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Identification
- Summary
Thyroid, porcine is a naturally-occurring peptide hormone used for the replacement therapy for hypothyroidism of any etiology, treatment for euthyroid goiters, and management of thyroid cancers.
- Generic Name
- Thyroid, porcine
- DrugBank Accession Number
- DB09100
- Background
Thyroid extract is dried and powdered thyroid glands from pigs containing tiiodothyronine (T3) and thyroxine (T4) used to supplement low or absent thyroid activity.4,10 Thyroid extract has been described in literature to treat hypothyroidism since 18912 but its use dates back as far as the 6th century.4 Thyroid extract is no longer considered a first line therapy as it delivers a dose that is inconsistent with the stated strength of the tablet.3 Currently, patients are more likely to be treated with levothyroxine.3
Thyroid extracts were never FDA approved as their use in the United States predates the FDA.4
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
- Not Available
- Synonyms
- Pig thyroid
- Porcine thyroid
- Sus scrofa thyroid
- Thyroid (pork)
- Thyroid extract, porcine
Pharmacology
- Indication
Thyroid extract is indicated for replacement therapy in decreased or absent thyroid function.10
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Hypothyroidism •••••••••••• •••••• - Contraindications & Blackbox Warnings
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Thyroid extract increases the metabolic rate of patients with hypothyroidism.8,9 The therapeutic index of thyroid extract is wide, as patients can be given varying doses.10 The duration of action is long as thyroid extract is generally given once daily.10 Patients should not use thyroid extract for weight loss.10
- Mechanism of action
T3 binding to the thyroid hormone receptor (TR), changes the conformation of the TR, allowing it to bind to the retinoid X receptor (RXR) and form a coactivator complex.8 The coactivator complex has histone acetyltransferase activity, which activates genes.8 In the absence of T3, TR and RXR form a corepressor complex with histone deacetylase activity, which represses genes.8 The macroscopic effects of thyroid hormones is an increase in the metabolic rate.9 T4 has similar but weaker activity to T3.9
Target Actions Organism UThyroid hormone receptor alpha substrateHumans UThyroid hormone receptor beta substrateHumans - Absorption
T4 is 48-79% absorbed in the gastrointestinal tract and T3 is 95% absorbed.10 L-triiodothyronine reaches a Cmax of 320±60ng/L, with a Tmax of 1.8±0.3h.6 Levothyroxin has a Tmax of2-3h.5
- Volume of distribution
Data regarding the volume of distribution of thyroid extract is not readily available as it is a mixture of many compounds.10 Levothyroxine, a synthetic form of T4, has a volume of distribution of 11-15L.5 L-triiodothyronine, a synthetic form of T3, has an apparent volume of distribution of 14.9±4.2L.6
- Protein binding
Thyroid hormones are more than 99% protein bound, typically to albumin, transthyretin, and thyroxine-binding globulin.1,10
- Metabolism
Approximately one third of the active T4 is deiodinated to the active T3, one third is deiodinated to the inactive reverse T3 (rT3), and one third is glucuronidated or sulfated.7 Deiodination is mediated by iodothryonine deiodinases, glucuronidation is mediated by glucuronyltransferases, and sulfation is mediated by sulfotransferases.7,5 T3 and rT3 are further deiodinated to diiodothyronine (T2), iodothyronine (T1), and their reverse forms.5 T4 can also undergo ether bond cleavage or oxidative deamination but these pathways are incredibly minor.7
- Route of elimination
Data regarding the route of elimination of thyroid extract is not readily available as it is a mixture of many compounds.10 20% of the body's naturally produced thyroxine is eliminated in the feces.7
