Drug Transporter (DT) Information

General Information of DT
DT ID DTD0019
Gene Name SLC10A1
Protein Name Sodium/taurocholate cotransporting polypeptide
Gene ID
6554
UniProt ID
Q14973
TCDB ID
2.A.28.1.9
3D Structure

Modelled DT Structure

Method: multi-sequence alignment based machine learning

Detail: Structure Info

Synonyms Cell growth-inhibiting gene 29 protein; NTCP; Na(+)/bile acid cotransporter; Na(+)/taurocholate transport protein; SLC10A1; Sodium/bile acid cotransporter; Solute carrier family 10 member 1
DT Family Bile Acid:Na(+) Symporter (BASS) Family ;
Function This tranporter strictly dependent on the extracellular presence of sodium and exhibits broad substrate specificity and transports various non-bile acid organic compounds as well.
Disease(s) Hypercholesterolemia [ICD-11:5C80.0]
Hypothyroidism [ICD-11:5A00.2]
Hyperlipidaemia [ICD-11:5C8Z]
Endogenous Substrate(s) Bile acids; Bile conjugates; Steroids; Cholate; Tauroursodeoxycholate
Variability Data of This Drug Transporter (DT)

Regulatory Variability Data of This DT (VARIDT 4.0)

(α) Tissue Distribution Level of Sodium/taurocholate cotransporting polypeptide
Tissue Distribution Level (TD)

(β) Cell Distribution Level of Sodium/taurocholate cotransporting polypeptide
Cell Distribution Level (CD)

(γ) Organelle Distribution Level of Sodium/taurocholate cotransporting polypeptide
Organelle Distribution Level (Subc)

Regulatory Variability Data of This DT

(α) Microbiota Influence of Sodium/taurocholate cotransporting polypeptide
Microbiota Influence (MBI)

(β) Post-translational Modification of Sodium/taurocholate cotransporting polypeptide
Post-translational Modification (PTM)

(γ) Transcriptional Regulation of Sodium/taurocholate cotransporting polypeptide
Transcriptional Regulation (TSR)

(δ) Epigenetic Regulation of Sodium/taurocholate cotransporting polypeptide
Epigenetic Regulation (EGR)

(ε) Exogenous Modulation of Sodium/taurocholate cotransporting polypeptide
Exogenous Modulation (EGM)

Structural Variability Data of This DT

(β) Inter-species Structural Differences
Inter-species Structural Differences (ISD)

General Variability Data of This DT

(α) Genetic Polymorphisms of Sodium/taurocholate cotransporting polypeptide
Genetic Polymorphisms of This DT (GPD)

(β) Disease-specific Protein Abundances of Sodium/taurocholate cotransporting polypeptide
Disease-specific Protein Abundances of This DT (DPAD)

(γ) Species- and Tissue-specific DT Abundances
Species/Tissue-specific Protein Abundances of This DT (S/TPAD)
Molecular Transporting Profile of This DT

Full List of Drug(s) Transported by This DT

 Approved Drug

 Click to Show/Hide the Full List of Drug:           5 Drugs in Total
Drug Name Highest Status Detail Indication ICD 11 Ref
Cerivastatin
 Approved Drug Info Hyperlipidaemia 5C8Z [1]
Estrone sulfate
 Approved Drug Info Menopausal symptoms MF32 [2]
Liothyronine
 Approved Drug Info Hypothyroidism 5A00.2 [3]
Pitavastatin calcium
 Approved Drug Info Dyslipidaemias 5C8Z [4]
Rosuvastatin
 Approved Drug Info Hypercholesterolemia 5C80.0 [5]

 Withdrawn, Discontinued or Preclinical Drug

 Click to Show/Hide the Full List of Drug:           2 Drugs in Total
Drug Name Highest Status Detail Indication ICD 11 Ref
Sodium taurocholate
 Preclinical Drug Info Type 2 diabetes 5A11 [6]
Taurocholic acid
 Terminated Drug Info Type 2 diabetes 5A11 [7]

