2020 February: RECENT PUBLICATIONS 


Transporter structure

  • FASEB J. 2020;In press. ABCG2 requires a single aromatic amino acid to "clamp" substrates and inhibitors into the binding pocket. Gose T, Shafi T, Fukuda Y, Das S, Wang Y, Allcock A, Gavan McHarg A, Lynch J, Chen T, Tamai I, Shelat A, Ford RC, Schuetz JD. PubMed

Protein concentrations in human tissues

  • NAR Genomics and Bioinformatics, Volume 2, Issue 1, March 2020. Global variability analysis of mRNA and protein concentrations across and within human tissues. Wegler C, Ölander M, Wiśniewski RJ, Lundquist P, Zettl K, Åsberg A, Hjelmesæth J, AnderssonTB, Artursson P. PubMed

New insight into bile flow

  • J Pharmacol Exp Ther. 2019;371:713–717. Hepatic bile formation: Canalicular osmolarity and paracellular and transcellular water flow. Marinelli RA, Vore M, Javitt NB. PubMed

Transporters and liver disease

  • Pharmacol Rev. 2020;72:343-379. Solute Carrier Transporters as potential targets for the treatment of metabolic disease. Schumann T, König J, Henke C, Willmes DM, Bornstein SR, Jordan J, Fromm MF, Birkenfeld AL. PubMed
  • Can J Gastroenterol Hepatol. 2019;2019:1085717.  Expression analysis of ATP-Binding Cassette Transporters ABCB11 and ABCB4 in primary sclerosing cholangitis and variety of pediatric and adult cholestatic and noncholestatic liver diseases. Thoeni C, Waldherr R, Scheuerer J, Schmitteckert S, Roeth R, Niesler B, Cutz E, Flechtenmacher C, Goeppert B, Schirmacher P, Lasitschka F. PubMed
  • Pharmacol Rev. 2020;72:253-319. Organic Cation Transporters in Health and Disease. Koepsell H. PubMed
  • J Pharmacol Exp Ther. 2020;372:308-319. Profiling of drug-metabolizing enzymes and transporters in human tissue biopsy samples: A review of the literature. Rodrigues AD, Rowland A. PubMed
  • Biochem Pharmacol. 2019;174:113780. Interaction of Oatp1b2 expression and nonalcoholic steatohepatitis on pravastatin plasma clearance. Toth EL, Clarke JD, Csanaky IL, Cherrington NJ. PubMed
  • Expert Opin Drug Metab Toxicol. 2020;In press. Modulation of expression/function of intestinal P-glycoprotein under disease states. Murakami T, Bodor E, Bodor N. PubMed

Liver imaging

  • Liver Int. 2020;40:447-455. [18F]-Fluoro-2-deoxy-D-galactose positron emission tomography/computed tomography as complementary imaging tool in patients with hepatocellular carcinoma. Bak-Fredslund KP, Keiding S, Villadsen GE, Kramer S, Schlander S, Sørensen M. PubMed
  • Eur J Radiol. 2020 ;In press. Evaluating hepatotoxic effects of chemotherapeutic agents with gadoxetic-acid-enhanced magnetic resonance imaging. Theilig D, Elkilany A, Jann H, Roderburg C, Hamm B, Fehrenbach U, Geisel D. PubMed
  • Eur Radiol. 2020;In press. Gadoxetic acid-enhanced MR imaging for hepatocellular carcinoma: molecular and genetic background. Kitao A, Matsui O, Yoneda N, Kozaka K, Kobayashi S, Koda W, Inoue D, Ogi T, Yoshida K, Gabata T. PubMed
  • Nucl Med Biol. 2020;In press. Automated two-step manufacturing of [11C]glyburide radiopharmaceutical for PET imaging in humans. Caillé F, Gervais P, Auvity S, Coulon C, Marie S, Tournier N, Kuhnast B. PubMed
  • Drug Metab Pharmacokinet. 2020;35:76-88. Recent progress in in vivo phenotyping technologies for better prediction of transporter-mediated drug-drug interactions. Maeda K. For monitoring the organ concentration of drugs, positron emission tomography can be a powerful tool. PubMed
  • Expert Opin Drug Metab Toxicol. 2020:1-16. Use of imaging to assess the activity of hepatic transporters. Hernández Lozano I, Langer O. PubMed

Cancer treatment

  • Clin Pharmacol Ther. 2020;In press. Higher systemic exposure to unbound active metabolites of regorafenib is associated with short progression-free survival in colorectal cancer patients. Kubota Y, Fujita KI, Takahashi T, Sunakawa Y, Ishida H, Hamada K, Ichikawa W Tsunoda T, Shimada K, Masuo Y, Kato Y, Sasaki Y. PubMed