- Half-life
Data regarding the half life of thyroid extract is not readily available as it is a mixture of many compounds.10 Levothyroxine, a synthetic form of T4, has a half life of 6.2 days in euthyroid patients and 7.5 days in hypothyroid patients.5 T3 has a half life of 1.0 days in euthyroid patients and 1.4 days in hypothyroid patients.5
- Clearance
Data regarding the clearance of thyroid extract is not readily available as it is a mixture of many compounds.10 The clearance of levothyroxine, a synthetic form of T4, is 0.044L/h in euthyroid patients and 0.038L/h in hypothyroid patients.5
- Adverse Effects
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Patients experiencing and overdose may present with symptoms of a hypermetabolic state.10 Overdose may be treated by symptomatic and supportive treatment, dose reduction or temporarily stopping the medication, induction of vomiting, administering oxygen, cardiac glycosides, as well as methods to control fever, hypoglycemia, and fluid loss.10
- 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 softwareAcalabrutinib The therapeutic efficacy of Thyroid, porcine can be decreased when used in combination with Acalabrutinib. Acarbose Thyroid, porcine may decrease the hypoglycemic activities of Acarbose. Acebutolol The therapeutic efficacy of Thyroid, porcine can be decreased when used in combination with Acebutolol. Acenocoumarol The risk or severity of bleeding can be increased when Thyroid, porcine is combined with Acenocoumarol. Acetohexamide Thyroid, porcine may decrease the hypoglycemic activities of Acetohexamide. - 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 Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image APur Thyroid Tablet 60 mg/1 Oral Vitruvias Therapeutics 2024-01-12 Not applicable US 
APur Thyroid Tablet 120 mg/1 Oral Vitruvias Therapeutics 2024-01-12 Not applicable US APur Thyroid Tablet 30 mg/1 Oral Vitruvias Therapeutics 2024-01-12 Not applicable US APur Thyroid Tablet 90 mg/1 Oral Vitruvias Therapeutics 2024-01-12 Not applicable US APur Thyroid Tablet 15 mg/1 Oral Vitruvias Therapeutics 2024-01-12 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image APur Thyroid Thyroid, porcine (60 mg/1) Tablet Oral Vitruvias Therapeutics 2024-01-12 Not applicable US APur Thyroid Thyroid, porcine (120 mg/1) Tablet Oral Vitruvias Therapeutics 2024-01-12 Not applicable US APur Thyroid Thyroid, porcine (30 mg/1) Tablet Oral Vitruvias Therapeutics 2024-01-12 Not applicable US APur Thyroid Thyroid, porcine (90 mg/1) Tablet Oral Vitruvias Therapeutics 2024-01-12 Not applicable US APur Thyroid Thyroid, porcine (15 mg/1) Tablet Oral Vitruvias Therapeutics 2024-01-12 Not applicable US
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 6RV024OAUQ
- CAS number
- Not Available
References
- General References
- Rabah SA, Gowan IL, Pagnin M, Osman N, Richardson SJ: Thyroid Hormone Distributor Proteins During Development in Vertebrates. Front Endocrinol (Lausanne). 2019 Aug 8;10:506. doi: 10.3389/fendo.2019.00506. eCollection 2019. [Article]
- Murray GR: Note on the Treatment of Myxoedema by Hypodermic Injections of an Extract of the Thyroid Gland of a Sheep. Br Med J. 1891 Oct 10;2(1606):796-7. doi: 10.1136/bmj.2.1606.796. [Article]
- McAninch EA, Bianco AC: The Swinging Pendulum in Treatment for Hypothyroidism: From (and Toward?) Combination Therapy. Front Endocrinol (Lausanne). 2019 Jul 9;10:446. doi: 10.3389/fendo.2019.00446. eCollection 2019. [Article]
- Mateo RCI, Hennessey JV: Thyroxine and treatment of hypothyroidism: seven decades of experience. Endocrine. 2019 Oct;66(1):10-17. doi: 10.1007/s12020-019-02006-8. Epub 2019 Jul 18. [Article]
