Identification
- Generic Name
- Genistein
- DrugBank Accession Number
- DB01645
- Background
An isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA topoisomerases, type II) activity and is used as an antineoplastic and antitumor agent. Experimentally, it has been shown to induce G2 phase arrest in human and murine cell lines.
Additionally, genistein has antihelmintic activity. It has been determined to be the active ingredient in Felmingia vestita, which is a plant traditionally used against worms. It has shown to be effective in the treatment of common liver fluke, pork trematode and poultry cestode.
Further, genistein is a phytoestrogen which has selective estrogen receptor modulator properties. It has been investigated in clinical trials as an alternative to classical hormone therapy to help prevent cardiovascular disease in postmenopausal women 1.
Natural sources of genistein include tofu, fava beans, soybeans, kudzu, and lupin.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for Genistein (DB01645)
- Weight
- Average: 270.2369
Monoisotopic: 270.05282343 - Chemical Formula
- C15H10O5
- Synonyms
- 4',5,7-trihydroxyisoflavone
- 4H-1-BENZOPYRAN-4-ONE, 5,7-DIHYDROXY-3-(4-HYDROXYPHENYL)-
- 5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one
- 5,7-dihydroxy-3-(4-hydroxyphenyl)-chromen-4-one
- 5,7,4'-trihydroxyisoflavone
- Genistein
- Genisteol
- Genisterin
- External IDs
- BIO-300
- FW-635I-2
- NPI-031L
- NSC-36586
- SIPI-807-1
Pharmacology
- Indication
Currently Genistein is being studied in clinical trials as a treatment for prostate cancer.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prevention of Calcium deficiency ••• ••• ••••••• •••••••••••• Prevention of Deficiency, vitamin d ••• ••• ••••••• •••••••••••• Treatment of Osteodystrophy ••• ••• ••••••• •••••••••••• Prevention of Osteodystrophy ••• ••• ••••••• •••••••••••• Treatment of Osteomalacia ••• ••• ••••••• •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Not Available
- Mechanism of action
Genistein may inhibit cancer cell growth by blocking enzymes required for cell growth.
Genistein may decrease cardiovascular risk in postmenopausal women by interacting with the nuclear estrogen receptors to alter the transcription of cell specific genes. In randomized clinical trials, genistein was seen to increase the ratio of nitric oxide to endothelin and improved flow-mediated endothelium dependent vasodilation in healthy postmenopausal women 1. In addition, genistein may have beneficial effects on glucose metabolism by inhibiting islet tyrosine kinase activity as well as insulin release dependent on glucose and sulfonylurea 1.
Target Actions Organism UNuclear receptor coactivator 1 Not Available Humans UEstrogen receptor alpha Not Available Humans UNuclear receptor coactivator 2 Not Available Humans USteroid hormone receptor ERR2 agonistHumans USteroid hormone receptor ERR1 agonistHumans UNuclear receptor subfamily 1 group I member 2 Not Available Humans URAC-alpha serine/threonine-protein kinase Not Available Humans UG-protein coupled estrogen receptor 1 Not Available Humans UCytochrome P450 1B1 Not Available Humans USex hormone-binding globulin Not Available Humans UEstrogen receptor beta Not Available Humans UDNA topoisomerase 2-alpha Not Available Humans UProtein-tyrosine kinase 2-beta Not Available Humans UCystic fibrosis transmembrane conductance regulator activatorHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Hover over products below to view reaction partners
