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  2. The organic anion transporting polypeptides OATP1B1 and OATP1B3 are membrane proteins that mediate uptake of drugs into the liver for subsequent conjugation and biliary excretion, a key step in drug elimination from the human body.
    DOI: 10.1038/s41467-023-41552-8
    Publication: Nat Commun. 2023; 14: 5774.
    Published: 2023

    Structure of human drug transporters OATP1B1 and OATP1B3

    www.ncbi.nlm.nih.gov/pmc/articles/PMC10507018/
    www.ncbi.nlm.nih.gov/pmc/articles/PMC10507018/
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    What are OATP1B1 and OATP1B3 transporters?
    OATP1B1 and OATP1B3 are transporters that are expressed on the sinusoidal membrane of hepatocytes; they accept a number of therapeutic reagents as their substrates. In vitro and in vivo studies have shown that some drugs inhibit these transporters and cause clinically relevant drugdrug interactions (DDIs).

    Clinical Importance of OATP1B1 and OATP1B3 in Drug­Drug

    sciencedirect.com
    What is OATP1B1 & OATP1B3?
    OATP1B1 and OATP1B3 mediate the hepatic uptake of many clinically important drugs (e.g., the 3-hydroxy-3-methylglutaryl-coenzyme (HMG-CoA) reductase inhibitors, anti-diabetics, anti-cancers) and endogenous compounds (e.g., bile acids) .

    Regulation of Organic Anion Transporting Polypeptides (OATP) 1B1- and

    ncbi.nlm.nih.gov
    What are ATP1B1 & OATP1B3 substrates?
    Although named “organic anion” transporter, OATP1B1 and OATP1B3 transport anionic, cationic, zwitterionic, and neutral lipophilic drugs; substrates are mainly amphipathic organic anions with a molecular weight greater than 300 Da ( Hagenbuch and Stieger, 2013 ).

    Elucidation of OATP1B1 and 1B3 transporter function using transgenic …

    sciencedirect.com
    Does inhibition of OATP1B1 and -1B3 cause drug-drug interactions?
    This review focuses on OATP1B1 and -1B3, which are specifically expressed in the liver and considered to be of particular importance for hepatic drug elimination and drug pharmacokinetics. Recent literature has indicated that inhibition of these transporters may result in drug-drug interactions.

    Role of the liver-specific transporters OATP1B1 and OATP1B3

    pubmed.ncbi.nlm.nih.gov
    What are the key findings in OATP1B1 structure?
    The key findings in our OATP1B1 structure are the location, shape and chemical nature of the drug binding pocket. Given that one of the main functions of OATP1B1 and OATP1B3 is drug uptake, our OATP1B1 structure captured a state prior to cytoplasmic substrate release. We propose that the transport can be thought to involve at least three states.

    Structure of human drug transporters OATP1B1 and OATP1B3

    nature.com
    Where are OATP1B1 and 1B3 located?
    OATP1B1, 1B3 and 2B1 are mainly located at the sinusoidal membranes of human hepatocytes and mediate the influx of their substrates from blood into the hepatocytes, and may thus represent an important step preceding elimination of drugs by metabolism or biliary excretion (Niemi, 2007).

    Impact of OATP transporters on pharmacokinetics - PMC

    ncbi.nlm.nih.gov
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  4. National Center for Biotechnology Information
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7559291

    Role of OATP1B1 and OATP1B3 in Drug-Drug Interactions Mediated by Tyrosine Kinase Inhibitors

     
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  5. Nature
    https://www.nature.com/articles/s41467-023-41552-8

    Structure of human drug transporters OATP1B1 and OATP1B3

    Tags:
    Oatp1b1 and Oatp1b3
    Oatp1b1 Drugs
    Organic anion
  6. National Center for Biotechnology Information
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5877716