- Colucci P, Yue CS, Ducharme M, Benvenga S: A Review of the Pharmacokinetics of Levothyroxine for the Treatment of Hypothyroidism. Eur Endocrinol. 2013 Mar;9(1):40-47. doi: 10.17925/EE.2013.09.01.40. Epub 2013 Mar 15. [Article]
- Van Tassell B, Wohlford GF 4th, Linderman JD, Smith S, Yavuz S, Pucino F, Celi FS: Pharmacokinetics of L-Triiodothyronine in Patients Undergoing Thyroid Hormone Therapy Withdrawal. Thyroid. 2019 Oct;29(10):1371-1379. doi: 10.1089/thy.2019.0101. Epub 2019 Sep 12. [Article]
- Peeters RP, Visser TJ: Metabolism of Thyroid Hormone . [Article]
- Zhang J, Lazar MA: The mechanism of action of thyroid hormones. Annu Rev Physiol. 2000;62:439-66. doi: 10.1146/annurev.physiol.62.1.439. [Article]
- Hulbert AJ: Thyroid hormones and their effects: a new perspective. Biol Rev Camb Philos Soc. 2000 Nov;75(4):519-631. doi: 10.1017/s146479310000556x. [Article]
- Health Canada Approved Drug Products: Desiccated Thyroid Oral Tablets [Link]
- External Links
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 Not Available Thyroid Cancer 1 somestatus stop reason just information to hide Not Available Not Yet Recruiting Treatment Graves' Disease / Hyperthyroidism 1 somestatus stop reason just information to hide Not Available Recruiting Not Available Parathyroid Diseases / Thyroid Gland Diseases 1 somestatus stop reason just information to hide Not Available Recruiting Not Available RAI-Refractory Thyroid Cancer / Thyroid Cancer 1 somestatus stop reason just information to hide Not Available Recruiting Diagnostic Thyroid Gland Medullary Carcinoma 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 120 mg/1 Tablet Oral 15 mg/1 Tablet Oral 180 mg/1 Tablet Oral 240 mg/1 Tablet Oral 30 mg/1 Tablet Oral 300 mg/1 Tablet Oral 60 mg/1 Tablet Oral 90 mg/1 Tablet, coated Oral 60 mg Tablet Oral 125 mg Tablet Oral 30 mg Tablet, sugar coated Oral 60 mg Tablet Oral 60 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Isoform Alpha-1 Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine.
- Specific Function
- chromatin DNA binding
- Gene Name
- THRA
- Uniprot ID
- P10827
- Uniprot Name
- Thyroid hormone receptor alpha
- Molecular Weight
- 54815.055 Da
References
- Ortiga-Carvalho TM, Sidhaye AR, Wondisford FE: Thyroid hormone receptors and resistance to thyroid hormone disorders. Nat Rev Endocrinol. 2014 Oct;10(10):582-91. doi: 10.1038/nrendo.2014.143. Epub 2014 Aug 19. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine.
- Specific Function
- chromatin DNA binding
- Gene Name
- THRB
- Uniprot ID
- P10828
- Uniprot Name
- Thyroid hormone receptor beta
- Molecular Weight
- 52787.16 Da
References
- Ortiga-Carvalho TM, Sidhaye AR, Wondisford FE: Thyroid hormone receptors and resistance to thyroid hormone disorders. Nat Rev Endocrinol. 2014 Oct;10(10):582-91. doi: 10.1038/nrendo.2014.143. Epub 2014 Aug 19. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Responsible for the deiodination of T4 (3,5,3',5'-tetraiodothyronine) into T3 (3,5,3'-triiodothyronine) and of T3 into T2 (3,3'-diiodothyronine). Plays a role in providing a source of plasma T3 by deiodination of T4 in peripheral tissues such as liver and kidney.
- Specific Function
- selenium binding
- Gene Name
- DIO1
- Uniprot ID
- P49895
- Uniprot Name
- Type I iodothyronine deiodinase
- Molecular Weight
- 28924.21 Da
References
- Bernal J, Guadano-Ferraz A, Morte B: Thyroid hormone transporters--functions and clinical implications. Nat Rev Endocrinol. 2015 Jul;11(7):406-17. doi: 10.1038/nrendo.2015.66. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Responsible for the deiodination of T4 (3,5,3',5'-tetraiodothyronine) into T3 (3,5,3'-triiodothyronine). Essential for providing the brain with appropriate levels of T3 during the critical period of development.
