburide
0.0088
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Hexachlorophene
0.009
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens tyrphostin AG 808
0.0092
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens GW5074
0.0092
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens tolfenamic acid

General Information

General Information Comment Organism
metabolism pantothenate kinase catalyzes the rate-controlling step in coenzyme A biosynthesis Homo sapiens