Studies on the role of OATP2B1 in pharmacology and physiology

OATP2B1 (SLCO2B1, formerly OATP-B) is a member of the Organic Anion Transporting Polypeptide family of drug transporters. OATP2B1 is a membrane protein that facilitates cellular entry of its substrates and is ubiquitously expressed in the human organism. Its high abundance in intestine, liver and kidney is assumed to influence the handling of its substrates in these organs of pharmacokinetic relevance. However, even if it was first described in 2000 - its in vivo role still remains to be determined.

In the past, we have conducted multiple studies on the expression and function of OATP2B1 [1,2]. Within those studies we have identified substrates [6, 4]. Moreover we were able to describe mechanisms modifying its transcription [4] and mechanisms modifying its activity (post-transcriptional interaction with PDZK1) [5], whereby linking OATP2B1 more and more to other functions, but drug transport.

Within our ongoing research program on OATP2B1, we are focusing on the impact of this modulator of cellular entry on the pharmacology and physiology.


[1] Organic anion transporting polypeptide 2B1 and breast cancer resistance protein interact in the transepithelial transport of steroid sulfates in human placenta. Grube M, Reuther S, Meyer zu Schwabedissen H, Köck K, Draber K, Ritter CA, Fusch C, Jedlitschky G, Kroemer HK. Drug Metab Dispos. 2007; 35(1):30-5. (

[2] Characterization of OATP1B3 and OATP2B1 transporter expression in the islet of the adult human pancreas. Kim M, Deacon P, Tirona RG, Kim RB, Pin CL, Meyer zu Schwabedissen HE, Wang R, Schwarz UI. Histochem Cell Biol. 2017;148(4):345-357. doi: 10.1007/s00418-017-1580-6. (

[3] Expression of OATP2B1 as determinant of drug effects in the microcompartment of the coronary artery. Hussner J, Begunk R, Boettcher K, Gliesche DG, Prestin K, Meyer zu Schwabedissen HE. Vascul Pharmacol. 2015;72:25-34. doi: 10.1016/j.vph.2015.06.006. (

[4] Thyroid Hormones Are Transport Substrates and Transcriptional Regulators of Organic Anion Transporting Polypeptide 2B1. Meyer zu Schwabedissen HE, Ferreira C, Schaefer AM, Oufir M, Seibert I, Hamburger M, Tirona RG. Mol Pharmacol. 2018; 94(1):700-712. doi: 10.1124/mol.117.111161. (

[5] The scaffold protein PDZK1 modulates expression and function of the organic anion transporting polypeptide 2B1. Ferreira C, Hagen P, Stern M, Hussner J, Zimmermann U, Grube M, Meyer zu Schwabedissen HE. Eur J Pharm Sci. 2018;120:181-190. doi: 10.1016/j.ejps.2018.05.006. (

[6] Hyperforin-Induced Activation of the Pregnane X Receptor Is Influenced by the Organic Anion-Transporting Polypeptide 2B1. Schäfer AM, Potterat O, Seibert I, Fertig O, Meyer zu Schwabedissen HE. Mol Pharmacol. 2019; 95(3):313-323. doi: 10.1124/mol.118.114066.  (