- Specific Function
- selenium binding
- Gene Name
- DIO2
- Uniprot ID
- Q92813
- Uniprot Name
- Type II iodothyronine deiodinase
- Molecular Weight
- 30551.48 Da
References
- Bernal J, Guadano-Ferraz A, Morte B: Thyroid hormone transporters--functions and clinical implications. Nat Rev Endocrinol. 2015 Jul;11(7):406-17. doi: 10.1038/nrendo.2015.66. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Responsible for the deiodination of T4 (3,5,3',5'-tetraiodothyronine) into RT3 (3,3',5'-triiodothyronine) and of T3 (3,5,3'-triiodothyronine) into T2 (3,3'-diiodothyronine). RT3 and T2 are inactive metabolites. May play a role in preventing premature exposure of developing fetal tissues to adult levels of thyroid hormones. Can regulate circulating fetal thyroid hormone concentrations throughout gestation. Essential role for regulation of thyroid hormone inactivation during embryological development.
- Specific Function
- thyroxine 5'-deiodinase activity
- Gene Name
- DIO3
- Uniprot ID
- P55073
- Uniprot Name
- Thyroxine 5-deiodinase
- Molecular Weight
- 33947.175 Da
References
- Bernal J, Guadano-Ferraz A, Morte B: Thyroid hormone transporters--functions and clinical implications. Nat Rev Endocrinol. 2015 Jul;11(7):406-17. doi: 10.1038/nrendo.2015.66. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of a wide variety of acceptor molecules bearing a hydroxyl or an amine groupe. Sulfonation increases the water solubility of most compounds, and therefore their renal excretion, but it can also result in bioactivation to form active metabolites. Displays broad substrate specificity for small phenolic compounds. Plays an important role in the sulfonation of endogenous molecules such as steroid hormones and 3,3'-diiodothyronin (PubMed:10199779, PubMed:12471039, PubMed:16221673, PubMed:21723874, PubMed:22069470, PubMed:7834621). Mediates the sulfate conjugation of a variety of xenobiotics, including the drugs acetaminophen and minoxidil (By similarity). Mediates also the metabolic activation of carcinogenic N-hydroxyarylamines leading to highly reactive intermediates capable of forming DNA adducts, potentially resulting in mutagenesis (PubMed:7834621). May play a role in gut microbiota-host metabolic interaction. O-sulfonates 4-ethylphenol (4-EP), a dietary tyrosine-derived metabolite produced by gut bacteria. The product 4-EPS crosses the blood-brain barrier and may negatively regulate oligodendrocyte maturation and myelination, affecting the functional connectivity of different brain regions associated with the limbic system.
- Specific Function
- 3'-phosphoadenosine 5'-phosphosulfate binding
- Gene Name
- SULT1A1
- Uniprot ID
- P50225
- Uniprot Name
- Sulfotransferase 1A1
- Molecular Weight
- 34165.13 Da
References
- Peeters RP, Visser TJ: Metabolism of Thyroid Hormone . [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of catecholamines, phenolic drugs and neurotransmitters. Is also responsible for the sulfonation and activation of minoxidil. Mediates the metabolic activation of carcinogenic N-hydroxyarylamines to DNA binding products and could so participate as modulating factor of cancer risk.
- Specific Function
- aryl sulfotransferase activity
- Gene Name
- SULT1A2
- Uniprot ID
- P50226
- Uniprot Name
- Sulfotransferase 1A2
- Molecular Weight
- 34309.49 Da
References
- Peeters RP, Visser TJ: Metabolism of Thyroid Hormone . [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of phenolic monoamines (neurotransmitters such as dopamine, norepinephrine and serotonin) and phenolic and catechol drugs.
- Specific Function
- amine sulfotransferase activity
- Gene Name
- SULT1A3
- Uniprot ID
- P0DMM9
- Uniprot Name
- Sulfotransferase 1A3
- Molecular Weight
- 34195.96 Da
References
- Peeters RP, Visser TJ: Metabolism of Thyroid Hormone . [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of dopamine, small phenols such as 1-naphthol and p-nitrophenol and thyroid hormones, including 3,3'-diiodothyronine, triidothyronine (T3) and reverse triiodothyronine (rT3) (PubMed:28084139, PubMed:9443824, PubMed:9463486). May play a role in gut microbiota-host metabolic interaction. O-sulfonates 4-ethylphenol (4-EP), a dietary tyrosine-derived metabolite produced by gut bacteria. The product 4-EPS crosses the blood-brain barrier and may negatively regulate oligodendrocyte maturation and myelination, affecting the functional connectivity of different brain regions associated with the limbic system (PubMed:35165440).