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Genistein can be increased when it is combined with Abametapir. Abatacept The metabolism of Genistein can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Genistein. Abiraterone The serum concentration of Genistein can be increased when it is combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Genistein. - Food Interactions
- Not Available
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Prunetol / Sophoricol
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image CALCİDAY G 1000 MG/880 IU/50 MG EFERVESAN TABLET, 40 ADET Genistein (50 mg) + Calcium carbonate (1000 mg) + Cholecalciferol (880 iu) Tablet, effervescent Oral NUVOMED İLAÇ SAN.TİC. A.Ş. 2020-08-14 Not applicable Turkey 
CALCIDAY G 1200 MG/800 IU/50 MG EFERVESAN TABLET, 45 ADET Genistein (50 mg) + Calcium (1200 mg) + Cholecalciferol (800 iu) Tablet, effervescent Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2020-08-14 Not applicable Turkey OSMEGA 600 MG/400 IU/25 MG EFERVESAN TABLET, 30 ADET Genistein (25 mg) + Calcium (600 mg) + Cholecalciferol (400 iu) Tablet, effervescent Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2011-10-04 Not applicable Turkey OSMEGA 600 MG/400 IU/25 MG EFERVESAN TABLET, 60 ADET Genistein (25 mg) + Calcium (600 mg) + Cholecalciferol (400 iu) Tablet, effervescent Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2011-10-04 Not applicable Turkey
Categories
- Drug Categories
- Anticarcinogenic Agents
- Antineoplastic Agents
- BCRP/ABCG2 Inhibitors
- Benzopyrans
- Chromones
- Compounds used in a research, industrial, or household setting
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (weak)
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (moderate)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (weak)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Enzyme Inhibitors
- Estrogens, Non-Steroidal
- Flavonoids
- Heterocyclic Compounds, Fused-Ring
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Isoflavones
- OATP1B1/SLCO1B1 Inhibitors
- Organic Anion Transporting Polypeptide 2B1 Inhibitors
- P-glycoprotein inhibitors
- Phytoestrogens
- Protective Agents
- Protein Kinase Inhibitors
- Pyrans
- Tyrosine Kinase Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as isoflavones. These are polycyclic compounds containing a 2-isoflavene skeleton which bears a ketone group at the C4 carbon atom.
- Kingdom
- Organic compounds
- Super Class
- Phenylpropanoids and polyketides
- Class
- Isoflavonoids
- Sub Class
- Isoflav-2-enes
- Direct Parent
- Isoflavones
- Alternative Parents
- Hydroxyisoflavonoids / Chromones / Pyranones and derivatives / 1-hydroxy-4-unsubstituted benzenoids / 1-hydroxy-2-unsubstituted benzenoids / Benzene and substituted derivatives / Vinylogous acids / Heteroaromatic compounds / Oxacyclic compounds / Organooxygen compounds show 2 more
- Substituents
- 1-benzopyran / 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / Aromatic heteropolycyclic compound / Benzenoid / Benzopyran / Chromone / Heteroaromatic compound / Hydrocarbon derivative / Hydroxyisoflavonoid show 11 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- 7-hydroxyisoflavones (CHEBI:28088) / isoflavones, Isoflavonoids (C06563) / Isoflavonoids (LMPK12050218)
- Affected organisms
- Humans and other mammals
- Helminthic Microorganisms
- Parasitic nematodes and other roundworms
Chemical Identifiers
- UNII
- DH2M523P0H
- CAS number
- 446-72-0
- InChI Key
- TZBJGXHYKVUXJN-UHFFFAOYSA-N
- InChI
- InChI=1S/C15H10O5/c16-9-3-1-8(2-4-9)11-7-20-13-6-10(17)5-12(18)14(13)15(11)19/h1-7,16-18H
- IUPAC Name
- 5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one
- SMILES
- OC1=CC=C(C=C1)C1=COC2=C(C(O)=CC(O)=C2)C1=O
References
- Synthesis Reference
J. Mark Weber, Andreas Constantinou, Paul E. Hessler, "Process of preparing genistein." U.S. Patent US5554519, issued June, 1994.
