General Information of Drug (ID: DM4XAU7)

Drug Name
PGF2alpha Drug Info
Synonyms Amoglandin; Cerviprost; Cyclosin; Enzaprost; Panacelan; prostaglandin F2alpha
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Clinical trial [1]
Cross-matching ID
PubChem CID
5280363
ChEBI ID
CHEBI:15553
CAS Number
CAS 551-11-1
TTD Drug ID
DM4XAU7
VARIDT Drug ID
DR00007
INTEDE Drug ID
DR1917

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Prostaglandin D2 receptor (PTGDR) TTNVEIR PD2R_HUMAN Agonist [2]
Prostaglandin D2 receptor 2 (PTGDR2) TTQDMX5 PD2R2_HUMAN Agonist [3]
Prostaglandin E2 receptor EP1 (PTGER1) TTG1QMU PE2R1_HUMAN Agonist [4]
Prostaglandin E2 receptor EP2 (PTGER2) TT1ZAVI PE2R2_HUMAN Agonist [5]
Prostaglandin E2 receptor EP3 (PTGER3) TTPNGDE PE2R3_HUMAN Agonist [6]
Prostaglandin E2 receptor EP4 (PTGER4) TT79WV3 PE2R4_HUMAN Agonist [4]
Prostaglandin F2-alpha receptor (PTGFR) TTT2ZAR PF2R_HUMAN Agonist [7]
Thromboxane A2 receptor (TBXA2R) TT2O84V TA2R_HUMAN Agonist [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic anion transporting polypeptide 2A1 (SLCO2A1) DT021JD SO2A1_HUMAN Preclinical [8]
Organic anion transporting polypeptide 3A1 (SLCO3A1) DTVNRXW SO3A1_HUMAN Preclinical [9]
Organic anion transporter 2 (SLC22A7) DT0OC1Q S22A7_HUMAN Preclinical [10]
Organic anion transporter 4 (SLC22A11) DT06JWZ S22AB_HUMAN Preclinical [11]
Multidrug resistance-associated protein 4 (ABCC4) DTCSGPB MRP4_HUMAN Preclinical [12]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Preclinical [11]
Organic anion transporter 1 (SLC22A6) DTQ23VB S22A6_HUMAN Preclinical [11]
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Preclinical [11]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Preclinical [11]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
NADPH-dependent carbonyl reductase 1 (CBR1) DE9JFMC CBR1_HUMAN Phase 2 [13]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Prostaglandin F2-alpha receptor (PTGFR) DTT PTGFR 0.379 2.744 3.609 1.138
Prostaglandin D2 receptor 2 (PTGDR2) DTT PTGDR2 4.436 5.954 4.217 4.641
Prostaglandin E2 receptor EP3 (PTGER3) DTT PTGER3 4.768 4.711 6.12 3.579
Prostaglandin D2 receptor (PTGDR) DTT PTGDR 1.609 4.087 1.433 1.963
Prostaglandin E2 receptor EP4 (PTGER4) DTT PTGER4 4.907 7.298 6.097 7.251
Thromboxane A2 receptor (TBXA2R) DTT TBXA2R 6.075 5.925 6.729 6.096
Prostaglandin E2 receptor EP2 (PTGER2) DTT PTGER2 4.75 5.888 5.066 4.466
Organic anion transporter 3 (SLC22A8) DTP OAT3 2.722 2.07 8.103 3.597
Organic anion transporting polypeptide 3A1 (SLCO3A1) DTP OATP3A1 4.875 5.404 5.38 4.624
Organic cation transporter 1 (SLC22A1) DTP `OCT1 10.261 4.162 4.07 3.797
Organic anion transporter 1 (SLC22A6) DTP OAT1 4.413 2.233 7.194 4.655
Multidrug resistance-associated protein 4 (ABCC4) DTP MRP4 4.797 7.054 6.875 5.42
Organic cation transporter 2 (SLC22A2) DTP `OCT2 3.766 3.548 7.303 3.548
Organic anion transporter 2 (SLC22A7) DTP OAT2 6.588 1.202 4.42 4.07
Organic anion transporter 4 (SLC22A11) DTP OAT4 1.926 2.585 6.595 3.336
Organic anion transporting polypeptide 2A1 (SLCO2A1) DTP OATP2A1 5.629 6.995 8.616 7.337
NADPH-dependent carbonyl reductase 1 (CBR1) DME CBR1 7.303 5.776 7.91 9.608
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Solid tumour/cancer
ICD Disease Classification 2A00-2F9Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Prostaglandin F2-alpha receptor (PTGFR) DTT PTGFR 8.25E-02 -0.05 -0.14
Organic anion transporter 3 (SLC22A8) DTP OAT3 5.19E-01 -8.88E-03 -2.08E-02
Organic anion transporting polypeptide 3A1 (SLCO3A1) DTP OATP3A1 1.83E-05 3.48E-01 6.12E-01
Organic cation transporter 1 (SLC22A1) DTP SLC22A1 8.54E-01 1.24E-02 7.20E-02
Organic anion transporter 1 (SLC22A6) DTP OAT1 7.18E-01 -4.56E-02 -1.42E-01
Multidrug resistance-associated protein 4 (ABCC4) DTP MRP4 3.73E-06 2.82E-01 7.01E-01
Organic cation transporter 2 (SLC22A2) DTP SLC22A2 8.22E-01 -1.05E-02 -3.83E-02
Organic anion transporter 2 (SLC22A7) DTP OAT2 5.96E-02 -5.09E-02 -3.48E-01
Organic anion transporter 4 (SLC22A11) DTP OAT4 4.61E-04 -7.04E-02 -3.49E-01
Organic anion transporting polypeptide 2A1 (SLCO2A1) DTP OATP2A1 3.03E-03 -9.85E-02 -3.19E-01
NADPH-dependent carbonyl reductase 1 (CBR1) DME CBR1 3.47E-01 1.55E-01 2.60E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81.
2 The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93.
3 Expression and molecular pharmacology of the mouse CRTH2 receptor. J Pharmacol Exp Ther. 2003 Aug;306(2):463-70.
4 Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes. Eur J Pharmacol. 1997 Dec 11;340(2-3):227-41.
5 Importance of the extracellular domain for prostaglandin EP(2) receptor function. Mol Pharmacol. 1999 Sep;56(3):545-51.
6 Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24.
7 Identification by site-directed mutagenesis of amino acids contributing to ligand-binding specificity or signal transduction properties of the human FP prostanoid receptor. Biochem J. 2003 Apr 15;371(Pt 2):443-9.
8 Cloning, in vitro expression, and tissue distribution of a human prostaglandin transporter cDNA(hPGT). J Clin Invest. 1996 Sep 1;98(5):1142-9.
9 Molecular characterization of human and rat organic anion transporter OATP-D. Am J Physiol Renal Physiol. 2003 Dec;285(6):F1188-97.
10 Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors. J Pharmacol Exp Ther. 2002 Jun;301(3):797-802.
11 Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8.
12 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
13 Metabolism of prostaglandins by the nonpregnant human uterus. J Clin Endocrinol Metab. 1983 Apr;56(4):678-85.