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Drug-Target Interaction

Drug

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PubChem ID:3463
Structure:
Synonyms:
1A Brand of Gemfibrozil
2,2-Dimethyl-5-(2,5-dimethylphenoxy)pentanoic acid
2,2-Dimethyl-5-(2,5-dimethylphenoxy)valeriansaeure
2,2-Dimethyl-5-(2,5-xylyloxy)valeriansaeure
2,2-Dimethyl-5-(2,5-xylyloxy)valeric acid
25812-30-0
5-(2,5-Dimethyl-Phenoxy)-2,2-Dimethyl-Pentanoic Acid
5-(2,5-Dimethylphenoxy)-2,2-dimethylpentanoic acid
5-[(2,5-dimethylphenyl)oxy]-2,2-dimethylpentanoic acid
AB00052003
AC-4225
AC1L1FZT
AC1Q2JC7
AIDS-121781
AIDS121781
AKOS001606691
Alphapharm Brand of Gemfibrozil
Apo Gemfibrozil
Apo-Gemfibrozil
ApoGemfibrozil
Apotex Brand of Gemfibrozil
ARONIS24091
Ausgem
Bayvit Brand of Gemfibrozil
Bayvit, Gemfibrozilo
BB_SC-4837
Bexal Brand of Gemfibrozil
Bexal, Gemfibrozilo
Biochemie Brand of Gemfibrozil
Bolutol
BPBio1_000251
BRD-K11129031-001-05-1
BRN 1881200
Brozil
BSPBio_000227
BSPBio_002060
Bull Brand of Gemfibrozil
C07020
C15H22O3
Cantabria Brand of Gemfibrozil
CAS-25812-30-0
CCG-40111
CCRIS 318
CHEBI:5296
Chem mart Brand of Gemfibrozil
Chem mart Gemfibrozil
CHEMBL457
Cholespid
CI 719
CI-719
CI719
Clearol
CPD000058393
D00334
D015248
DB01241
DBL Gemfibrozil
Decrelip
DivK1c_000138
Douglas Brand of Gemfibrozil
EINECS 247-280-2
Elmogan
Farmasierra Brand of Gemfibrozil
Faulding Brand of Gemfibrozil
Ferrer Brand of Gemfibrozil
Fetinor
Fibratol
Fibrocit
G9518_SIGMA
GEM
Gem-S
Gemcor, Lopid, Jezil, Gen-Fibro, Gemfibrozil
Gemd
Gemfi 1A Pharma
Gemfibril
Gemfibromax
Gemfibrosil
GEMFIBROZIL
Gemfibrozil (JAN/USP/INN)
GEMFIBROZIL (SEE ALSO PEROXISOME PROJECT (GEMFIBROZIL))
Gemfibrozil [USAN:BAN:INN]
Gemfibrozil, GenRX
Gemfibrozil, Healthsense
Gemfibrozil, SBPA
Gemfibrozil-Supplied by Selleck Chemicals
Gemfibrozilo
Gemfibrozilo Bayvit
Gemfibrozilo Bexal
Gemfibrozilo Ur
Gemfibrozilo [INN-Spanish]
Gemfibrozilum
Gemfibrozilum [INN-Latin]
Gemhexal
Gemlipid
Gemnpid
Gen Gemfibrozil
Gen-Fibro
Gen-Gemfibrozil
GenGemfibrozil
Genlip
Genpharm Brand of Gemfibrozil
GenRX Gemfibrozil
Gevilon
Gevilon Uno
GFZ
Gozid
Healthsense Brand of Gemfibrozil
Healthsense Gemfibrozil
Hexal Brand of Gemfibrozil
Hidil
Hipolixan
HMS1568L09
HMS1920B07
HMS2090K14
HMS2091H11
HMS2095L09
HMS2230H24
HMS3259M12
HMS500G20
I01-1855
IDI1_000138
Innogem
Innogen
Ipolipid
Ipsen Brand of Gemfibrozil
Jezil
KBio1_000138
KBio2_001305
KBio2_003873
KBio2_006441
KBio3_001280
KBioGR_000964
KBioSS_001305
Lanaterom
Lifibron
Lipazil
Lipigem
Lipira
Lipizyl
Lipox Gemfi
Lipozid
Lipur
Litarek
Lopid
Lopid (TN)
Lopid R
Low-Lip
LS-1085
Menarini Brand of Gemfibrozil
Micolip
MLS000028421
MLS001055364
NCGC00016794-01
NCGC00016794-02
NCGC00016794-03
NCGC00016794-04
NCGC00016794-05
NCGC00016794-06
NCGC00016794-07
NCGC00016794-08
NCGC00016794-09
NCGC00016794-10
NCGC00016794-11
NCGC00022722-03
NCGC00022722-04
NCGC00022722-05
NCGC00022722-06
NCGC00022722-07
nchembio790-comp22
NINDS_000138
Normolip
Novo Gemfibrozil
Novo-Gemfibrozil
Novopharm Brand of Gemfibrozil
Nu Gemfibrozil
Nu Pharm Brand of Gemfibrozil
Nu-Gemfibrozil
Nu-Pharm Brand of Gemfibrozil
NuGemfibrozil
Parke Davis Brand of Gemfibrozil
Pentanoic acid, 5-(2,5-dimethylphenoxy)-2,2-dimethyl-
PEROXISOME PROJECT (GEMFIBROZIL) (SEE ALSO GEMFIBROZIL)
Pfizer Brand of Gemfibrozil
Pharmascience Brand of Gemfibrozil
Pilder
PMS Gemfibrozil
PMS-Gemfibrozil
Polyxit
Prestwick0_000214
Prestwick1_000214
Prestwick2_000214
Prestwick3_000214
Prestwick_637
Progemzal
Quimifar Brand of Gemfibrozil
Reducel
Regulip
Renabrazin
S1729_Selleck
SAM002564211
SBB012457
SBPA Gemfibrozil
Sigma Brand of Gemfibrozil
Sinelip
SMR000058393
SPBio_001174
SPBio_002148
SPECTRUM1500313
Spectrum2_001097
Spectrum3_000440
Spectrum4_000562
Spectrum5_000750
Spectrum5_001991
Spectrum_000825
SR-01000000056
SR-01000000056-6
ST072198
STK618740
Synbrozil
Taborcil
TAD Brand of Gemfibrozil
Tentroc
Terry White Chemists Brand of Gemfibrozil
Terry White Chemists Gemfibrozil
TEVA-A
TL8002081
Trialmin
UNII-Q8X02027X3
United Drug Brand of Gemfibrozil
Valeric acid, 2,2-dimethyl-5-(2,5-xylyloxy)-
Warner Lambert Brand of Gemfibrozil
Warner-Lambert Brand of Gemfibrozil
WL-Gemfibrozil
ATC-Codes:
Side-Effects:
Side-EffectFrequency
dyspepsia0.020499999
abdominal pain0.014857144
diarrhea0.0128333345
fatigue0.0071666664
nausea0.0050
vomiting0.0049999994
acute appendicitis0.004666667
atrial fibrillation0.0040
eczema0.0039999993
vertigo0.0033333332
constipation0.0031666665
rash0.0031428565
headache0.0024285712
flatulence0.0010
blurred vision0.0
myalgia0.0
urticaria0.0
thrombocytopenia0.0
myopathy0.0
pancreatitis0.0
impotence0.0
jaundice0.0
leukopenia0.0
synovitis0.0
rhabdomyolysis0.0
pruritus0.0
peripheral neuritis0.0
eosinophilia0.0
edema0.0
alopecia0.0
anemia0.0
angioedema0.0
arthralgia0.0
photosensitivity0.0
cholecystitis0.0
cholelithiasis0.0
dizziness0.0
somnolence0.0
dermatitis0.0
decreased libido0.0
exfoliative dermatitis0.0
vasculitis0
bacterial infections0
convulsions0
cataract0
liver function tests abnormal0
anaphylaxis0
epigastric pain0
hepatoma0
urinary tract infection0
cerebral hemorrhage0
lupus0
gout0
confusion0
common cold0
pain0
colitis0
paresthesia0
cough0
syncope0
chest pain0
peripheral vascular disorder0