US5554519- General References
- Crisafulli A, Altavilla D, Marini H, Bitto A, Cucinotta D, Frisina N, Corrado F, D'Anna R, Squadrito G, Adamo EB, Marini R, Romeo A, Cancellieri F, Buemi M, Squadrito F: Effects of the phytoestrogen genistein on cardiovascular risk factors in postmenopausal women. Menopause. 2005 Mar;12(2):186-92. [Article]
- Toner E, Brennan GP, Wells K, McGeown JG, Fairweather I: Physiological and morphological effects of genistein against the liver fluke, Fasciola hepatica. Parasitology. 2008 Sep;135(10):1189-203. doi: 10.1017/S0031182008004630. [Article]
- External Links
- Human Metabolome Database
- HMDB0003217
- KEGG Compound
- C06563
- PubChem Compound
- 5280961
- PubChem Substance
- 46509060
- ChemSpider
- 4444448
- BindingDB
- 19459
- 25696
- ChEBI
- 28088
- ChEMBL
- CHEMBL44
- ZINC
- ZINC000018825330
- Therapeutic Targets Database
- DCL000330
- PharmGKB
- PA165109660
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- GEN
- Wikipedia
- Genistein
- PDB Entries
- 1qkm / 1x7j / 1x7r / 2qa8 / 3kgt / 3kgu / 4fj1 / 5auz / 5av4 / 5kda … show 3 more
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 2 Active Not Recruiting Treatment Bladder Cancer 1 2 Completed Prevention Bone Diseases / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Depression / Myocardial Ischemia / Osteoporosis / Postmenopausal 1 2 Completed Prevention Breast Cancer 1 2 Completed Treatment Adenocarcinoma of Prostate / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer 1 2 Completed Treatment Breast Cancer 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, effervescent Oral Capsule Oral Tablet, orally disintegrating Oral 30 mg/1 - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 301.5 dec °C PhysProp - Predicted Properties
Property Value Source Water Solubility 0.123 mg/mL ALOGPS logP 3.04 ALOGPS logP 3.08 Chemaxon logS -3.3 ALOGPS pKa (Strongest Acidic) 6.55 Chemaxon pKa (Strongest Basic) -5.3 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 86.99 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 71.68 m3·mol-1 Chemaxon Polarizability 26.59 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9877 Blood Brain Barrier + 0.6785 Caco-2 permeable + 0.7002 P-glycoprotein substrate Substrate 0.5 P-glycoprotein inhibitor I Non-inhibitor 0.9288 P-glycoprotein inhibitor II Non-inhibitor 0.7828 Renal organic cation transporter Non-inhibitor 0.9075 CYP450 2C9 substrate Non-substrate 0.7672 CYP450 2D6 substrate Non-substrate 0.9105 CYP450 3A4 substrate Non-substrate 0.6821 CYP450 1A2 substrate Inhibitor 0.9254 CYP450 2C9 inhibitor Inhibitor 0.8949 CYP450 2D6 inhibitor Non-inhibitor 0.9232 CYP450 2C19 inhibitor Inhibitor 0.8881 CYP450 3A4 inhibitor Inhibitor 0.796 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.8009 Ames test Non AMES toxic 0.9638 Carcinogenicity Non-carcinogens 0.9276 Biodegradation Not ready biodegradable 0.8572 Rat acute toxicity 3.2988 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9569 hERG inhibition (predictor II) Non-inhibitor 0.8917
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 171.7192907 predictedDarkChem Lite v0.1.0 [M-H]- 161.1052285 predictedDarkChem Lite v0.1.0 [M-H]- 170.2301907 predictedDarkChem Lite v0.1.0 [M-H]- 171.8592907 predictedDarkChem Lite v0.1.0 [M-H]- 158.3607 predictedDeepCCS 1.0 (2019) [M+H]+ 173.6543907 predictedDarkChem Lite v0.1.0 [M+H]+ 159.9063086 predictedDarkChem Lite v0.1.0 [M+H]+ 172.2131907 predictedDarkChem Lite v0.1.0 [M+H]+ 173.0464907 predictedDarkChem Lite v0.1.0 [M+H]+ 160.7187 predictedDeepCCS 1.0 (2019) [M+Na]+ 171.7683907 predictedDarkChem Lite v0.1.0 [M+Na]+ 165.5106977 predictedDarkChem Lite v0.1.0 [M+Na]+ 171.5011907 predictedDarkChem Lite v0.1.0 [M+Na]+ 171.6346907 predictedDarkChem Lite v0.1.0 [M+Na]+ 166.81186 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Transcription coactivator activity
- Specific Function
- Nuclear receptor coactivator that directly binds nuclear receptors and stimulates the transcriptional activities in a hormone-dependent fashion. Involved in the coactivation of different nuclear re...
- Gene Name
- NCOA1
- Uniprot ID
- Q15788
- Uniprot Name
- Nuclear receptor coactivator 1
- Molecular Weight
- 156755.44 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Transcription coactivator activity
- Specific Function
- Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to ...
- Gene Name
- NCOA2
- Uniprot ID
- Q15596
- Uniprot Name
- Nuclear receptor coactivator 2
- Molecular Weight
- 159155.645 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- Nuclear receptor, may regulate ESR1 transcriptional activity. Induces the expression of PERM1 in the skeletal muscle.