- Specific Function
- aryl sulfotransferase activity
- Gene Name
- SULT1B1
- Uniprot ID
- O43704
- Uniprot Name
- Sulfotransferase 1B1
- Molecular Weight
- 34898.955 Da
References
- Peeters RP, Visser TJ: Metabolism of Thyroid Hormone . [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of phenolic compounds. Does not sulfonate steroids, dopamine, acetaminophen, or alpha-naphthol (PubMed:10481272, PubMed:10783263, PubMed:9852044). Catalyzes the sulfonation of the carcinogenic N-Hydroxy-2-acetylaminofluorene leading to highly reactive intermediates capable of forming DNA adducts, potentially resulting in mutagenesis (PubMed:9852044).
- Specific Function
- aryl sulfotransferase activity
- Gene Name
- SULT1C2
- Uniprot ID
- O00338
- Uniprot Name
- Sulfotransferase 1C2
- Molecular Weight
- 34879.905 Da
References
- Peeters RP, Visser TJ: Metabolism of Thyroid Hormone . [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of estradiol and estrone (PubMed:11006110, PubMed:11884392, PubMed:7779757). Is a key enzyme in estrogen homeostasis, the sulfation of estrogens leads to their inactivation. Also sulfates dehydroepiandrosterone (DHEA), pregnenolone, (24S)-hydroxycholesterol and xenobiotic compounds like ethinylestradiol, equalenin, diethyl stilbesterol and 1-naphthol at significantly lower efficiency (PubMed:11006110, PubMed:19589875). Does not sulfonate cortisol, testosterone and dopamine (PubMed:11006110, PubMed:7779757). May play a role in gut microbiota-host metabolic interaction. O-sulfonates 4-ethylphenol (4-EP), a dietary tyrosine-derived metabolite produced by gut bacteria. The product 4-EPS crosses the blood-brain barrier and may negatively regulate oligodendrocyte maturation and myelination, affecting the functional connectivity of different brain regions associated with the limbic system.
- Specific Function
- aryl sulfotransferase activity
- Gene Name
- SULT1E1
- Uniprot ID
- P49888
- Uniprot Name
- Sulfotransferase 1E1
- Molecular Weight
- 35126.185 Da
References
- Peeters RP, Visser TJ: Metabolism of Thyroid Hormone . [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017).
- Specific Function
- antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
References
- Rabah SA, Gowan IL, Pagnin M, Osman N, Richardson SJ: Thyroid Hormone Distributor Proteins During Development in Vertebrates. Front Endocrinol (Lausanne). 2019 Aug 8;10:506. doi: 10.3389/fendo.2019.00506. eCollection 2019. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Thyroid hormone-binding protein. Probably transports thyroxine from the bloodstream to the brain.
- Specific Function
- hormone activity
- Gene Name
- TTR
- Uniprot ID
- P02766
- Uniprot Name
- Transthyretin
- Molecular Weight
- 15886.88 Da
References
- Rabah SA, Gowan IL, Pagnin M, Osman N, Richardson SJ: Thyroid Hormone Distributor Proteins During Development in Vertebrates. Front Endocrinol (Lausanne). 2019 Aug 8;10:506. doi: 10.3389/fendo.2019.00506. eCollection 2019. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Major thyroid hormone transport protein in serum.
- Specific Function
- serine-type endopeptidase inhibitor activity
- Gene Name
- SERPINA7
- Uniprot ID
- P05543
- Uniprot Name
- Thyroxine-binding globulin
- Molecular Weight
- 46324.12 Da
References
- Rabah SA, Gowan IL, Pagnin M, Osman N, Richardson SJ: Thyroid Hormone Distributor Proteins During Development in Vertebrates. Front Endocrinol (Lausanne). 2019 Aug 8;10:506. doi: 10.3389/fendo.2019.00506. eCollection 2019. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Specific thyroid hormone transmembrane transporter, that mediates both uptake and efflux of thyroid hormones across the cell membrane independently of pH or a Na(+) gradient. Major substrates are the iodothyronines T3 and T4 and to a lesser extent rT3 and 3,3-diiodothyronine (3,3'-T2) (PubMed:16887882, PubMed:18337592, PubMed:20628049, PubMed:23550058, PubMed:26426690, PubMed:27805744, PubMed:31436139). Acts as an important mediator of thyroid hormone transport, especially T3, through the blood-brain barrier (Probable) (PubMed:28526555).