Prediction of hepatic clearance

  • Drug Metab Pharmacokinet. 2020;35:56-70. Recent advances in preclinical in vitro approaches towards quantitative prediction of hepatic clearance and drug-drug interactions involving organic anion transporting polypeptide (OATP) 1B transporters. Nozaki Y, Izumi SPubMed
  • Drug Metab Pharmacokinet. 2020;35:18-29. Identification and quantitation of enzyme and transporter contributions to hepatic clearance for the assessment of potential drug-drug interactions. Kimoto E, Obach RS, Varma MVS. PubMed

Transporter expression/function

  • J Pharmacol Exp Ther. 2020;372:46-53. Plasma membrane cholesterol regulates the allosteric binding of 1-Methyl-4-Phenylpyridinium to Organic Cation Transporter 2 (SLC22A2). Hörmann S, Gai Z, Kullak-Ublick GA, Visentin M. PubMed
  • J Pharm Pharm Sci. 2019;22:567-575. Probe cocktail to assess transporter function in Sandwich-Cultured Human Hepatocytes. Guo C, Brouwer KLR, Brouwer KR, Stewart PW, Mosley C. PubMed
  • Biochem Pharmacol. 2020;In press. Nicotinic acid transport into human liver involves organic anion transporter 2 (SLC22A7). Mathialagan S, Bi YA, Costales C, Kalgutkar AS, Rodrigues AD, Varma MVS. PubMed
  • Drug Metab Dispos. 2020;48:93-105. Pharmacokinetics of Organic Cation Transporter 1 (OCT1) substrates in Oct1/2 knockout mice and species difference in hepatic OCT1-mediated uptake. Morse BL, Kolur A, Hudson LR, Hogan AT, Chen LH, Brackman RM, Sawada GA, Fallon JK, Smith PC, Hillgren KM. PubMed
  • Drug Metab Dispos. 2020;In press. MRP3 is responsible for the efflux transport of Curcumin glucuronide from hepatocytes to the blood. Jia YM, Zhu T, Zhou H, Ji JZ, Tai T, Xie HG. PubMed
  • Drug Metab Dispos. 2020;48:205–216. Induction of human intestinal and hepatic Organic Anion Transporting Polypeptides; Where is the evidence for its relevance in Drug-Drug Interactions? Rodrigues AD, Lai Y, Shen H, Varma MVS, Rowland A, Oswald S. PubMed
  • AAPS J. 2019;22:16. Impact of Interleukin-6 on drug-metabolizing enzymes and transporters in intestinal cells. Simon F, Garcia J, Guyot L, Guitton J, Vilchez G, Bardel C, Chenel M, Tod M, Payen L. PubMed
  • J Pharm Pharm Sci. 2019;22:576-584. Decrease in Multidrug Resistance-associated Protein 2 activities by knockdown of Phosphatidylinositol 4-phosphate 5-kinase in hepatocytes and cancer cells. Kawase A, Inoue, Hirosoko M, Sugihara Y, Shimada H, Iwaki M. PubMed

Machine learning and transporters

  • J Biol Chem. 2020. pii: jbc.RA119.010729. Unique metabolite preferences of the drug transporters OAT1 and OAT3 analyzed by machine learning. Nigam AK, Li JG, Lall K, Shi D, Bush KT2 Bhatnagar V, Abagyan R, Nigam SK. PubMed

Transporters and Gut-Liver-Kidney axis

  • Sci Rep. 2019 ;9:11879. A Network of SLC and ABC transporter and DME genes involved in remote sensing and signaling in the Gut-Liver-Kidney axis. Rosenthal SB, Bush KT, Nigam SK. PubMed

Liver concentrations

  • Clin Pharmacol Ther. 2020;In press. Fine-Needle Aspiration for the evaluation of hepatic pharmacokinetics of Vaniprevir: a randomized trial in patients with hepatitis C Virus infection. Gao W, Webber AL, Maxwell J, Anderson M, Caro L, Chung C, Miltenburg AMM, Popa S, Van Dyck K, Wenning L, Mangin E, Fandozzi C, Railkar R, Shire NJ, Fraser I, Howell B, Talal AH, Stoch SA. PubMed
  • AAPS J. 2020;22:20. Estimation of the effect of OAT2-mediated active uptake on Meloxicam exposure in the human liver. Li R, Mathialagan S, Novak JJ, Eng H, Riccardi K, Litchfield J. PubMed

Drug-induced liver injury

  • Nat Rev Drug Discov. 2020;19:131-148. Managing the challenge of drug-induced liver injury: a roadmap for the development and deployment of preclinical predictive models. Weaver RJ, Blomme EA, Chadwick AE, Copple IM, Gerets HHJ, Goldring CE, Guillouzo A, Hewitt PG, Ingelman-Sundberg M, Jensen KG, Juhila S, Klingmüller U, Labbe G, Liguori MJ, Lovatt CA, Morgan P, Naisbitt DJ, Pieters RHH, Snoeys J, van de Water B, Williams DP, Park BK. PubMed