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Literature summary 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

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

Protein Variants

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.33 1,4-phenylene-bis(1,2-ethanediyl)bis-isothiourea dihydrobromide
-
Homo sapiens
2.7.1.33 acetyl-CoA complete inhibition of isoform PanK3 at 0.008 mM Homo sapiens
2.7.1.33 ADP competitive inhibitor of isoform PanK3 with respect to ATP1 and a mixed-type inhibitor with respect to pantothenate Homo sapiens
2.7.1.33 chloranil
-
Homo sapiens
2.7.1.33 dehydroisoandrosterone about 30% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
2.7.1.33 Dehydroisoandrosterone sulfate about 8% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
2.7.1.33 ephedrine hydrochloride
-
Homo sapiens
2.7.1.33 estradiol about 80% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
2.7.1.33 Estradiol sulfate about 90% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
2.7.1.33 Estrone sulfate about 50% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
2.7.1.33 Fusidic acid
-
Homo sapiens
2.7.1.33 glipizide
-
Homo sapiens
2.7.1.33 glyburide
-
Homo sapiens
2.7.1.33 GW5074
-
Homo sapiens
2.7.1.33 Hexachlorophene
-
Homo sapiens
2.7.1.33 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
2.7.1.33 additional information isoform PanK3 is not inhibited by estrone Homo sapiens
2.7.1.33 pioglitazone hydrochloride
-
Homo sapiens
2.7.1.33 pregnenolone sulfate about 10% residual activity at 0.1 mM (isoform PanK3); about 92% residual activity at 0.1 mM (isoform PanK3) Homo sapiens
2.7.1.33 Psi-rhodomyrtoxin
-
Homo sapiens
2.7.1.33 Reactive blue 2
-
Homo sapiens
2.7.1.33 Ro 41-0960
-
Homo sapiens
2.7.1.33 rosiglitazone
-
Homo sapiens
2.7.1.33 tamoxifen
-
Homo sapiens
2.7.1.33 tolfenamic acid
-
Homo sapiens
2.7.1.33 tyrphostin AG 528
-
Homo sapiens
2.7.1.33 tyrphostin AG 808
-
Homo sapiens
2.7.1.33 WIN 62577
-
Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.1.33 0.014
-
(R)-pantothenate isoform PanK3, at pH 7.5 and 37°C Homo sapiens
2.7.1.33 0.311
-
ATP isoform PanK3, at pH 7.5 and 37°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.33 Homo sapiens
-
-
-
2.7.1.33 Homo sapiens Q9H999 isoform PanK3
-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.7.1.33 PanK1b isoform Homo sapiens
2.7.1.33 PanK2 isoform Homo sapiens
2.7.1.33 PanK3 isoform Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.33 0.0001
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Fusidic acid
2.7.1.33 0.0004
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens 1,4-phenylene-bis(1,2-ethanediyl)bis-isothiourea dihydrobromide
2.7.1.33 0.0007
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens WIN 62577
2.7.1.33 0.001
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens pioglitazone hydrochloride
2.7.1.33 0.0013
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Reactive blue 2
2.7.1.33 0.0016
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens ephedrine hydrochloride
2.7.1.33 0.0016
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Psi-rhodomyrtoxin
2.7.1.33 0.0017
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens rosiglitazone
2.7.1.33 0.0025
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens pregnenolone sulfate
2.7.1.33 0.003
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens tyrphostin AG 528
2.7.1.33 0.0035
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Dehydroisoandrosterone sulfate
2.7.1.33 0.0039
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Ro 41-0960
2.7.1.33 0.0052
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens glipizide
2.7.1.33 0.0059
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens chloranil
2.7.1.33 0.0068
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens glyburide
2.7.1.33 0.0088
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens Hexachlorophene
2.7.1.33 0.009
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens tyrphostin AG 808
2.7.1.33 0.0092
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens GW5074
2.7.1.33 0.0092
-
isoform PanK3, at pH 7.5 and 37°C Homo sapiens tolfenamic acid

General Information

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