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Drug-Target Interaction

Drug

show drug details
PubChem ID:5280360
Structure:
Synonyms:
(15S)-Prostaglandin E2
(5Z,11-alpha,13E,15S)-11,15-Dihydroxy-9-oxoprosta-5,13-dien-1-oic acid
(5Z,11.alpha.,13E,15S)-11,15-Dihydroxy-9-oxoprosta-5,13-dien-1-oic acid
(5Z,11alpha,13E,15S)-11,15-Dihydroxy-9-oxoprosta-5,13-dien-1-oic
(5Z,11alpha,13E,15S)-11,15-dihydroxy-9-oxoprosta-5,13-dien-1-oic acid
(5Z,11alpha,13E,15S)-11,15-Dihydroxy-9-oxoprosta-5,13-dienoic acid
(5Z,13E)-(15S)-11alpha,15-Dihydroxy-9-oxoprost-13-enoate
(5Z,13E)-(15S)-11alpha,15-Dihydroxy-9-oxoprosta-5,13-dienoate
(5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dien-1-oic acid
(E,Z)-(1R,2R,3R)-7-(3-Hydroxy-2-((3S)-(3-hydroxy-1-octenyl))-5-oxocyclopentyl)-5-heptenoic acid
(Z)-7-[(1R,2R,3R)-3-Hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxocyclopentyl]hept-5-enoic acid
363-24-6
5-Heptenoic acid, 7-(3-hydroxy-2-(3-hydroxy-1-octenyl)-5-oxocyclopentyl)-
5-Heptenoic acid, 7-(3-hydroxy-2-(3-hydroxy-1-octenyl)-5-oxocyclopentyl)- (8CI)
5-Heptenoic acid, 7-(3-hydroxy-2-(3-hydroxy-1-octenyl)-5-oxocyclopentyl)-,
5-Heptenoic acid, 7-(3-hydroxy-2-(3-hydroxy-1-octenyl)-5-oxocyclopentyl)-, l-
7-(3-Hydroxy-2-(3-hydroxy-1-octenyl)-5-oxocyclopentyl)-5-heptenoic acid
AIDS-003352
AIDS-166064
AIDS003352
AIDS166064
BMS-279654 & PGE2
BSPBio_001490
C00584
C20H32O5
Cervidil
Cervidil (TN)
CHEBI:15551
D00079
Dinoproston
Dinoprostona
Dinoprostona [INN-Spanish]
Dinoprostone
Dinoprostone (JAN/USP/INN)
Dinoprostone [USAN:BAN:INN:JAN]
Dinoprostone [USAN:INN:BAN:JAN]
Dinoprostonum
Dinoprostonum [INN-Latin]
EINECS 206-656-6
Glandin
IDI1_033960
l-7-(3-Hydroxy-2-(3-hydroxy-1-octenyl)-5-oxocyclopentyl)-5-heptenoic acid
l-PGE2
l-Prostaglandin E2
LMFA03010003
LS-125823
Minprositin E2
Minprostin E2
NCGC00092361-01
NCGC00092361-02
NCGC00092361-03
NCGC00092361-04
NCGC00092361-05
nchembio.106-comp6
nchembio.147-comp12
NSC 165560
NSC 196514
P0409_SIGMA
P5640_SIGMA
P6532_SIGMA
PGE2
PGE2 alpha
PGE2alpha
Prepidil
Prepidil (TN)
Prepidil Gel
Prestwick_793
Propess
Prosta-5,13-dien-1-oic acid, (5Z,11-alpha,13E,15S)-11,15-dihydroxy-9-oxo-
Prosta-5,13-dien-1-oic acid, 11,15-dihydroxy-9-oxo-, (5Z,11alpha,13E,15S)-
Prostaglandin E2
Prostaglandin E2 alpha
Prostaglandin E2alpha
Prostin
Prostin E2
Prostin E2 (TN)
SMP2_000056
U 12062
U-12062
ATC-Codes:
Side-Effects:
Side-EffectFrequency
abdominal pain0.0010
vomiting0.0010
fever0.0010
nausea0.0010
diarrhea0.0010
breast tenderness0
vaginitis0
tremor0
tachycardia0
syncope0
pharyngitis0
paresthesia0
weakness0
pain0
nocturnal leg cramps0
hearing loss0
increased sweating0
sepsis0
myalgia0
eye pain0
neck rigidity0
blurred vision0
chills0
urinary retention0
bradycardia0
vulvitis0
wheezing0
myocardial infarction0
dizziness0
dehydration0
cough0
chest pain0
bronchospasm0
back pain0
arthritis0
arthralgia0
arrhythmia0
dyspnea0
endometritis0
rash0
muscle cramps0
laryngitis0
hypotension0
hypertension0
hot flashes0
hiccup0
hemorrhage0
headache0
flushing0
acidosis0

