Tauroursodeoxycholic acid
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Identification
- Summary
Tauroursodeoxycholic acid is the taurine conjugate of ursodeoxycholic acid with antiapoptotic and ER stress response dampening effects used in some countries to treat gallstones. It is also being investigated for a wide variety of other conditions.
- Brand Names
- Relyvrio
- Generic Name
- Tauroursodeoxycholic acid
- DrugBank Accession Number
- DB08834
- Background
Tauroursodeoxycholic acid, also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid 3 that is produced in humans at a low concentration.3 It is a taurine conjugate of ursodeoxycholic acid 2 with comparable therapeutic efficacy and safety,3 but a much higher hydrophilicity.1 Normally, hydrophilic bile acids regulates hydrophobic bile acids and their cytotoxic effects. Tauroursodeoxycholic acid can reduce the absorption of cholesterol in the small intestine, thereby reducing the body's intake of dietary cholesterol and the body cholesterol content.4
Tauroursodeoxycholic acid is currently used in Europe to treat and prevent gallstones as a bile acid derivative.7 Due to a range of its molecular properties - namely its anti-apoptotic effects - tauroursodeoxycholic acid has been examined in inflammatory metabolic diseases and neurodegenerative diseases.2,3
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 499.71
Monoisotopic: 499.296759347 - Chemical Formula
- C26H45NO6S
- Synonyms
- Tauroursodeoxycholate
- Tauroursodesoxycholic acid
- Taurursodiol
- TUDCA
- Ursodeoxycholyltaurine
- Ursodoxicoltaurine
- External IDs
- UR-906
Pharmacology
- Indication
Tauroursodeoxycholic acid is used to prevent and treat gallstone formation.7
Tauroursodeoxycholic acid is used in combination with phenylbutyric acid to treat amyotrophic lateral sclerosis (ALS) in adults.8,9
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 Used in combination to manage Amyotrophic lateral sclerosis (als) Combination Product in combination with: Phenylbutyric acid (DB06819) •••••••••••• ••••• •••••••••• Used in combination to manage Amyotrophic lateral sclerosis (als) Combination Product in combination with: Phenylbutyric acid (DB06819) •••••••••••• Treatment of Gallstone formation •••••••••••• ••••••• Prevention of Gallstone formation •••••••••••• ••••••• - 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
Tauroursodeoxycholic acid works to decrease bile acid 1 and cholesterol levels.4 It reduces the cholesterol content and increases the bile acid content in gallbladder bile to prevent the formation of cholesterol gallstones.4
Tauroursodeoxycholic acid possesses anti-apoptotic and anti-inflammatory properties. These findings provoked the investigations of tauroursodeoxycholic acid as a potential therapeutic agent for neurodegenerative diseases, such as amyotrophic lateral sclerosis, Alzheimer's disease, and Parkinson's disease.2 Other studies also suggest that tauroursodeoxycholic acid can promote angiogenesis and suppress adipogenesis of adipose-derived mesenchymal stem cells (MSCs). Anti-osteoporotic effects of tauroursodeoxycholic acid have also been documented, as it was shown to enhance osteogenic differentiation of bone marrow-derived MSCs.3
- Mechanism of action
About 90% of gallstones are formed by cholesterol, which may be caused by altered gut microbiota from a high-fat diet and other factors. The gut microbiota regulates bile acid metabolism; thus, altered composition in gut microbiota may significantly change the bile acid pool and alter cholesterol secretion.4
While the exact mechanism of action of tauroursodeoxycholic acid in reducing and preventing gallstone formation is unclear, tauroursodeoxycholic acid may achieve this effect in a number of ways. A recent mouse study suggests that tauroursodeoxycholic acid inhibits intestinal cholesterol absorption and lowers liver cholesterol levels by upregulating the bile acid excretion from the liver to the gallbladder. Tauroursodeoxycholic acid lowers the bile cholesterol saturation in the gallbladder, thereby increasing the solubility of cholesterol in bile. It can also maintain a specific gut microbiota composition to promote the synthesis of bile acids and reduce liver inflammation caused by the lipopolysaccharide in the blood. Ultimately, tauroursodeoxycholic acid enhances the synthesis of bile acids in the liver and reduces cholesterol in the serum and liver.4
