Identification

Name
Allylestrenol
Accession Number
DB01431
Type
Small Molecule
Groups
Approved
Description

A synthetic steroid with progestational activity. It is widely marketed throughout Europe, including Russia and many other European countries, and is also available in Japan, Hong Kong, India, Bangladesh, Indonesia, and much of Southeast Asia, though notably not in the United States or Canada.

Structure
Thumb
Synonyms
  • 17α-allylestr-4-en-17β-ol
  • 3-deketo-17α-allyl-19-nortestosterone
  • Allyl estrenol
  • Allyloestrenol
External IDs
NSC-37723
International/Other Brands
Gestanin / Gestanol / Gestanon / Gestin / Gestrenol / Maintaine / Orageston / Perselin / Profar / Turinal
Categories
UNII
I47VB5DZ8O
CAS number
432-60-0
Weight
Average: 300.4782
Monoisotopic: 300.245315646
Chemical Formula
C21H32O
InChI Key
ATXHVCQZZJYMCF-XUDSTZEESA-N
InChI
InChI=1S/C21H32O/c1-3-12-21(22)14-11-19-18-9-8-15-6-4-5-7-16(15)17(18)10-13-20(19,21)2/h3,6,16-19,22H,1,4-5,7-14H2,2H3/t16-,17+,18+,19-,20-,21-/m0/s1
IUPAC Name
(1S,2R,10R,11S,14R,15S)-15-methyl-14-(prop-2-en-1-yl)tetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadec-6-en-14-ol
SMILES

Pharmacology

Indication

Allylestrenol was designed to be used for miscarriage prevention, prevention of premature labour and has been investigated for possible use in men for treatment for benign prostatic hyperplasia.

Structured Indications
Not Available
Pharmacodynamics

Allylestrenol is a progestogen structurally related to progesterone that has been given in threatened and recurrent miscarriage, and to prevent premature labour. However, with the exception of proven progesterone deficiency, such use is no longer recommended. In threatened miscarriage in progesterone-deficient women a suggested dose is 5 mg three times daily by mouth for 5 to 7 days.

Mechanism of action

Allylestrenol is similar in structure and function to progesterone. Progesterone shares the pharmacological actions of the progestins. Progesterone binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Progesterone will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge. In women who have adequate endogenous estrogen, progesterone transforms a proliferative endometrium into a secretory one. Progesterone is essential for the development of decidual tissue and is necessary to increase endometrial receptivity for implantation of an embryo. Once an embryo has been implanted, progesterone acts to maintain the pregnancy. Progesterone also stimulates the growth of mammary alveolar tissue and relaxes uterine smooth muscle. It has little estrogenic and androgenic activity.

TargetActionsOrganism
AProgesterone receptor
agonist
Human
UEstrogen receptor alpha
agonist
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination

The glucuronide and sulfate conjugates of pregnanediol and pregnanolone are excreted in the urine and bile. Progesterone metabolites which are excreted in the bile may undergo enterohepatic recycling or may be excreted in the feces. Progesterone metabolites are excreted mainly by the kidneys.

Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabThe therapeutic efficacy of Abciximab can be decreased when used in combination with Allylestrenol.Approved
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be decreased when used in combination with Allylestrenol.Approved
AmiodaroneThe metabolism of Allylestrenol can be decreased when combined with Amiodarone.Approved, Investigational
AncrodThe therapeutic efficacy of Ancrod can be decreased when used in combination with Allylestrenol.Investigational
Antithrombin III humanThe therapeutic efficacy of Antithrombin III human can be decreased when used in combination with Allylestrenol.Approved
ApixabanThe therapeutic efficacy of Apixaban can be decreased when used in combination with Allylestrenol.Approved
AprepitantThe serum concentration of Allylestrenol can be increased when it is combined with Aprepitant.Approved, Investigational
ArdeparinThe therapeutic efficacy of Ardeparin can be decreased when used in combination with Allylestrenol.Approved, Investigational, Withdrawn
ArgatrobanThe therapeutic efficacy of Argatroban can be decreased when used in combination with Allylestrenol.Approved, Investigational
AtazanavirThe metabolism of Allylestrenol can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Allylestrenol can be decreased when combined with Atomoxetine.Approved
BecaplerminThe therapeutic efficacy of Becaplermin can be decreased when used in combination with Allylestrenol.Approved, Investigational
BivalirudinThe therapeutic efficacy of Bivalirudin can be decreased when used in combination with Allylestrenol.Approved, Investigational
BoceprevirThe metabolism of Allylestrenol can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Allylestrenol can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Allylestrenol can be decreased when it is combined with Bosentan.Approved, Investigational
CarbamazepineThe metabolism of Allylestrenol can be increased when combined with Carbamazepine.Approved, Investigational
CeritinibThe serum concentration of Allylestrenol can be increased when it is combined with Ceritinib.Approved
CertoparinThe therapeutic efficacy of Certoparin can be decreased when used in combination with Allylestrenol.Approved, Investigational
Citric AcidThe therapeutic efficacy of Citric Acid can be decreased when used in combination with Allylestrenol.Approved, Nutraceutical, Vet Approved
ClarithromycinThe metabolism of Allylestrenol can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Allylestrenol can be decreased when combined with Clemastine.Approved
ClotrimazoleThe metabolism of Allylestrenol can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Allylestrenol can be decreased when combined with Cobicistat.Approved
Conestat alfaAllylestrenol may increase the thrombogenic activities of Conestat alfa.Approved
ConivaptanThe serum concentration of Allylestrenol can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Allylestrenol can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Allylestrenol can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe therapeutic efficacy of Dabigatran etexilate can be decreased when used in combination with Allylestrenol.Approved
DabrafenibThe serum concentration of Allylestrenol can be decreased when it is combined with Dabrafenib.Approved
DalteparinThe therapeutic efficacy of Dalteparin can be decreased when used in combination with Allylestrenol.Approved
DanaparoidThe therapeutic efficacy of Danaparoid can be decreased when used in combination with Allylestrenol.Approved, Withdrawn
DarexabanThe therapeutic efficacy of Darexaban can be decreased when used in combination with Allylestrenol.Investigational
DarunavirThe metabolism of Allylestrenol can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Allylestrenol can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Allylestrenol can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Allylestrenol can be decreased when combined with Delavirdine.Approved
DesirudinThe therapeutic efficacy of Desirudin can be decreased when used in combination with Allylestrenol.Approved
DextranThe therapeutic efficacy of Dextran can be decreased when used in combination with Allylestrenol.Approved, Vet Approved
Dextran 40The therapeutic efficacy of Dextran 40 can be decreased when used in combination with Allylestrenol.Approved
Dextran 70The therapeutic efficacy of Dextran 70 can be decreased when used in combination with Allylestrenol.Approved
Dextran 75The therapeutic efficacy of Dextran 75 can be decreased when used in combination with Allylestrenol.Approved