- Specific Function
- amino acid transmembrane transporter activity
- Gene Name
- SLC16A2
- Uniprot ID
- P36021
- Uniprot Name
- Monocarboxylate transporter 8
- Molecular Weight
- 59510.86 Da
References
- Bernal J, Guadano-Ferraz A, Morte B: Thyroid hormone transporters--functions and clinical implications. Nat Rev Endocrinol. 2015 Jul;11(7):406-17. doi: 10.1038/nrendo.2015.66. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Mediates the Na(+)-independent high affinity transport of organic anions such as the thyroid hormones L-thyroxine (T4), L-thyroxine sulfate (T4S), and 3,3',5'-triiodo-L-thyronine (reverse T3, rT3) at the plasma membrane (PubMed:12351693, PubMed:18566113, PubMed:19129463). Regulates T4 levels in different brain regions by transporting T4, and also by serving as an export pump for T4S, which is a source of T4 after hydrolysis by local sulfatases (PubMed:18566113). Increases the access of these substrates to the intracellular sites where they are metabolized by the deiodinases (PubMed:18566113). Other potential substrates, such as triiodothyronine (T3), 17-beta-glucuronosyl estradiol (17beta-estradiol 17-O-(beta-D-glucuronate)), estrone-3-sulfate (E1S) and sulfobromophthalein (BSP) are transported with much lower efficiency (PubMed:12351693, PubMed:19129463). Transports T4 and E1S in a pH-insensitive manner (PubMed:19129463). Facilitates the transport of thyroid hormones across the blood-brain barrier and into glia and neuronal cells in the brain (PubMed:30296914).
- Specific Function
- bile acid transmembrane transporter activity
- Gene Name
- SLCO1C1
- Uniprot ID
- Q9NYB5
- Uniprot Name
- Solute carrier organic anion transporter family member 1C1
- Molecular Weight
- 78695.625 Da
References
- Bernal J, Guadano-Ferraz A, Morte B: Thyroid hormone transporters--functions and clinical implications. Nat Rev Endocrinol. 2015 Jul;11(7):406-17. doi: 10.1038/nrendo.2015.66. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Putative organic anion antiporter with apparent broad substrate specificity. Recognizes various substrates including thyroid hormone L-thyroxine, prostanoids such as prostaglandin E1 and E2, bile acids such as taurocholate, glycolate and glycochenodeoxycholate and peptide hormones such as L-arginine vasopressin, likely operating in a tissue-specific manner (PubMed:10873595, PubMed:14631946, PubMed:16971491, PubMed:19129463, PubMed:30063921). The transport mechanism, its electrogenicity and potential tissue-specific counterions remain to be elucidated (Probable).
- Specific Function
- organic anion transmembrane transporter activity
- Gene Name
- SLCO3A1
- Uniprot ID
- Q9UIG8
- Uniprot Name
- Solute carrier organic anion transporter family member 3A1
- Molecular Weight
- 76552.135 Da
References
- Bernal J, Guadano-Ferraz A, Morte B: Thyroid hormone transporters--functions and clinical implications. Nat Rev Endocrinol. 2015 Jul;11(7):406-17. doi: 10.1038/nrendo.2015.66. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Organic anion antiporter with apparent broad substrate specificity. Recognizes various substrates including thyroid hormones 3,3',5-triiodo-L-thyronine (T3), L-thyroxine (T4) and 3,3',5'-triiodo-L-thyronine (rT3), conjugated steroids such as estrone 3-sulfate and estradiol 17-beta glucuronide, bile acids such as taurocholate and prostanoids such as prostaglandin E2, likely operating in a tissue-specific manner (PubMed:10873595, PubMed:19129463, PubMed:30343886). May be involved in uptake of metabolites from the circulation into organs such as kidney, liver or placenta. Possibly drives the selective transport of thyroid hormones and estrogens coupled to an outward glutamate gradient across the microvillous membrane of the placenta (PubMed:30343886). The transport mechanism, its electrogenicity and potential tissue-specific counterions remain to be elucidated (Probable).
