SLCO1B3
Encyclopedia
Solute carrier organic anion transporter family member 1B3 (SLCO1B3) also known as organic anion-transporting polypeptide 1B3 (OATP1B3) is a protein
that in humans is encoded by the SLCO1B3 gene
.
OATP1B3 is a 12-transmembrane domain influx transporter. Normally expressed in the liver, the transporter functions to uptake large, non-polar drugs and hormones from the portal vein.
In addition, higher expression of OATP1B3 mRNA was also detected in testicular cancer.
Protein
Proteins are biochemical compounds consisting of one or more polypeptides typically folded into a globular or fibrous form, facilitating a biological function. A polypeptide is a single linear polymer chain of amino acids bonded together by peptide bonds between the carboxyl and amino groups of...
that in humans is encoded by the SLCO1B3 gene
Gene
A gene is a molecular unit of heredity of a living organism. It is a name given to some stretches of DNA and RNA that code for a type of protein or for an RNA chain that has a function in the organism. Living beings depend on genes, as they specify all proteins and functional RNA chains...
.
OATP1B3 is a 12-transmembrane domain influx transporter. Normally expressed in the liver, the transporter functions to uptake large, non-polar drugs and hormones from the portal vein.
Clinical significance
OATP1B3 has also been indentified as a transporter aberrantly expressed in prostate cancer and implicated in prostate cancer progression. Increasing mRNA expression of OATP1B3 was also correlated to prostate cancer Gleason score.In addition, higher expression of OATP1B3 mRNA was also detected in testicular cancer.
Substrates
Small molecules that are transported by SLCO1B3 include:- AmanitinAmanitinAmanitin may refer to several related amatoxins:* α-Amanitin* β-Amanitin* γ-Amanitin* ε-Amanitin...
- AtrasentanAtrasentanAtrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer.It is an endothelin receptor antagonist selective for subtype A...
- BilirubinBilirubinBilirubin is the yellow breakdown product of normal heme catabolism. Heme is found in hemoglobin, a principal component of red blood cells. Bilirubin is excreted in bile and urine, and elevated levels may indicate certain diseases...
- BosentanBosentanBosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary artery hypertension . It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer.-Mechanism of action:Bosentan is...
- BQ-123BQ-123BQ-123 is a cyclic peptide consisting of five amino acids. The amino acid sequence is D-tryptamine-D-aspartic acid-L-proline-D-valine-L-leucine....
- BromsulphthaleinBromsulphthaleinBromsulphthalein is a dye used in liver function tests. Its excretion is measured....
(BSP) - CDCA-NBD
- CholateCholic acidCholic acid is a bile acid, a white crystalline substance insoluble in water , with a melting point of 200-201 °C. Salts of cholic acid are called cholates. Cholic acid, along with chenodeoxycholic acid, is one of two major bile acids produced by the liver where it is synthesized from cholesterol...
(CA) - CholecystokininCholecystokininCholecystokinin is a peptide hormone of the gastrointestinal system responsible for stimulating the digestion of fat and protein...
octapeptide (CCK-8) - Dehydroepiandroserone-3-sulfate (DHEAS)
- Deltorphin II
- Demethylphalloin
- DigoxinDigoxinDigoxin INN , also known as digitalis, is a purified cardiac glycoside and extracted from the foxglove plant, Digitalis lanata. Its corresponding aglycone is digoxigenin, and its acetyl derivative is acetyldigoxin...
- Docetaxel
- [D-penicillamine2,5]enkephalin (DPDPE)
- EnalaprilEnalaprilEnalapril is an angiotensin converting enzyme inhibitor used in the treatment of hypertension and some types of chronic heart failure. ACE raises blood pressure by constricting blood vessels. ACE inhibitors like enalapril prevent this effect. Enalapril has been shown to lower the death rate in...
- Estradiol-17β-glucuronide 5–25
- Estrone-3-sulfateEstrone sulfateEstrone sulfate is a sulfated estrone.It has been described as a prognosis indicator for prostate cancer.It is a component of Premarin....
- FexofenadineFexofenadineFexofenadine is an antihistamine drug used in the treatment of hayfever and similar allergy symptoms...
- FluvastatinFluvastatinFluvastatin is a member of the drug class of statins, used to treat hypercholesterolemia and to prevent cardiovascular disease....
- Fluo-3
- GlutathioneGlutathioneGlutathione is a tripeptide that contains an unusual peptide linkage between the amine group of cysteine and the carboxyl group of the glutamate side-chain...
(GSH) - GlycocholateGlycocholic acidGlycocholic acid, or cholylglycine, is a crystalline bile acid involved in the emulsification of fats. It occurs as a sodium salt in the bile of mammals. It is a conjugate of cholic acid with glycine. Its anion is called glycocholate....