Tauroursodeoxycholic acid inhibits cell apoptosis by disrupting the mitochondrial pathway of cell death. It works by inhibiting oxygen-radical production, ameliorating endoplasmic reticulum (ER) stress, and stabilizing the unfolded protein response. Other anti-apoptotic processes mediated by tauroursodeoxycholic acid include cytochrome c release, caspase activation, DNA and nuclear fragmentation, and inhibition of p53 transactivation. It is believed that tauroursodeoxycholic acid works on multiple cellular targets to inhibit apoptosis and upregulate survival pathways.2
Target Actions Organism UIntegrin alpha-5 activatorHumans - Absorption
Not Available
- Volume of distribution
There is evidence that tauroursodeoxycholic acid crosses the blood brain barrier in humans.2
- Protein binding
Not Available
- Metabolism
There is little biotransformation of tauroursodeoxycholic acid. It is partially deconjugated by intestinal microflora to form unconjugated bile acids.5,6
- 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
There is no information available regarding the LD50 and overdose of tauroursodeoxycholic acid.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Tauroursodeoxycholic acid. Acenocoumarol The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Tauroursodeoxycholic acid. Acetylsalicylic acid The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Tauroursodeoxycholic acid. Alteplase The risk or severity of bleeding and bruising can be increased when Alteplase is combined with Tauroursodeoxycholic acid. Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Tauroursodeoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. - Food Interactions
- No interactions found.
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.
- Product Ingredients
Ingredient UNII CAS InChI Key Tauroursodeoxycholic acid dihydrate U7XRV7RZ1I 117609-50-4 BNXLUNVCHFIPFY-GUBAPICVSA-N - International/Other Brands
- Tauro (Teofarma) / Taurolite (Bio-Gen)
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Albrioza Tauroursodeoxycholic acid (1 g / sachet) + Sodium phenylbutyrate (3 g / sachet) Powder, for suspension Oral Amylyx Pharmaceuticals Inc 2022-07-29 2024-09-23 Canada Relyvrio Tauroursodeoxycholic acid dihydrate (1 g/1) + Sodium phenylbutyrate (3 g/1) Powder, for suspension Oral Amylyx Pharmaceuticals Inc 2022-09-29 2025-02-28 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image TAUROLITE 250 MG 100 KAPSUL Tauroursodeoxycholic acid (250 mg) Capsule Oral BİO-GEN İLAÇ SAN.TİC.LTD. ŞTİ. 2018-12-25 Not applicable Turkey
Categories
- ATC Codes
- N07XX19 — Sodium phenylbutyrate and ursodoxicoltaurine
- N07XX — Other nervous system drugs
- N07X — OTHER NERVOUS SYSTEM DRUGS
- N07 — OTHER NERVOUS SYSTEM DRUGS
- N — NERVOUS SYSTEM
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as taurinated bile acids and derivatives. These are bile acid derivatives containing a taurine conjugated to the bile acid moiety.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Bile acids, alcohols and derivatives
- Direct Parent
- Taurinated bile acids and derivatives
- Alternative Parents
- Dihydroxy bile acids, alcohols and derivatives / 7-alpha-hydroxysteroids / 3-alpha-hydroxysteroids / N-acyl amines / Sulfonyls / Organosulfonic acids / Alkanesulfonic acids / Secondary carboxylic acid amides / Secondary alcohols / Cyclic alcohols and derivatives show 5 more
- Substituents
- 3-alpha-hydroxysteroid / 3-hydroxysteroid / 7-alpha-hydroxysteroid / 7-hydroxysteroid / Alcohol / Aliphatic homopolycyclic compound / Alkanesulfonic acid / Carbonyl group / Carboxamide group / Carboxylic acid derivative show 22 more
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- bile acid taurine conjugate (CHEBI:80774) / Taurine conjugates (LMST05040015)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 60EUX8MN5X
- CAS number
- 14605-22-2
- InChI Key
- BHTRKEVKTKCXOH-LBSADWJPSA-N
- InChI
- InChI=1S/C26H45NO6S/c1-16(4-7-23(30)27-12-13-34(31,32)33)19-5-6-20-24-21(9-11-26(19,20)3)25(2)10-8-18(28)14-17(25)15-22(24)29/h16-22,24,28-29H,4-15H2,1-3H3,(H,27,30)(H,31,32,33)/t16-,17+,18-,19-,20+,21+,22+,24+,25+,26-/m1/s1
- IUPAC Name
- 2-[(4R)-4-[(1S,2S,5R,7S,9S,10R,11S,14R,15R)-5,9-dihydroxy-2,15-dimethyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadecan-14-yl]pentanamido]ethane-1-sulfonic acid
- SMILES
- [H][C@@]12CC[C@H]([C@H](C)CCC(=O)NCCS(O)(=O)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])[C@@H](O)C[C@]2([H])C[C@H](O)CC[C@]12C
References
- Synthesis Reference
Zhuo, Chao; Feng, Wei; Wu, Da-jun; Xiong, Zhi-gang. Synthesis of tauroursodeoxycholic acid. Hecheng Huaxue (2002), 10(5), 444-446.