- Specific Function
- organic anion transmembrane transporter activity
- Gene Name
- SLCO4A1
- Uniprot ID
- Q96BD0
- Uniprot Name
- Solute carrier organic anion transporter family member 4A1
- Molecular Weight
- 77192.505 Da
References
- Bernal J, Guadano-Ferraz A, Morte B: Thyroid hormone transporters--functions and clinical implications. Nat Rev Endocrinol. 2015 Jul;11(7):406-17. doi: 10.1038/nrendo.2015.66. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- The heterodimer with SLC3A2 functions as a sodium-independent, high-affinity transporter that mediates uptake of large neutral amino acids such as phenylalanine, tyrosine, leucine, histidine, methionine, tryptophan, valine, isoleucine and alanine (PubMed:10049700, PubMed:10574970, PubMed:11557028, PubMed:11564694, PubMed:12117417, PubMed:12225859, PubMed:15769744, PubMed:18262359, PubMed:25998567, PubMed:30867591, PubMed:9751058). The heterodimer with SLC3A2 mediates the uptake of L-DOPA (By similarity). Functions as an amino acid exchanger (PubMed:11557028, PubMed:12117417, PubMed:12225859, PubMed:30867591). May play a role in the transport of L-DOPA across the blood-brain barrier (By similarity). May act as the major transporter of tyrosine in fibroblasts (Probable). May mediate blood-to-retina L-leucine transport across the inner blood-retinal barrier (By similarity). Can mediate the transport of thyroid hormones diiodothyronine (T2), triiodothyronine (T3) and thyroxine (T4) across the cell membrane (PubMed:11564694). When associated with LAPTM4B, the heterodimer formed by SLC3A2 and SLC7A5 is recruited to lysosomes to promote leucine uptake into these organelles, and thereby mediates mTORC1 activation (PubMed:25998567). Involved in the uptake of toxic methylmercury (MeHg) when administered as the L-cysteine or D,L-homocysteine complexes (PubMed:12117417). Involved in the cellular activity of small molecular weight nitrosothiols, via the stereoselective transport of L-nitrosocysteine (L-CNSO) across the membrane (PubMed:15769744).
- Specific Function
- amino acid transmembrane transporter activity
- Gene Name
- SLC7A5
- Uniprot ID
- Q01650
- Uniprot Name
- Large neutral amino acids transporter small subunit 1
- Molecular Weight
- 55009.62 Da
References
- Bernal J, Guadano-Ferraz A, Morte B: Thyroid hormone transporters--functions and clinical implications. Nat Rev Endocrinol. 2015 Jul;11(7):406-17. doi: 10.1038/nrendo.2015.66. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- As a major transporter of conjugated bile salts from plasma into the hepatocyte, it plays a key role in the enterohepatic circulation of bile salts necessary for the solubilization and absorption of dietary fat and fat-soluble vitamins (PubMed:14660639, PubMed:24867799, PubMed:34060352, PubMed:8132774). It is strictly dependent on the extracellular presence of sodium (PubMed:14660639, PubMed:24867799, PubMed:34060352, PubMed:8132774). It exhibits broad substrate specificity and transports various bile acids, such as taurocholate, cholate, as well as non-bile acid organic compounds, such as estrone sulfate (PubMed:14660639, PubMed:34060352). Works collaboratively with the ileal transporter (NTCP2), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation (PubMed:33222321).
- Specific Function
- bile acid
- Gene Name
- SLC10A1
- Uniprot ID
- Q14973
- Uniprot Name
- Hepatic sodium/bile acid cotransporter
- Molecular Weight
- 38118.64 Da
References
- Bernal J, Guadano-Ferraz A, Morte B: Thyroid hormone transporters--functions and clinical implications. Nat Rev Endocrinol. 2015 Jul;11(7):406-17. doi: 10.1038/nrendo.2015.66. Epub 2015 May 5. [Article]
Drug created at September 16, 2015 21:09 / Updated at April 23, 2024 11:38