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Drug-Target Interaction

Drug

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PubChem ID:5280863
Structure:
Synonyms:
"3,4′,5,7-tetrahydroxyflavone"
3,4′,5,7-Tetrahydroxyflavone
3,4',5,7-Tetrahydroxyflavone
3,5,7,4'-Tetrahydroxyflavone
3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-1- benzopyran-4-one
3,5,7-Trihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one
3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
3,5,7-trihydroxy-2-(4-hydroxyphenyl)chromen-4-one
3,5,7-Trihydroxy-2-[4-hydroxy- phenyl]-4H-1-benzopyran-4-one
3,5,7-triOH-Flavone
4H-1-Benzopyran-4-one,
4H-1-Benzopyran-4-one, 3,5,7-trihydroxy-2-(4-hydroxyphenyl)-
4H-1-Benzopyran-4-one, 3,5,7-trihydroxy-2-(4-hydroxyphenyl)- (9CI)
4H-1-Benzopyran-4-one, 3,5,7-trihydroxy-2-(4-hydroxyphenyl)-5,7,4'-Trihydroxyflavonol
4H-1-Benzopyran-4-one,3,5,7-trihydroxy-2-(4-hydroxyphenyl)-5,7,4'-Trihydroxyflavonol
5,7,4'-Trihydroxyflavonol
5-18-05-00251 (Beilstein Handbook Reference)
520-18-3
60010_FLUKA
60010_SIGMA
A91A6666-86C8-4B33-B3EF-F74CD3CD7F47
AB00514046
AC-544
AC1NQXP1
ACon1_001867
AI3-36096
AIDS-001404
AIDS001404
BIDD:ER0134
BIDD:PXR0073
BPBio1_001294
BRD-K12807006-001-05-2
BRN 0304401
BSPBio_001176
C.I. 75640
C05903
C15H10O6
Campherol
CAS-520-18-3
CCG-202823
CCRIS 41
CHEBI:28499
CHEMBL150
DB01852
EINECS 208-287-6
Flavone, 3,4',5,7-tetrahydroxy-
Flavone, 3,4',5,7-tetrahydroxy- (7CI,8CI)
HMS1571K18
HMS2098K18
HMS2267I09
HSCI1_000027
I06-0240
Indigo yellow
K0018
K0133_SIGMA
Kaemferol
Kaempferol
Kaempferol-Supplied by Selleck Chemicals
Kaempherol
Kampcetin
Kampferol
Kampherol
Kempferol
KMP
LMPK12110003
LS-176
MEGxp0_001283
MLS000697730
MLS001055391
MLS001074884
MolPort-001-741-568
NCGC00016480-01
NCGC00016480-02
NCGC00016480-03
NCGC00016480-04
NCGC00016480-05
NCGC00016480-06
NCGC00016480-07
NCGC00091036-01
NCGC00091036-02
NCGC00164322-01
NCGC00179275-01
NCGC00179275-02
nchembio.2007.28-comp30
nchembio718-comp14
Nimbecetin
NSC 407289
NSC 656277
NSC-407289
NSC-656277
NSC407289
NSC656277
Oprea1_650954
Pelargidenolon
Pelargidenolon 1497
Pelargidenon
Populnetin
Prestwick0_001098
Prestwick1_001098
Prestwick2_001098
Prestwick3_001098
Rhamnolutein
Rhamnolutin
Robigenin
S00111
S2314_Selleck
SMR000112585
SPBio_003058
ST030560
Swartziol
TNP00039
Trifolitin
ZINC03869768

Target

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Uniprot ID:CP1A2_HUMAN
Synonyms:
CYPIA2
Cytochrome P450 1A2
P(3)450
P450 4
P450-P3
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2HI4
Structure:
2HI4

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
--716-

References:

16226778
Effect of Ginkgo biloba extract on procarcinogen-bioactivating human CYP1 enzymes: identification of isorhamnetin, kaempferol, and quercetin as potent inhibitors of CYP1B1.. Thomas K H Chang; Jie Chen; Eugene Y H Yeung (2006) Toxicology and applied pharmacology display abstract
In the present study, we investigated the effect of Ginkgo biloba extracts and some of its individual constituents on the catalytic activity of human cytochrome P450 enzymes CYP1B1, CYP1A1, and CYP1A2. G. biloba extract of known abundance of terpene trilactones and flavonol glycosides inhibited 7-ethoxyresorufin O-dealkylation catalyzed by human recombinant CYP1B1, CYP1A1, and CYP1A2, and human liver microsomes, with apparent Ki values of 2 +/- 0.3, 5 +/- 0.5, 16 +/- 1.4, and 39 +/- 1.2 microg/ml (mean +/- SE), respectively. In each case, the mode of inhibition was of the mixed type. Bilobalide, ginkgolides A, B, C, and J, quercetin 3-O-rutinoside, kaempferol 3-O-rutinoside, and isorhamentin 3-O-rutinoside were not responsible for the inhibition of CYP1 enzymes by G. biloba extract, as determined by experiments with these individual chemicals at the levels present in the extract. In contrast, the aglycones of quercetin, kaempferol, and isorhamentin inhibited CYP1B1, CYP1A1, and CYP1A2. Among the three flavonol aglycones, isorhamentin was the most potent in inhibiting CYP1B1 (apparent Ki = 3 +/- 0.1 nM), whereas quercetin was the least potent in inhibiting CYP1A2 (apparent Ki = 418 +/- 50 nM). The mode of inhibition was competitive, noncompetitive, or mixed, depending on the enzyme and the flavonol. G. biloba extract also reduced benzo[a]pyrene hydroxylation, and the effect was greater with CYP1B1 than with CYP1A1 as the catalyst. Overall, our novel findings indicate that G. biloba extract and the flavonol aglycones isorhamnetin, kaempferol, and quercetin preferentially inhibit the in vitro catalytic activity of human CYP1B1.