Target

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Uniprot ID:NOS3_HUMAN
Synonyms:
cNOS
Constitutive NOS
EC-NOS
Endothelial NOS
eNOS
Nitric oxide synthase, endothelial
NOS type III
NOSIII
EC-Numbers:1.14.13.39
Organism:Homo sapiens
Human
PDB IDs:1M9J 1M9K 1M9M 1M9Q 1M9R 3EAH 3NOS
Structure:
3NOS

Binding Affinities:

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

References:

12244038
Gemfibrozil, a lipid-lowering drug, inhibits the induction of nitric-oxide synthase in human astrocytes.. Kalipada Pahan; Malabendu Jana; Xiaojuan Liu; Bradley S Taylor; Charles Wood; Susan M Fischer (2002) The Journal of biological chemistry display abstract
Gemfibrozil, a lipid-lowering drug, inhibited cytokine-induced production of NO and the expression of inducible nitric-oxide synthase (iNOS) in human U373MG astroglial cells and primary astrocytes. Similar to gemfibrozil, clofibrate, another fibrate drug, also inhibited the expression of iNOS. Inhibition of human iNOS promoter-driven luciferase activity by gemfibrozil in cytokine-stimulated U373MG astroglial cells suggests that this compound inhibits the transcription of iNOS. Since gemfibrozil is known to activate peroxisome proliferator-activated receptor-alpha (PPAR-alpha), we investigated the role of PPAR-alpha in gemfibrozil-mediated inhibition of iNOS. Gemfibrozil induced peroxisome proliferator-responsive element (PPRE)-dependent luciferase activity, which was inhibited by the expression of DeltahPPAR-alpha, the dominant-negative mutant of human PPAR-alpha. However, DeltahPPAR-alpha was unable to abrogate gemfibrozil-mediated inhibition of iNOS suggesting that gemfibrozil inhibits iNOS independent of PPAR-alpha. The human iNOS promoter contains consensus sequences for the binding of transcription factors, including interferon-gamma (IFN-gamma) regulatory factor-1 (IRF-1) binding to interferon-stimulated responsive element (ISRE), signal transducer and activator of transcription (STAT) binding to gamma-activation site (GAS), nuclear factor-kappaB (NF-kappaB), activator protein-1 (AP-1), and CCAAT/enhancer-binding protein beta (C/EBPbeta); therefore, we investigated the effect of gemfibrozil on the activation of these transcription factors. The combination of interleukin (IL)-1beta and IFN-gamma induced the activation of NF-kappaB, AP-1, C/EBPbeta, and GAS but not that of ISRE, suggesting that IRF-1 may not be involved in cytokine-induced expression of iNOS in human astrocytes. Interestingly, gemfibrozil strongly inhibited the activation of NF-kappaB, AP-1, and C/EBPbeta but not that of GAS in cytokine-stimulated astroglial cells. These results suggest that gemfibrozil inhibits the induction of iNOS probably by inhibiting the activation of NF-kappaB, AP-1, and C/EBPbeta and that gemfibrozil, a prescribed drug for humans, may further find its therapeutic use in neuroinflammatory diseases.