Molecule Information

General Information of the Molecule (ID: Mol00210)

• Name: Solute carrier family 21 member 8 (SLC21A8) ,Homo sapiens
• Synonyms: Liver-specific organic anion transporter 2; LST-2; Organic anion transporter 8; Organic anion-transporting polypeptide 8; OATP-8; Solute carrier family 21 member 8; LST2; OATP1B3; OATP8; SLC21A8
• Molecule Type: Protein
• Gene Name: SLCO1B3
• Gene ID: 28234
• Location: chr12:20810702-20916911[+]
• Sequence:
  MDQHQHLNKTAESASSEKKKTRRCNGFKMFLAALSFSYIAKALGGIIMKISITQIERRFD
  ISSSLAGLIDGSFEIGNLLVIVFVSYFGSKLHRPKLIGIGCLLMGTGSILTSLPHFFMGY
  YRYSKETHINPSENSTSSLSTCLINQTLSFNGTSPEIVEKDCVKESGSHMWIYVFMGNML
  RGIGETPIVPLGISYIDDFAKEGHSSLYLGSLNAIGMIGPVIGFALGSLFAKMYVDIGYV
  DLSTIRITPKDSRWVGAWWLGFLVSGLFSIISSIPFFFLPKNPNKPQKERKISLSLHVLK
  TNDDRNQTANLTNQGKNVTKNVTGFFQSLKSILTNPLYVIFLLLTLLQVSSFIGSFTYVF
  KYMEQQYGQSASHANFLLGIITIPTVATGMFLGGFIIKKFKLSLVGIAKFSFLTSMISFL
  FQLLYFPLICESKSVAGLTLTYDGNNSVASHVDVPLSYCNSECNCDESQWEPVCGNNGIT
  YLSPCLAGCKSSSGIKKHTVFYNCSCVEVTGLQNRNYSAHLGECPRDNTCTRKFFIYVAI
  QVINSLFSATGGTTFILLTVKIVQPELKALAMGFQSMVIRTLGGILAPIYFGALIDKTCM
  KWSTNSCGAQGACRIYNSVFFGRVYLGLSIALRFPALVLYIVFIFAMKKKFQGKDTKASD
  NERKVMDEANLEFLNNGEHFVPSAGTDSKTCNLDMQDNAAAN
• Function: Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
• Uniprot ID: SO1B3_HUMAN
• Ensembl ID: ENSG00000111700
• HGNC ID: HGNC:10961

Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens

Type(s) of Resistant Mechanism of This Molecule

  IDUE: Irregularity in Drug Uptake and Drug Efflux

Drug Resistance Data Categorized by Drug

Approved Drug(s) 1 drug(s) in total

Rosuvastatin

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Disease Class: Hyperlipidemia [1]

• Sensitive Disease: Hyperlipidemia [ICD-11: 5C80.Z]
• Sensitive Drug: Rosuvastatin
• Molecule Alteration: Expression; Down-regulation
• Experimental Note: Identified from the Human Clinical Data
• Mechanism Description: Enasidenib (and its metabolite, AGI-16903) at clinically relevant concentrations has effects on multiple drug metabolic enzymes and transporters, including inhibition of P-gp, BCRP, OATP1B1, and OATP1B3 transporters. When a single dose of rosuvastatin was administered together with 28 days of dosing of enasidenib, the AUC0-30 and AUC0-inf of rosuvastatin increased by =249% and 244%, respectively; and the Cmax increased by 366%, when compared to the single dose of rosuvastatin administered alone.

Disease- and Tissue-specific Abundances of This Molecule

ICD Disease Classification 05

Hyperlipoproteinaemia [ICD-11: 5C80]

Differential expression of molecule in resistant diseases

• The Studied Tissue: Whole blood
• The Specified Disease: Familial hypercholesterolemia
• The Expression Level of Disease Section Compare with the Healthy Individual Tissue: p-value: 1.65E-01; Fold-change: -6.07E-02; Z-score: -3.77E-01

References

• Ref 1: Assessment of Transporter-Mediated Drug Interactions for Enasidenib Based on a Cocktail Study in Patients With Relapse or Refractory Acute Myeloid Leukemia or Myelodysplastic Syndrome. J Clin Pharmacol. 2022 Apr;62(4):494-504. doi: 10.1002/jcph.1979. Epub 2021 Oct 27.