DicoumarolThe therapeutic efficacy of Dicoumarol can be decreased when used in combination with Allylestrenol.Approved
DihydroergotamineThe metabolism of Allylestrenol can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Allylestrenol can be decreased when combined with Diltiazem.Approved
DoxycyclineThe metabolism of Allylestrenol can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Allylestrenol can be decreased when combined with Dronedarone.Approved
Edetic AcidThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Allylestrenol.Approved, Vet Approved
EdoxabanThe therapeutic efficacy of Edoxaban can be decreased when used in combination with Allylestrenol.Approved
EnoxaparinThe therapeutic efficacy of Enoxaparin can be decreased when used in combination with Allylestrenol.Approved
EnzalutamideThe serum concentration of Allylestrenol can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Allylestrenol can be decreased when combined with Erythromycin.Approved, Vet Approved
Ethyl biscoumacetateThe therapeutic efficacy of Ethyl biscoumacetate can be decreased when used in combination with Allylestrenol.Withdrawn
Ferulic acidThe therapeutic efficacy of Ferulic acid can be decreased when used in combination with Allylestrenol.Experimental
FluconazoleThe metabolism of Allylestrenol can be decreased when combined with Fluconazole.Approved
FluindioneThe therapeutic efficacy of Fluindione can be decreased when used in combination with Allylestrenol.Investigational
FluvoxamineThe metabolism of Allylestrenol can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxThe therapeutic efficacy of Fondaparinux can be decreased when used in combination with Allylestrenol.Investigational
Fondaparinux sodiumThe therapeutic efficacy of Fondaparinux sodium can be decreased when used in combination with Allylestrenol.Approved, Investigational
FosamprenavirThe metabolism of Allylestrenol can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Allylestrenol can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Allylestrenol can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Allylestrenol can be increased when it is combined with Fusidic Acid.Approved
GabexateThe therapeutic efficacy of Gabexate can be decreased when used in combination with Allylestrenol.Investigational
HeparinThe therapeutic efficacy of Heparin can be decreased when used in combination with Allylestrenol.Approved, Investigational
Human C1-esterase inhibitorAllylestrenol may increase the thrombogenic activities of Human C1-esterase inhibitor.Approved
IdelalisibThe serum concentration of Allylestrenol can be increased when it is combined with Idelalisib.Approved
IdraparinuxThe therapeutic efficacy of Idraparinux can be decreased when used in combination with Allylestrenol.Investigational
ImatinibThe metabolism of Allylestrenol can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Allylestrenol can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Allylestrenol can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Allylestrenol can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Allylestrenol can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Allylestrenol can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Allylestrenol can be decreased when combined with Ketoconazole.Approved, Investigational
LepirudinThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Allylestrenol.Approved
LetaxabanThe therapeutic efficacy of Letaxaban can be decreased when used in combination with Allylestrenol.Investigational
LopinavirThe metabolism of Allylestrenol can be decreased when combined with Lopinavir.Approved
LovastatinThe metabolism of Allylestrenol can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Allylestrenol can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Allylestrenol can be increased when combined with Lumacaftor.Approved
MelagatranThe therapeutic efficacy of Melagatran can be decreased when used in combination with Allylestrenol.Experimental
MifepristoneThe serum concentration of Allylestrenol can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Allylestrenol can be decreased when it is combined with Mitotane.Approved
NadroparinThe therapeutic efficacy of Nadroparin can be decreased when used in combination with Allylestrenol.Approved
NafamostatThe therapeutic efficacy of Nafamostat can be decreased when used in combination with Allylestrenol.Approved, Investigational
NefazodoneThe metabolism of Allylestrenol can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Allylestrenol can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Allylestrenol can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Allylestrenol can be increased when combined with Nevirapine.Approved