- General References
- Crosignani A, Battezzati PM, Setchell KD, Invernizzi P, Covini G, Zuin M, Podda M: Tauroursodeoxycholic acid for treatment of primary biliary cirrhosis. A dose-response study. Dig Dis Sci. 1996 Apr;41(4):809-15. doi: 10.1007/BF02213140. [Article]
- Vang S, Longley K, Steer CJ, Low WC: The Unexpected Uses of Urso- and Tauroursodeoxycholic Acid in the Treatment of Non-liver Diseases. Glob Adv Health Med. 2014 May;3(3):58-69. doi: 10.7453/gahmj.2014.017. [Article]
- Ahn TK, Kim KT, Joshi HP, Park KH, Kyung JW, Choi UY, Sohn S, Sheen SH, Shin DE, Lee SH, Han IB: Therapeutic Potential of Tauroursodeoxycholic Acid for the Treatment of Osteoporosis. Int J Mol Sci. 2020 Jun 16;21(12). pii: ijms21124274. doi: 10.3390/ijms21124274. [Article]
- Lu Q, Jiang Z, Wang Q, Hu H, Zhao G: The effect of Tauroursodeoxycholic acid (TUDCA) and gut microbiota on murine gallbladder stone formation. Ann Hepatol. 2021 Jul-Aug;23:100289. doi: 10.1016/j.aohep.2020.100289. Epub 2020 Nov 18. [Article]
- Setchell KD, Rodrigues CM, Podda M, Crosignani A: Metabolism of orally administered tauroursodeoxycholic acid in patients with primary biliary cirrhosis. Gut. 1996 Mar;38(3):439-46. doi: 10.1136/gut.38.3.439. [Article]
- Invernizzi P, Setchell KD, Crosignani A, Battezzati PM, Larghi A, O'Connell NC, Podda M: Differences in the metabolism and disposition of ursodeoxycholic acid and of its taurine-conjugated species in patients with primary biliary cirrhosis. Hepatology. 1999 Feb;29(2):320-7. doi: 10.1002/hep.510290220. [Article]
- AIFA: Tauro (Tauroursodeoxycholic Acid) Oral Capsules [Link]
- Health Canada Approved Drug Products: ALBRIOZA (sodium phenylbutyrate and ursodoxicoltaurine) Oral Powder for suspension [Link]
- FDA Approved Drug Products: RELYVRIO (sodium phenylbutyrate and taurursodiol) for oral suspension [Link]
- External Links
- KEGG Compound
- C16868
- PubChem Compound
- 9848818
- PubChem Substance
- 175427112
- ChemSpider
- 8024531
- BindingDB
- 50236230
- 2613950
- ChEBI
- 80774
- ChEMBL
- CHEMBL272427
- ZINC
- ZINC000003914813
- PDBe Ligand
- 5D5
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ursodoxicoltaurine
- PDB Entries
- 5dlv / 5dlw
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Basic Science Diabetes / Obesity / Resistance, Insulin 1 somestatus stop reason just information to hide Not Available Completed Basic Science Endoplasmic Reticulum Stress / HIV Related Insulin Resistance / Protease Inhibitor Related Insulin Resistance 1 somestatus stop reason just information to hide Not Available Completed Treatment Cholestasis 1 somestatus stop reason just information to hide Not Available Completed Treatment Cystic Fibrosis (CF) 1 somestatus stop reason just information to hide 4 Unknown Status Prevention Gallstones 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Powder, for suspension Oral Capsule Oral 150 MG Capsule Oral 250 MG Capsule, delayed release Oral 500 MG Tablet, extended release Oral 500 MG - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US10857162 No 2020-12-08 2033-12-24 US US10251896 No 2019-04-09 2033-12-24 US US9872865 No 2018-01-23 2033-12-24 US US11071742 No 2021-07-27 2033-12-24 US US11583542 No 2020-07-27 2040-07-27 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00748 mg/mL ALOGPS logP 1.38 ALOGPS logP 1.1 Chemaxon logS -4.8 ALOGPS pKa (Strongest Acidic) -0.8 Chemaxon pKa (Strongest Basic) -0.32 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 123.93 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 130.68 m3·mol-1 Chemaxon Polarizability 56.75 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9774 Blood Brain Barrier + 0.8416 Caco-2 