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Identification of Glycochenodeoxycholate 3-O-Glucuronide and Glycodeoxycholate 3-O-Glucuronide as Highly Sensitive

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Glycochenodeoxycholate and glycodeoxycholate 3-O-glucuronides (GCDCA-3G and GDCA-3G) are specific biomarkers for organic anion transporting polypeptide 1B1 (OATP1B1) function. GCDCA-3G demonstrates high sensitivity and specificity for detecting OATP1B1 genotype variations.

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Area of Science:

  • Pharmacogenomics and Drug Metabolism
  • Biomarker Discovery
  • Hepatobiliary Transport

Background:

  • Organic anion transporting polypeptide 1B1 (OATP1B1) plays a crucial role in the hepatic uptake of various substances.
  • Genetic variations in the SLCO1B1 gene, which encodes OATP1B1, can significantly impact drug efficacy and toxicity.
  • Identifying reliable endogenous biomarkers for OATP1B1 activity is essential for personalized medicine.

Purpose of the Study:

  • To evaluate the sensitivity and specificity of endogenous glycochenodeoxycholate 3-O-glucuronide (GCDCA-3G) and glycodeoxycholate 3-O-glucuronide (GDCA-3G) as substrates for OATP1B1 in humans.
  • To investigate the association between plasma levels of GCDCA-3G and GDCA-3G and the SLCO1B1 rs4149056 polymorphism.
  • To determine the predominant OATP transporter responsible for the hepatic uptake of GCDCA-3G and GDCA-3G.

Main Methods:

  • Measurement of plasma GCDCA-3G and GDCA-3G levels using liquid chromatography-tandem mass spectrometry in 356 healthy volunteers.
  • Genome-wide association study (GWAS) to identify genetic variants associated with plasma GCDCA-3G and GDCA-3G concentrations.
  • In vitro uptake assays using cells expressing OATP1B1, OATP1B3, and OATP2B1 to determine transporter specificity.

Main Results:

  • Plasma levels of GCDCA-3G and GDCA-3G were significantly lower in women than in men.
  • The SLCO1B1 rs4149056 (c.521T>C) polymorphism was strongly associated with plasma GCDCA-3G and GDCA-3G concentrations, with higher levels observed in individuals with the c.521C/C genotype.
  • GCDCA-3G demonstrated high sensitivity (98-99%) and specificity (100%) in detecting the SLCO1B1 c.521C/C genotype, with distinct cutoff values for men and women.
  • In vitro studies confirmed that GCDCA-3G and GDCA-3G are preferentially transported by OATP1B1 compared to OATP1B3 and OATP2B1.

Conclusions:

  • Hepatic uptake of GCDCA-3G and GDCA-3G is primarily mediated by OATP1B1.
  • GCDCA-3G serves as a highly sensitive and specific endogenous biomarker for OATP1B1 activity and SLCO1B1 genotype in humans.
  • These findings support the use of GCDCA-3G as a valuable tool in pharmacogenomic studies and personalized medicine.