NilotinibThe metabolism of Allylestrenol can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Allylestrenol can be decreased when combined with Olaparib.Approved
OsimertinibThe serum concentration of Allylestrenol can be increased when it is combined with Osimertinib.Approved
OtamixabanThe therapeutic efficacy of Otamixaban can be decreased when used in combination with Allylestrenol.Investigational
PalbociclibThe serum concentration of Allylestrenol can be increased when it is combined with Palbociclib.Approved
PentobarbitalThe metabolism of Allylestrenol can be increased when combined with Pentobarbital.Approved, Vet Approved
Pentosan PolysulfateThe therapeutic efficacy of Pentosan Polysulfate can be decreased when used in combination with Allylestrenol.Approved
PhenindioneThe therapeutic efficacy of Phenindione can be decreased when used in combination with Allylestrenol.Approved, Investigational
PhenobarbitalThe metabolism of Allylestrenol can be increased when combined with Phenobarbital.Approved
PhenprocoumonThe therapeutic efficacy of Phenprocoumon can be decreased when used in combination with Allylestrenol.Approved, Investigational
PhenytoinThe metabolism of Allylestrenol can be increased when combined with Phenytoin.Approved, Vet Approved
PosaconazoleThe metabolism of Allylestrenol can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Allylestrenol can be increased when combined with Primidone.Approved, Vet Approved
Protein CThe therapeutic efficacy of Protein C can be decreased when used in combination with Allylestrenol.Approved
Protein S humanThe therapeutic efficacy of Protein S human can be decreased when used in combination with Allylestrenol.Approved
ProtocatechualdehydeThe therapeutic efficacy of Protocatechualdehyde can be decreased when used in combination with Allylestrenol.Approved
RanolazineThe metabolism of Allylestrenol can be decreased when combined with Ranolazine.Approved, Investigational
ReviparinThe therapeutic efficacy of Reviparin can be decreased when used in combination with Allylestrenol.Approved, Investigational
RifabutinThe metabolism of Allylestrenol can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Allylestrenol can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Allylestrenol can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Allylestrenol can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe therapeutic efficacy of Rivaroxaban can be decreased when used in combination with Allylestrenol.Approved
SaquinavirThe metabolism of Allylestrenol can be decreased when combined with Saquinavir.Approved, Investigational
SildenafilThe metabolism of Allylestrenol can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Allylestrenol can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Allylestrenol can be increased when it is combined with Simeprevir.Approved
St. John's WortThe serum concentration of Allylestrenol can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Allylestrenol can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Allylestrenol can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Allylestrenol.Approved, Investigational
TelaprevirThe metabolism of Allylestrenol can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Allylestrenol can be decreased when combined with Telithromycin.Approved
TiclopidineThe metabolism of Allylestrenol can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Allylestrenol can be decreased when it is combined with Tocilizumab.Approved
TroxerutinThe therapeutic efficacy of Troxerutin can be decreased when used in combination with Allylestrenol.Investigational
UlipristalThe therapeutic efficacy of Allylestrenol can be decreased when used in combination with Ulipristal.Approved
VenlafaxineThe metabolism of Allylestrenol can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Allylestrenol can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Allylestrenol can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinThe therapeutic efficacy of Warfarin can be decreased when used in combination with Allylestrenol.Approved
XimelagatranThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Allylestrenol.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Allylestrenol can be decreased when combined with Ziprasidone.Approved
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB15500
KEGG Drug
D01374
KEGG Compound
C12811
PubChem Compound
235905
PubChem Substance
46506946
ChemSpider
205855
ChEBI
31189
ChEMBL
CHEMBL3185133
Therapeutic Targets Database
DPR000085
PharmGKB
PA164745307
ATC Codes
G03DC01 — Allylestrenol