Target

show target details
Uniprot ID:PGES2_HUMAN
Synonyms:
Microsomal prostaglandin E synthase 2
mPGES-2
Prostaglandin E synthase 2
EC-Numbers:5.3.99.3
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

16533161
Prostaglandin E synthase: a novel drug target for inflammation and cancer.. Makoto Murakami; Ichiro Kudo (2006) Current pharmaceutical design display abstract
Prostaglandin E synthase (PGES), which converts cyclooxygenase (COX)-derived prostaglandin (PG) H(2) to PGE(2), occurs in multiple forms with distinct enzymatic properties, modes of expression, cellular and subcellular localizations and intracellular functions. Two of them are membrane-bound enzymes and have been designated as mPGES-1 and mPGES-2. mPGES-1 is a perinuclear protein belonging to the MAPEG (for membrane-associated proteins involved in eicosanoid and GSH metabolism) family. This enzyme is markedly induced by proinflammatory stimuli, is down-regulated by anti-inflammatory glucocorticoids, and is functionally coupled with cyclooxygenase (COX)-2 in marked preference to COX-1. mPGES-2 is synthesized as a Golgi membrane-associated protein, and the proteolytic removal of the N-terminal hydrophobic domain leads to the formation of a mature cytosolic enzyme. This enzyme is rather constitutively expressed in various cells and tissues and is functionally coupled with both COX-1 and COX-2. Cytosolic PGES (cPGES) is constitutively expressed in a wide variety of cells and is functionally linked to COX-1 to promote immediate PGE(2) production. This review highlights the latest understanding of the expression, regulation and functions of these three PGES enzymes. In particular, recent gene targeting studies of mPGES-1 have revealed that this enzyme represents a novel target for anti-inflammatory and anti-cancer drugs.
17878511
Membrane prostaglandin E synthase-1: a novel therapeutic target.. Bengt Samuelsson; Ralf Morgenstern; Per-Johan Jakobsson (2007) Pharmacological reviews display abstract
Prostaglandin E(2) (PGE(2)) is the most abundant prostaglandin in the human body. It has a large number of biological actions that it exerts via four types of receptors, EP1-4. PGE(2) is formed from arachidonic acid by cyclooxygenase (COX-1 and COX-2)-catalyzed formation of prostaglandin H(2) (PGH(2)) and further transformation by PGE synthases. The isomerization of the endoperoxide PGH(2) to PGE(2) is catalyzed by three different PGE synthases, viz. cytosolic PGE synthase (cPGES) and two membrane-bound PGE synthases, mPGES-1 and mPGES-2. Of these isomerases, cPGES and mPGES-2 are constitutive enzymes, whereas mPGES-1 is mainly an induced isomerase. cPGES uses PGH(2) produced by COX-1 whereas mPGES-1 uses COX-2-derived endoperoxide. mPGES-2 can use both sources of PGH(2). mPGES-1 is a member of the membrane associated proteins involved in eicosanoid and glutathione metabolism (MAPEG) superfamily. It requires glutathione as an essential cofactor for its activity. mPGES-1 is up-regulated in response to various proinflammatory stimuli with a concomitant increased expression of COX-2. The coordinate increased expression of COX-2 and mPGES-1 is reversed by glucocorticoids. Differences in the kinetics of the expression of the two enzymes suggest distinct regulatory mechanisms for their expression. Studies, mainly from disruption of the mPGES-1 gene in mice, indicate key roles of mPGES-1-generated PGE(2) in female reproduction and in pathological conditions such as inflammation, pain, fever, anorexia, atherosclerosis, stroke, and tumorigenesis. These findings indicate that mPGES-1 is a potential target for the development of therapeutic agents for treatment of several diseases.