(GCA) - Glycoursodeoxycholate (GUDCA)
- IrinotecanIrinotecanIrinotecan is a drug used for the treatment of cancer.Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1. In chemical terms, it is a semisynthetic analogue of the natural alkaloid camptothecin....
- Leukotriene C4Leukotriene C4Leukotriene C4 is a leukotriene....
(LTC4) - MethotrexateMethotrexateMethotrexate , abbreviated MTX and formerly known as amethopterin, is an antimetabolite and antifolate drug. It is used in treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions. It acts by inhibiting the metabolism of folic acid. Methotrexate...
- MicrocystinMicrocystinMicrocystins are cyclic nonribosomal peptides produced by cyanobacteria . They are cyanotoxins and can be very toxic for plants and animals including humans. Their hepatotoxicity may cause serious damage to the liver. Microcystins can strongly inhibit protein phosphatases type 1 and 2A , and are...
- Monoglyucuronosyl
- OlmesartanOlmesartanOlmesartan medoxomil is an angiotensin II receptor antagonist used to treat high blood pressure.-Indications:...
- OuabainOuabainOuabain which is also named g-strophanthin, is a poisonous cardiac glycoside.-Sources:Ouabain is found in the ripe seeds of African plants Strophanthus gratus and the bark of Acokanthera ouabaio.-Function:...
- PaclitaxelPaclitaxelPaclitaxel is a mitotic inhibitor used in cancer chemotherapy. It was discovered in a U.S. National Cancer Institute program at the Research Triangle Institute in 1967 when Monroe E. Wall and Mansukh C. Wani isolated it from the bark of the Pacific yew tree, Taxus brevifolia and named it taxol...
- PhalloidinPhalloidinPhalloidin is one of a group of toxins from the death cap known as phallotoxins.-Background:Pioneering work on this toxin was done by the Nobel laureate Heinrich Wieland in the 1930s...
- PitavastatinPitavastatinPitavastatin is a member of the medication class of statins, marketed in the United States under the trade name Livalo. Like other statins, it is an inhibitor of HMG-CoA reductase, the enzyme that catalyses the first step of cholesterol synthesis. It has been available in Japan since 2003, and is...
- RifampicinRifampicinRifampicin or rifampin is a bactericidal antibiotic drug of the rifamycin group. It is a semisynthetic compound derived from Amycolatopsis rifamycinica ...
- Ro 48-5033 (BosentanBosentanBosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary artery hypertension . It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer.-Mechanism of action:Bosentan is...
metabolite) - RosuvastatinRosuvastatinRosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. It was developed by Shionogi.-Medical uses:The primary uses of rosuvastatin is for the treatment of dyslipidemia...
- SN-38SN-38SN-38 is the active metabolite of irinotecan ; it is 200 times more active than irinotecan itself.SN38 is metabolized via glucoronidation by UGT1A1....
- TaurocholateTaurocholic acidTaurocholic acid, known also as cholaic acid, cholyltaurine, or acidum cholatauricum, is a deliquescent yellowish crystalline bile acid involved in the emulsification of fats. It occurs as a sodium salt in the bile of mammals. It is a conjugate of cholic acid with taurine...
(TCA) - TaurochenodeoxycholateTaurochenodeoxycholic acidTaurochenodeoxycholic acid is a bile acidformed in the liver by conjugation of chenodeoxycholate with taurine, usually as the sodium salt. It acts as detergent to solubilise fats in the small intestine and is itself absorbed. It is used as a cholagogue and choleretic....
(TCDCA) - TaurodeoxycholateTaurodeoxycholic acidTaurodeoxycholic acid is a bile acid....
(TDCA) - TauroursodeoxycholateTaurochenodeoxycholic acidTaurochenodeoxycholic acid is a bile acidformed in the liver by conjugation of chenodeoxycholate with taurine, usually as the sodium salt. It acts as detergent to solubilise fats in the small intestine and is itself absorbed. It is used as a cholagogue and choleretic....
(TUDCA) - TelmisartanTelmisartanTelmisartan is an angiotensin II receptor antagonist used in the management of hypertension. It is marketed under the trade name Micardis , among others.-Administration:...
- ThyroxineThyroxineThyroxine, or 3,5,3',5'-tetraiodothyronine , a form of thyroid hormones, is the major hormone secreted by the follicular cells of the thyroid gland.-Synthesis and regulation:...
(T4) - TR-14035
- TriiodothyronineTriiodothyronineTriiodothyronine, C15H12I3NO4, also known as T3, is a thyroid hormone. It affects almost every physiological process in the body, including growth and development, metabolism, body temperature, and heart rate....
(T3) - ValsartanValsartanValsartan is an angiotensin II receptor antagonist , with particularly high affinity for the type I angiotensin receptor. By blocking the action of angiotensin, valsartan dilates blood vessels and reduces blood pressure...