permeable - 0.8957 P-glycoprotein substrate Non-substrate 0.5136 P-glycoprotein inhibitor I Non-inhibitor 0.6229 P-glycoprotein inhibitor II Non-inhibitor 0.7598 Renal organic cation transporter Non-inhibitor 0.8476 CYP450 2C9 substrate Non-substrate 0.7519 CYP450 2D6 substrate Non-substrate 0.7972 CYP450 3A4 substrate Substrate 0.654 CYP450 1A2 substrate Non-inhibitor 0.7814 CYP450 2C9 inhibitor Non-inhibitor 0.8625 CYP450 2D6 inhibitor Non-inhibitor 0.8685 CYP450 2C19 inhibitor Non-inhibitor 0.8426 CYP450 3A4 inhibitor Non-inhibitor 0.8612 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7175 Ames test Non AMES toxic 0.6103 Carcinogenicity Non-carcinogens 0.5359 Biodegradation Not ready biodegradable 0.972 Rat acute toxicity 2.0310 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.706 hERG inhibition (predictor II) Inhibitor 0.5549
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0f89-0000950000-60e13f1ebd252aa04cf3 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0w29-4439450000-6c287fcc0ff78e167c6b Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-0000900000-8ccdfe538f3c848f0cac Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-2100900000-3271d354e2e0f735573e Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-001j-9603200000-7bac0171160fc78c1299 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-00ks-2269000000-1a4d10c59abba4214d9a Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 223.622697 predictedDarkChem Lite v0.1.0 [M-H]- 223.72533 predictedDeepCCS 1.0 (2019) [M+H]+ 224.714697 predictedDarkChem Lite v0.1.0 [M+H]+ 225.57637 predictedDeepCCS 1.0 (2019) [M+Na]+ 223.674697 predictedDarkChem Lite v0.1.0 [M+Na]+ 232.18983 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Activator
- General Function
- Integrin alpha-5/beta-1 (ITGA5:ITGB1) is a receptor for fibronectin and fibrinogen. It recognizes the sequence R-G-D in its ligands. ITGA5:ITGB1 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGA5:ITGB1 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887, PubMed:17158881). ITGA5:ITGB1 acts as a receptor for fibronectin (FN1) and mediates R-G-D-dependent cell adhesion to FN1 (PubMed:33962943). ITGA5:ITGB1 is a receptor for IL1B and binding is essential for IL1B signaling (PubMed:29030430). ITGA5:ITGB3 is a receptor for soluble CD40LG and is required for CD40/CD40LG signaling (PubMed:31331973)
- Specific Function
- calcium ion binding
- Gene Name
- ITGA5
- Uniprot ID
- P08648
- Uniprot Name
- Integrin alpha-5
- Molecular Weight
- 114535.52 Da
References
- Vang S, Longley K, Steer CJ, Low WC: The Unexpected Uses of Urso- and Tauroursodeoxycholic Acid in the Treatment of Non-liver Diseases. Glob Adv Health Med. 2014 May;3(3):58-69. doi: 10.7453/gahmj.2014.017. [Article]
- Beuers U: beta1 integrin is a long-sought sensor for tauroursodeoxycholic acid. Hepatology. 2013 Mar;57(3):867-9. doi: 10.1002/hep.26228. [Article]
Enzymes
- Kind
- Protein
- Organism
- Rat
- Pharmacological action
- Unknown
- Actions
- Inducer
- 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
- Cyp3a1
- Uniprot ID
- P04800
- Uniprot Name
- Cytochrome P450 3A1
- Molecular Weight
- 57917.375 Da
References
- Paolini M, Pozzetti L, Piazza F, Cantelli-Forti G, Roda A: Bile acid structure and selective modulation of murine hepatic cytochrome P450-linked enzymes. Hepatology. 1999 Sep;30(3):730-9. [Article]
- Kind
- Protein
- Organism
- Rat
- Pharmacological action
- Unknown
- Actions
- Inducer
- 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
- 1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity
- Gene Name
- Cyp3a2
- Uniprot ID
- P05183
- Uniprot Name
- Cytochrome P450 3A2
- Molecular Weight