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)80 °CPhysProp
Predicted Properties
PropertyValueSource
Water Solubility0.000558 mg/mLALOGPS
logP5.14ALOGPS
logP4.83ChemAxon
logS-5.7ALOGPS
pKa (Strongest Basic)-0.17ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area20.23 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity93.14 m3·mol-1ChemAxon
Polarizability37.17 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9966
Blood Brain Barrier+0.9817
Caco-2 permeable+0.8469
P-glycoprotein substrateSubstrate0.6615
P-glycoprotein inhibitor IInhibitor0.5781
P-glycoprotein inhibitor IINon-inhibitor0.795
Renal organic cation transporterNon-inhibitor0.6625
CYP450 2C9 substrateNon-substrate0.807
CYP450 2D6 substrateNon-substrate0.9046
CYP450 3A4 substrateSubstrate0.6941
CYP450 1A2 substrateNon-inhibitor0.8345
CYP450 2C9 inhibitorNon-inhibitor0.8006
CYP450 2D6 inhibitorNon-inhibitor0.9427
CYP450 2C19 inhibitorInhibitor0.5498
CYP450 3A4 inhibitorNon-inhibitor0.8408
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6449
Ames testNon AMES toxic0.936
CarcinogenicityNon-carcinogens0.9458
BiodegradationNot ready biodegradable0.9828
Rat acute toxicity2.4200 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6669
hERG inhibition (predictor II)Non-inhibitor0.7541
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as estrane steroids. These are steroids with a structure based on the estrane skeleton.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Estrane steroids
Direct Parent
Estrane steroids
Alternative Parents
17-hydroxysteroids / Delta-4-steroids / Tertiary alcohols / Cyclic alcohols and derivatives / Hydrocarbon derivatives
Substituents
17-hydroxysteroid / Hydroxysteroid / Estrane-skeleton / Delta-4-steroid / Tertiary alcohol / Cyclic alcohol / Organic oxygen compound / Hydrocarbon derivative / Organooxygen compound / Alcohol
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
steroid (CHEBI:31189) / Estrane and derivatives, C21 steroids (gluco/mineralocorticoids, progestogens) and derivatives (C12811) / C21 steroids (gluco/mineralocorticoids, progestogins) and derivatives (LMST02030125)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
Gene Name
PGR
Uniprot ID
P06401
Uniprot Name
Progesterone receptor
Molecular Weight
98979.96 Da
References
  1. Madauss KP, Stewart EL, Williams SP: The evolution of progesterone receptor ligands. Med Res Rev. 2007 May;27(3):374-400. [PubMed:17013809]
  2. Gizard F, Robillard R, Gross B, Barbier O, Revillion F, Peyrat JP, Torpier G, Hum DW, Staels B: TReP-132 is a novel progesterone receptor coactivator required for the inhibition of breast cancer cell growth and enhancement of differentiation by progesterone. Mol Cell Biol. 2006 Oct;26(20):7632-44. [PubMed:17015480]
  3. Wu HB, Fabian S, Jenab S, Quinones-Jenab V: Progesterone receptors activation after acute cocaine administration. Brain Res. 2006 Dec 18;1126(1):188-92. Epub 2006 Nov 15. [PubMed:17109827]
  4. Boonyaratanakornkit V, McGowan E, Sherman L, Mancini MA, Cheskis BJ, Edwards DP: The role of extranuclear signaling actions of progesterone receptor in mediating progesterone regulation of gene expression and the cell cycle. Mol Endocrinol. 2007 Feb;21(2):359-75. Epub 2006 Nov 30. [PubMed:17138644]
  5. Tranguch S, Smith DF, Dey SK: Progesterone receptor requires a co-chaperone for signalling in uterine biology and implantation. Reprod Biomed Online. 2006 Nov;13(5):651-60. [PubMed:17169175]
  6. Bergink EW, Loonen PB, Kloosterboer HJ: Receptor binding of allylestrenol, a progestagen of the 19-nortestosterone series without androgenic properties. J Steroid Biochem. 1985 Aug;23(2):165-8. [PubMed:3928974]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da
References
  1. Kumar AS, Cureton E, Shim V, Sakata T, Moore DH, Benz CC, Esserman LJ, Hwang ES: Type and duration of exogenous hormone use affects breast cancer histology. Ann Surg Oncol. 2007 Feb;14(2):695-703. Epub 2006 Nov 14. [PubMed:17103262]
  2. Lessey BA, Palomino WA, Apparao KB, Young SL, Lininger RA: Estrogen receptor-alpha (ER-alpha) and defects in uterine receptivity in women. Reprod Biol Endocrinol. 2006;4 Suppl 1:S9. [PubMed:17118173]
  3. Yuri T, Tsukamoto R, Uehara N, Matsuoka Y, Tsubura A: Effects of different durations of estrogen and progesterone treatment on development of N-methyl-N-nitrosourea-induced mammary carcinomas in female Lewis rats. In Vivo. 2006 Nov-Dec;20(6B):829-36. [PubMed:17203775]
  4. Montero Girard G, Vanzulli SI, Cerliani JP, Bottino MC, Bolado J, Vela J, Becu-Villalobos D, Benavides F, Gutkind S, Patel V, Molinolo A, Lanari C: Association of estrogen receptor-alpha and progesterone receptor A expression with hormonal mammary carcinogenesis: role of the host microenvironment. Breast Cancer Res. 2007;9(2):R22. [PubMed:17341305]
  5. Ghebeh H, Tulbah A, Mohammed S, Elkum N, Bin Amer SM, Al-Tweigeri T, Dermime S: Expression of B7-H1 in breast cancer patients is strongly associated with high proliferative Ki-67-expressing tumor cells. Int J Cancer. 2007 Aug 15;121(4):751-8. [PubMed:17415709]
  6. Csaba G, Gonda AI, Karabelyos C: Contraceptive treatment increases the affinity of uterine estrogen receptor in adult rat: perinatal gestagen treatment changes the reaction. Horm Metab Res. 1996 Jan;28(1):16-9. [PubMed:8820988]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on July 24, 2007 10:58 / Updated on November 09, 2017 02:59