Endogenous Metabolites (EMs) Handled by This DT

 Endogenous Metabolites (EMs)

 Click to Show/Hide the Full List of EMs:           1 EMs in Total
EM Name PubChem CID Detail Experimental Material Ref
Bile acid unspecific N.A. EM Info Identified using mouse NASH model [8]

Drug-DT Affinity Assessed by Cell Line

 Approved Drug

 Click to Show/Hide the Full List of Drug:         39 Drugs in Total
Drug Name Highest Status Detail Cell Line Affinity Ref
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Estrone sulfate Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =27 microM [2]
Pitavastatin calcium Approved Drug Info Oocytes-NTCP Km =15.1 microM [4]
Pitavastatin calcium Approved Drug Info Oocytes-NTCP Km =15.1 microM [4]
Pitavastatin calcium Approved Drug Info Oocytes-NTCP Km =15.1 microM [4]
Pitavastatin calcium Approved Drug Info Oocytes-NTCP Km =15.1 microM [4]
Pitavastatin calcium Approved Drug Info Oocytes-NTCP Km =15.1 microM [4]
Pitavastatin calcium Approved Drug Info Oocytes-NTCP Km =15.1 microM [4]
Pitavastatin calcium Approved Drug Info Oocytes-NTCP Km =15.1 microM [4]
Pitavastatin calcium Approved Drug Info Oocytes-NTCP Km =15.1 microM [4]
Rosuvastatin Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =65 microM [5]
Rosuvastatin Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =65 microM [5]
Rosuvastatin Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =65 microM [5]
Rosuvastatin Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =65 microM [5]
Rosuvastatin Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =65 microM [5]
Rosuvastatin Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =65 microM [5]
Rosuvastatin Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =65 microM [5]
Rosuvastatin Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =65 microM [5]
Rosuvastatin Approved Drug Info Human cervical cancer cell line (Hela)-NTCP Km =65 microM [5]

 Withdrawn, Discontinued or Preclinical Drug

 Click to Show/Hide the Full List of Drug:         59 Drugs in Total
Drug Name Highest Status Detail Cell Line Affinity Ref
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.5 microM [2]
Sodium taurocholate Preclinical Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Sodium taurocholate Preclinical Drug Info Human embryonic kidney cells (HEK293)-NTCP Km =2.1 microM [6]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
Taurocholic acid Terminated Drug Info Human cervical cancer cell line (Hela)-NTCP Km =7.9 microM [7]
Taurocholic acid Terminated Drug Info Oocytes-NTCP Km =6.2 microM [9]
References
1 Differential effect of genetic variants of Na(+)-taurocholate co-transporting polypeptide (NTCP) and organic anion-transporting polypeptide 1B1 (OATP1B1) on the uptake of HMG-CoA reductase inhibitors. Xenobiotica. 2011 Jan;41(1):24-34.
2 Ethnicity-dependent polymorphism in Na+-taurocholate cotransporting polypeptide (SLC10A1) reveals a domain critical for bile acid substrate recognition. J Biol Chem. 2004 Feb 20;279(8):7213-22.
3 Identification of thyroid hormone transporters. Biochem Biophys Res Commun. 1999 Jan 19;254(2):497-501.
4 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
5 Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806.
6 Differential inhibition of rat and human Na+-dependent taurocholate cotransporting polypeptide (NTCP/SLC10A1)by bosentan: a mechanism for species differences in hepatotoxicity. J Pharmacol Exp Ther. 2007 Jun;321(3):1170-8.
7 Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity. J Pharmacol Exp Ther. 1999 Dec;291(3):1204-9.
8 Disruption of phospholipid and bile acid homeostasis in mice with nonalcoholic steatohepatitis. Hepatology. 2012 Jul;56(1):118-29.
9 Molecular cloning, chromosomal localization, and functional characterization of a human liver Na+/bile acid cotransporter. J Clin Invest. 1994 Mar;93(3):1326-31.

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