- 57731.215 Da
References
- Paolini M, Pozzetti L, Piazza F, Cantelli-Forti G, Roda A: Bile acid structure and selective modulation of murine hepatic cytochrome P450-linked enzymes. Hepatology. 1999 Sep;30(3):730-9. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane (PubMed:19129463, PubMed:7557095). Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) (PubMed:11159893, PubMed:12568656, PubMed:19129463, PubMed:23918469, PubMed:25560245, PubMed:9539145). Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision (PubMed:25560245). Involved in the uptake of clinically used drugs (PubMed:17301733, PubMed:20686826, PubMed:27777271). Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) (PubMed:19129463, PubMed:20358049). Also transports prostaglandin E2 (PubMed:19129463). Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons (PubMed:25132355). May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel (PubMed:23243220). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment (PubMed:19129463). Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions (PubMed:19129463). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- bile acid transmembrane transporter activity
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- Kullak-Ublick GA, Hagenbuch B, Stieger B, Schteingart CD, Hofmann AF, Wolkoff AW, Meier PJ: Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver. Gastroenterology. 1995 Oct;109(4):1274-82. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Heterodimer with SLC3A2, that functions as an antiporter by mediating the exchange of extracellular anionic L-cystine and intracellular L-glutamate across the cellular plasma membrane (PubMed:11133847, PubMed:11417227, PubMed:14722095, PubMed:15151999, PubMed:34880232, PubMed:35245456, PubMed:35352032). Provides L-cystine for the maintenance of the redox balance between extracellular L-cystine and L-cysteine and for the maintenance of the intracellular levels of glutathione that is essential for cells protection from oxidative stress (By similarity). The transport is sodium-independent, electroneutral with a stoichiometry of 1:1, and is drove by the high intracellular concentration of L-glutamate and the intracellular reduction of L-cystine (PubMed:11133847, PubMed:11417227). In addition, mediates the import of L-kynurenine leading to anti-ferroptotic signaling propagation required to maintain L-cystine and glutathione homeostasis (PubMed:35245456). Moreover, mediates N-acetyl-L-cysteine uptake into the placenta leading to subsequently down-regulation of pathways associated with oxidative stress, inflammation and apoptosis (PubMed:34120018). In vitro can also transport L-aspartate (PubMed:11417227). May participate in astrocyte and meningeal cell proliferation during development and can provide neuroprotection by promoting glutathione synthesis and delivery from non-neuronal cells such as astrocytes and meningeal cells to immature neurons (By similarity). Controls the production of pheomelanin pigment directly (By similarity)
- Specific Function
- cystine
- Gene Name
- SLC7A11
- Uniprot ID
- Q9UPY5
- Uniprot Name
- Cystine/glutamate transporter
- Molecular Weight
- 55422.44 Da
References
- Schroeder A, Eckhardt U, Stieger B, Tynes R, Schteingart CD, Hofmann AF, Meier PJ, Hagenbuch B: Substrate specificity of the rat liver Na(+)-bile salt cotransporter in Xenopus laevis oocytes and in CHO cells. Am J Physiol. 1998 Feb;274(2 Pt 1):G370-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Downregulator
- Curator comments
- This drug-target relationship was established in mice. The significance of this target relationship in humans is unknown.
