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Drug-Target Interaction

Drug

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PubChem ID:4696
Structure:
Synonyms:
(2,4-Dihydroxy-2H-pyran-3(6H)-ylidene)acetic acid, 3,4-lactone
(2,4-Dihydroxy-2H-pyran-3(6H)-ylidene)acetic acid-3,4-lactone
149-29-1
2,4-Dihydroxy-2H-pyran-.delta.-3(6H),.alpha.-acetic acid, 3,4-lactone
2,4-Dihydroxy-2H-pyran-delta-3(6H),alpha-acetic acid-3,4-lactone
2H-Pyran-.delta.(sup 3(6H),.alpha.)-acetic acid, 2,4-dihydroxy-,
2H-Pyran-.delta.(sup 3(6H),.alpha.)-acetic acid, 2,4-dihydroxy-, 3,4-lactone
2H-Pyran-.delta.(sup 3(6H),.alpha.)-acetic acid, 2,4-dihydroxy-,3,4-lactone
2H-Pyran-delta(sup 3(6H),alpha)-acetic acid, 2,4-dihydroxy-, 3,4-lactone
34127_FLUKA
34127_RIEDEL
4,6-Dihydro-4-hydroxy-2H-furo(3,2-c)pyran-2-one
4-Hydroxy-4,6-dihydrofuro[4,5-c]pyran-2-one
4-Hydroxy-4H-furo(3,2-C)pyran-2(6H)-one
4-Hydroxy-4H-furo[3,2-c]pyran-2(6H)-one
46914U_SUPELCO
4H-Furo(3,2-c)pyran-2(6H)-one, 4-hydroxy-
4H-Furo(3,3-c)pyran-2(6H)-one, 4-hydroxy-
4H-Furo[3,2-c]pyran-2(6H)-one, 4-hydroxy-
5-18-03-00005 (Beilstein Handbook Reference)
Acetic acid, (2,4-dihydroxy-2H-pyran-3(6H)-ylidene)-, 3,4-lactone
ACon1_002106
AIDS-031082
AIDS031082
BRN 0149675
BSPBio_002532
C7H6O4
CCRIS 4940
Clairformin
Clavacin
Clavatin
Claviform
Claviformin
DivK1c_000438
EINECS 205-735-2
Expansin
Expansine
Gigantin
HSDB 3522
IDI1_000438
KBio1_000438
KBio2_000355
KBio2_002923
KBio2_005491
KBio3_001752
KBioGR_001106
KBioSS_000355
Leucopin
LS-868
MEGxm0_000442
Mycoin
Mycoin C
Mycoin C3
Mycoine C3
Mycosin
NCGC00095272-01
NCGC00095272-02
NCGC00095272-03
NCGC00095272-04
NCGC00095272-05
nchembio.2007.59-comp24
nchembio790-comp32
NCI60_041782
Neuro_000008
NINDS_000438
NSC 32951
NSC 8120
NSC32951
NSC8120
P1639_SIGMA
PAT
PATULIN
Patulin solution
Patuline
Penatin
Penicidin
SCH 351633
Sch-351633
SMP1_000230
SPECTRUM1503904
Spectrum3_000796
Spectrum4_000753
Spectrum5_001659
Spectrum_000015
Tercinin
Terinin
WLN: T56 BOV GO IU & TJ FQ

Target

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Uniprot ID:AT1A3_MOUSE
Synonyms:
Na(+)/K(+) ATPase alpha(III) subunit
Na(+)/K(+) ATPase alpha-3 subunit
Sodium pump subunit alpha-3
Sodium/potassium-transporting ATPase subunit alpha-3
EC-Numbers:3.6.3.9
Organism:Mouse
Mus musculus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

26794
Effects of patulin on the kinetics of substrate and cationic ligand activation of adenosine triphosphatase in mouse brain.. T D Phillips; A W Hayes (1978) The Journal of pharmacology and experimental therapeutics display abstract
Patulin (4-hydroxy-4H-furo[3,2-c]pyran-2(6H)-one), a carcinogenic lactone produced as a major metabolite by several fungi, inhibited the Mg++-dependent Na+-K+ activated adenosine triphosphatase (ATPase) activity of mouse brain microsomal fractions with an estimated IC50 of 3.0 X 10(-4) M. Inhibition was concentration dependent. Hydrolysis of ATP was linear with both time and enzyme concentration either with or without patulin in reaction mixtures. Altered pH and activity curves for Na+-K+ ATPase demonstrated comparable inhibition by patulin in buffered acidic ranges through an optimum of 7.5, followed by a reduction of toxicity to this system at higher alkaline pH. Kinetic studies of cationic-substrate activation of Na+-K+ ATPase indicated noncompetitive inhibition with respect to ATP (at low affinity nucleotide-directed sites) and Na+ (in the presence of low, noninterfering concentrations of K+). Competitive inhibition with respect to activation of the Na+-k+-stimulated activity and K+-stimulated p-nitrophenyl phosphatase activity of the enzyme system was indicated by altered binding site parameters without change in apparent Vmax in the presence of patulin. Activity was partially restored by washing. Preincubation of patulin with dithiothreitol or glutathione protected the enzyme from inhibition. Results suggest that patulin exerted its effect on Na+-K+ ATPase either directly by interfering with K+ binding or indirectly by inducing a conformational change in the enzyme.