- Gene Name
- ESRRB
- Uniprot ID
- O95718
- Uniprot Name
- Steroid hormone receptor ERR2
- Molecular Weight
- 56207.085 Da
References
- Suetsugi M, Su L, Karlsberg K, Yuan YC, Chen S: Flavone and isoflavone phytoestrogens are agonists of estrogen-related receptors. Mol Cancer Res. 2003 Nov;1(13):981-91. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- Binds to an ERR-alpha response element (ERRE) containing a single consensus half-site, 5'-TNAAGGTCA-3'. Can bind to the medium-chain acyl coenzyme A dehydrogenase (MCAD) response element NRRE-1 and...
- Gene Name
- ESRRA
- Uniprot ID
- P11474
- Uniprot Name
- Steroid hormone receptor ERR1
- Molecular Weight
- 45509.11 Da
References
- Suetsugi M, Su L, Karlsberg K, Yuan YC, Chen S: Flavone and isoflavone phytoestrogens are agonists of estrogen-related receptors. Mol Cancer Res. 2003 Nov;1(13):981-91. [Article]
- Chen S, Ye J, Kijima I, Kinoshita Y, Zhou D: Positive and negative transcriptional regulation of aromatase expression in human breast cancer tissue. J Steroid Biochem Mol Biol. 2005 May;95(1-5):17-23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism an...
- Gene Name
- NR1I2
- Uniprot ID
- O75469
- Uniprot Name
- Nuclear receptor subfamily 1 group I member 2
- Molecular Weight
- 49761.245 Da
References
- Kretschmer XC, Baldwin WS: CAR and PXR: xenosensors of endocrine disrupters? Chem Biol Interact. 2005 Aug 15;155(3):111-28. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Protein serine/threonine/tyrosine kinase activity
- Specific Function
- AKT1 is one of 3 closely related serine/threonine-protein kinases (AKT1, AKT2 and AKT3) called the AKT kinase, and which regulate many processes including metabolism, proliferation, cell survival, ...
- Gene Name
- AKT1
- Uniprot ID
- P31749
- Uniprot Name
- RAC-alpha serine/threonine-protein kinase
- Molecular Weight
- 55686.035 Da
References
- Barve V, Ahmed F, Adsule S, Banerjee S, Kulkarni S, Katiyar P, Anson CE, Powell AK, Padhye S, Sarkar FH: Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells. J Med Chem. 2006 Jun 29;49(13):3800-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Steroid hormone binding
- Specific Function
- G-protein coupled estrogen receptor that binds to 17-beta-estradiol (E2) with high affinity, leading to rapid and transient activation of numerous intracellular signaling pathways. Stimulates cAMP ...
- Gene Name
- GPER1
- Uniprot ID
- Q99527
- Uniprot Name
- G-protein coupled estrogen receptor 1
- Molecular Weight
- 42247.12 Da
References
- Thomas P, Dong J: Binding and activation of the seven-transmembrane estrogen receptor GPR30 by environmental estrogens: a potential novel mechanism of endocrine disruption. J Steroid Biochem Mol Biol. 2006 Dec;102(1-5):175-9. Epub 2006 Nov 7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Oxygen binding
- 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 oxidizes a variety of structurally un...
- Gene Name
- CYP1B1
- Uniprot ID
- Q16678
- Uniprot Name
- Cytochrome P450 1B1
- Molecular Weight
- 60845.33 Da
References
- Shimada T, Tanaka K, Takenaka S, Murayama N, Martin MV, Foroozesh MK, Yamazaki H, Guengerich FP, Komori M: Structure-function relationships of inhibition of human cytochromes P450 1A1, 1A2, 1B1, 2C9, and 3A4 by 33 flavonoid derivatives. Chem Res Toxicol. 2010 Dec 20;23(12):1921-35. doi: 10.1021/tx100286d. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Androgen binding
- Specific Function
- Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone...