- General Function
- ABCG5 and ABCG8 form an obligate heterodimer that mediates Mg(2+)- and ATP-dependent sterol transport across the cell membrane (PubMed:27144356). Plays an essential role in the selective transport of dietary plant sterols and cholesterol in and out of the enterocytes and in the selective sterol excretion by the liver into bile (PubMed:11099417, PubMed:11138003, PubMed:15054092, PubMed:27144356). Required for normal sterol homeostasis (PubMed:11099417, PubMed:11138003, PubMed:15054092). The heterodimer with ABCG8 has ATPase activity (PubMed:16893193, PubMed:20210363, PubMed:27144356)
- Specific Function
- ABC-type transporter activity
- Gene Name
- ABCG5
- Uniprot ID
- Q9H222
- Uniprot Name
- ATP-binding cassette sub-family G member 5
- Molecular Weight
- 72503.02 Da
References
- Lu Q, Jiang Z, Wang Q, Hu H, Zhao G: The effect of Tauroursodeoxycholic acid (TUDCA) and gut microbiota on murine gallbladder stone formation. Ann Hepatol. 2021 Jul-Aug;23:100289. doi: 10.1016/j.aohep.2020.100289. Epub 2020 Nov 18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Downregulator
- Curator comments
- This drug-target relationship was established in mice. The significance of this target relationship in humans is unknown.
- General Function
- ABCG5 and ABCG8 form an obligate heterodimer that mediates Mg(2+)- and ATP-dependent sterol transport across the cell membrane. Plays an essential role in the selective transport of the dietary cholesterol in and out of the enterocytes and in the selective sterol excretion by the liver into bile (PubMed:11099417, PubMed:11452359, PubMed:15054092, PubMed:27144356). Required for normal sterol homeostasis (PubMed:11099417, PubMed:11452359, PubMed:15054092). The heterodimer with ABCG5 has ATPase activity (PubMed:16893193, PubMed:20210363, PubMed:27144356)
- Specific Function
- ABC-type transporter activity
- Gene Name
- ABCG8
- Uniprot ID
- Q9H221
- Uniprot Name
- ATP-binding cassette sub-family G member 8
- Molecular Weight
- 75678.03 Da
References
- Lu Q, Jiang Z, Wang Q, Hu H, Zhao G: The effect of Tauroursodeoxycholic acid (TUDCA) and gut microbiota on murine gallbladder stone formation. Ann Hepatol. 2021 Jul-Aug;23:100289. doi: 10.1016/j.aohep.2020.100289. Epub 2020 Nov 18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Regulator
- Curator comments
- This drug-target relationship was established in mice. The significance of this target relationship in humans is unknown.
- General Function
- Catalyzes the transport of the major hydrophobic bile salts, such as taurine and glycine-conjugated cholic acid across the canalicular membrane of hepatocytes in an ATP-dependent manner, therefore participates in hepatic bile acid homeostasis and consequently to lipid homeostasis through regulation of biliary lipid secretion in a bile salts dependent manner (PubMed:15791618, PubMed:16332456, PubMed:18985798, PubMed:19228692, PubMed:20010382, PubMed:20398791, PubMed:22262466, PubMed:24711118, PubMed:29507376, PubMed:32203132). Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts (PubMed:16332456). Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion (PubMed:15901796, PubMed:18245269)
- Specific Function
- ABC-type bile acid transporter activity
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Lu Q, Jiang Z, Wang Q, Hu H, Zhao G: The effect of Tauroursodeoxycholic acid (TUDCA) and gut microbiota on murine gallbladder stone formation. Ann Hepatol. 2021 Jul-Aug;23:100289. doi: 10.1016/j.aohep.2020.100289. Epub 2020 Nov 18. [Article]
Drug created at February 19, 2013 00:42 / Updated at October 22, 2022 01:06