- Gene Name
- SHBG
- Uniprot ID
- P04278
- Uniprot Name
- Sex hormone-binding globulin
- Molecular Weight
- 43778.755 Da
References
- Hong H, Branham WS, Ng HW, Moland CL, Dial SL, Fang H, Perkins R, Sheehan D, Tong W: Human sex hormone-binding globulin binding affinities of 125 structurally diverse chemicals and comparison with their binding to androgen receptor, estrogen receptor, and alpha-fetoprotein. Toxicol Sci. 2015 Feb;143(2):333-48. doi: 10.1093/toxsci/kfu231. Epub 2014 Oct 27. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent m...
- Gene Name
- ESR2
- Uniprot ID
- Q92731
- Uniprot Name
- Estrogen receptor beta
- Molecular Weight
- 59215.765 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Ubiquitin binding
- Specific Function
- Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segr...
- Gene Name
- TOP2A
- Uniprot ID
- P11388
- Uniprot Name
- DNA topoisomerase 2-alpha
- Molecular Weight
- 174383.88 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Signal transducer activity
- Specific Function
- Non-receptor protein-tyrosine kinase that regulates reorganization of the actin cytoskeleton, cell polarization, cell migration, adhesion, spreading and bone remodeling. Plays a role in the regulat...
- Gene Name
- PTK2B
- Uniprot ID
- Q14289
- Uniprot Name
- Protein-tyrosine kinase 2-beta
- Molecular Weight
- 115873.62 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Activator
- General Function
- Pdz domain binding
- Specific Function
- Involved in the transport of chloride ions. May regulate bicarbonate secretion and salvage in epithelial cells by regulating the SLC4A7 transporter. Can inhibit the chloride channel activity of ANO...
- Gene Name
- CFTR
- Uniprot ID
- P13569
- Uniprot Name
- Cystic fibrosis transmembrane conductance regulator
- Molecular Weight
- 168139.895 Da
References
- Roomans GM: Pharmacological approaches to correcting the ion transport defect in cystic fibrosis. Am J Respir Med. 2003;2(5):413-31. doi: 10.1007/BF03256668. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- 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 oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Hu M, Krausz K, Chen J, Ge X, Li J, Gelboin HL, Gonzalez FJ: Identification of CYP1A2 as the main isoform for the phase I hydroxylated metabolism of genistein and a prodrug converting enzyme of methylated isoflavones. Drug Metab Dispos. 2003 Jul;31(7):924-31. [Article]
- Xu X, Duncan AM, Merz BE, Kurzer MS: Effects of soy isoflavones on estrogen and phytoestrogen metabolism in premenopausal women. Cancer Epidemiol Biomarkers Prev. 1998 Dec;7(12):1101-8. [Article]
- Shimada H, Eto M, Ohtaguro M, Ohtsubo M, Mizukami Y, Ide T, Imamura Y: Differential mechanisms for the inhibition of human cytochrome P450 1A2 by apigenin and genistein. J Biochem Mol Toxicol. 2010 Jul-Aug;24(4):230-4. doi: 10.1002/jbt.20328. [Article]
- Breinholt VM, Rasmussen SE, Brosen K, Friedberg TH: In vitro metabolism of genistein and tangeretin by human and murine cytochrome P450s. Pharmacol Toxicol. 2003 Jul;93(1):14-22. [Article]
- Daily Med, Genistein [Link]
- Kind
- Protein
- Organism
- Rat
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
- Specific Function
- Aromatase activity
- Gene Name
- Cyp1a1
- Uniprot ID
- P00185
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 59392.695 Da
References
- Xu X, Duncan AM, Merz BE, Kurzer MS: Effects of soy isoflavones on estrogen and phytoestrogen metabolism in premenopausal women. Cancer Epidemiol Biomarkers Prev. 1998 Dec;7(12):1101-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid 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 oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid 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 oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Kopecna-Zapletalova M, Krasulova K, Anzenbacher P, Hodek P, Anzenbacherova E: Interaction of isoflavonoids with human liver microsomal cytochromes P450: inhibition of CYP enzyme activities. Xenobiotica. 2017 Apr;47(4):324-331. doi: 10.1080/00498254.2016.1195028. Epub 2016 Jun 17. [Article]
- Kind
- Protein
- Organism
- Rat
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Testosterone 6-beta-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 oxidizes a variety of structurally un...
- Gene Name
- Cyp3a1
- Uniprot ID
- P04800
- Uniprot Name
- Cytochrome P450 3A1
- Molecular Weight
- 57917.375 Da
References
- Jager W, Sartori M, Herzog W, Thalhammer T: Genistein metabolism in liver microsomes of Wistar and mutant TR(-)-rats. Res Commun Mol Pathol Pharmacol. 1998 Apr;100(1):105-16. [Article]
- Kind
- Protein
- Organism
- Rat
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Testosterone 6-beta-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 oxidizes a variety of structurally un...
- Gene Name
- Cyp3a2
- Uniprot ID
- P05183
- Uniprot Name
- Cytochrome P450 3A2
- Molecular Weight
- 57731.215 Da
References
- Jager W, Sartori M, Herzog W, Thalhammer T: Genistein metabolism in liver microsomes of Wistar and mutant TR(-)-rats. Res Commun Mol Pathol Pharmacol. 1998 Apr;100(1):105-16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- 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
- Xiao CQ, Chen R, Lin J, Wang G, Chen Y, Tan ZR, Zhou HH: Effect of genistein on the activities of cytochrome P450 3A and P-glycoprotein in Chinese healthy participants. Xenobiotica. 2012 Feb;42(2):173-8. doi: 10.3109/00498254.2011.615954. Epub 2011 Sep 26. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Identical protein binding
- Specific Function
- Thyroid hormone-binding protein. Probably transports thyroxine from the bloodstream to the brain.
- Gene Name
- TTR
- Uniprot ID
- P02766
- Uniprot Name
- Transthyretin
- Molecular Weight
- 15886.88 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Castro AF, Altenberg GA: Inhibition of drug transport by genistein in multidrug-resistant cells expressing P-glycoprotein. Biochem Pharmacol. 1997 Jan 10;53(1):89-93. [Article]
- Versantvoort CH, Rhodes T, Twentyman PR: Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds. Br J Cancer. 1996 Dec;74(12):1949-54. [Article]
- Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transporter activity
- Specific Function
- Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
- Gene Name
- ABCC1
- Uniprot ID
- P33527
- Uniprot Name
- Multidrug resistance-associated protein 1
- Molecular Weight
- 171589.5 Da
References
- Pec MK, Aguirre A, Fernandez JJ, Souto ML, Dorta JF, Villar J: Dehydrothyrsiferol does not modulate multidrug resistance-associated protein 1 resistance: a functional screening system for MRP1 substrates. Int J Mol Med. 2002 Nov;10(5):605-8. [Article]
- Nguyen H, Zhang S, Morris ME: Effect of flavonoids on MRP1-mediated transport in Panc-1 cells. J Pharm Sci. 2003 Feb;92(2):250-7. [Article]
- Hong J, Lambert JD, Lee SH, Sinko PJ, Yang CS: Involvement of multidrug resistance-associated proteins in regulating cellular levels of (-)-epigallocatechin-3-gallate and its methyl metabolites. Biochem Biophys Res Commun. 2003 Oct 10;310(1):222-7. [Article]
- Versantvoort CH, Rhodes T, Twentyman PR: Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds. Br J Cancer. 1996 Dec;74(12):1949-54. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- Imai Y, Tsukahara S, Asada S, Sugimoto Y: Phytoestrogens/flavonoids reverse breast cancer resistance protein/ABCG2-mediated multidrug resistance. Cancer Res. 2004 Jun 15;64(12):4346-52. [Article]
- Zhang S, Yang X, Morris ME: Flavonoids are inhibitors of breast cancer resistance protein (ABCG2)-mediated transport. Mol Pharmacol. 2004 May;65(5):1208-16. [Article]
- Perez M, Real R, Mendoza G, Merino G, Prieto JG, Alvarez AI: Milk secretion of nitrofurantoin, as a specific BCRP/ABCG2 substrate, in assaf sheep: modulation by isoflavones. J Vet Pharmacol Ther. 2009 Oct;32(5):498-502. doi: 10.1111/j.1365-2885.2008.01050.x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
- Gene Name
- SLCO2B1
- Uniprot ID
- O94956
- Uniprot Name
- Solute carrier organic anion transporter family member 2B1
- Molecular Weight
- 76709.98 Da
References
- Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [Article]
Drug created at June 13, 2005 13:24 / Updated at September 12, 2023 18:32