    Regulation of Organic Anion Transporting Polypeptides (OATP) …

    Tags:
    Oatp1b1 and Oatp1b3
    Organic anion
    Presidential Memorial Certificate
  7. Studies of oatp1b1 and oatp1b3
    National Center for Biotechnology Information
    Regulation of Organic Anion Transporting Polypeptides (OATP) 1B1- and OATP1B3-Mediated Transport: An Updated Review in the Context of OATP-Mediated Drug-Drug Interactions
    Organic anion transporting polypeptides (OATP) 1B1 and OATP1B3 are important hepatic transporters that mediate the uptake of many clinically important drugs, including statins from the blood into the liver. Reduced transport function of OATP1B1 and OATP1B3 can lead to clinically relevant drug-drug i...
    Author: Khondoker Ala…
    Published: 2018/03
    Publication: Int J Mol …
    PubMed
    Clinical importance of OATP1B1 and OATP1B3 in drug-drug interactions
    OATP1B1 and OATP1B3 are transporters that are expressed on the sinusoidal membrane of hepatocytes; they accept a number of therapeutic reagents as their substrates. In vitro and in vivo studies have shown that some drugs inhibit these transporters and cause clinically relevant drug-drug interactions...
    Author: Yoshihisa Shit…
    Published: 2011/6
    Keywords: National In…
    National Center for Biotechnology Information
    Assessing OATP1B1- and OATP1B3-mediated drug-drug interaction potential of vemurafenib using R-value and physiologically based pharmacokinetic models
    Organic anion transporting polypeptides (OATP) 1B1 and OATP1B3 are hepatic transport proteins that mediate the sinusoidal uptake of a variety of drugs (e.g. lipid lowering statins, anti-cancer drugs, and antibiotics). Inhibition of OATP1B1- and OATP1B3-mediated transport by co-administration with dr...
    Author: Ruhul Kayesh…
    Published: 2021/01
    DOI: 10.1016/j.xphs.20…
    PubMed
    Role of OATP1B1 and OATP1B3 in Drug-Drug Interactions Mediated by Tyrosine Kinase Inhibitors
    Failure to recognize important features of a drug's pharmacokinetic characteristics is a key cause of inappropriate dose and schedule selection, and can lead to reduced efficacy and increased rate of adverse drug reactions requiring medical intervention. As oral chemotherapeutic agents, tyrosine kin...
    Author: Dominique A …
    Published: 2020/09/09
    Keywords: OATP1B1; …
    ScienceDirect
    Invited Review Article Elucidation of OATP1B1 and 1B3 transporter function using transgenic rodent models and commonly known single nucleotide polymorphisms
    The clearance of many drugs from the blood into the liver, such as the statins, is dependent on the organic anion transporting polypeptides (OATPs). Patients with *5 and *15 polymorphisms of OATP1B1 remove less of the statin as it traverses the liver and thus more reaches the rest of the body, inclu...
    Published: 2020/07/15
    Cited By: 0
    Keywords: OATP1B1; …
    PubMed
    Structure of human drug transporters OATP1B1 and OATP1B3
    The organic anion transporting polypeptides OATP1B1 and OATP1B3 are membrane proteins that mediate uptake of drugs into the liver for subsequent conjugation and biliary excretion, a key step in drug elimination from the human body. Polymorphic variants of these transporters can cause reduced drug cl...
    Author: Anca-Denise …
    Published: 2023/09/18
    Keywords: National In…
    National Center for Biotechnology Information
    Impact of OATP transporters on pharmacokinetics
    Membrane transporters are now recognized as important determinants of the transmembrane passage of drugs. Organic anion transporting polypeptides (OATP) form a family of influx transporters expressed in various tissues important for pharmacokinetics. Of the 11 human OATP transporters, OATP1B1, OATP1...
    Author: A Kalliokoski, …
    Published: 2009/10
    Publication: Br J Phar…
    National Center for Biotechnology Information
    Structure of human drug transporters OATP1B1 and OATP1B3
    The liver facilitates vital processes due to its strategic location between the gut and the systemic circulation. It is exposed to most nutrients and xenobiotics, and consequently has a central role in protecting the body from toxic compounds by metabolism and excretion. These processes require the ...
    Author: Anca-Denise …
    Published: 2023
    Publication: Nat Com…
    PubMed
    Organic anion transporting polypeptide (OATP)1B1 and OATP1B3 as important regulators of the pharmacokinetics of substrate drugs
    Nobody doubts the importance of organic anion transporting polypeptide (OATP)1B1 and 1B3 in the clinical pharmacokinetics of substrate drugs. Based on the theory of pharmacokinetics, even if a drug is eliminated from the body by extensive metabolism, the rate-determining process of the hepatic intri...
    Author: Kazuya Maeda
    Published: 2015
    Keywords: National In…
    National Center for Biotechnology Information
    OATPs, OATs and OCTs: the organic anion and cation transporters of the SLCO and SLC22A gene superfamilies
    The human organic anion and cation transporters are classified within two SLC superfamilies. Superfamily SLCO (formerly SLC21A) consists of organic anion transporting polypeptides (OATPs), while the organic anion transporters (OATs) and the organic cation transporters (OCTs) are classified in the SL...
    Author: Megan Roth, A…
    Published: 2012/03
    Publication: Br J Phar…
    National Center for Biotechnology Information
    Complete OATP1B1 and OATP1B3 deficiency causes human Rotor syndrome by interrupting conjugated bilirubin reuptake into the liver
    Bilirubin, a breakdown product of heme, is normally glucuronidated and excreted by the liver into bile. Failure of this system can lead to a buildup of conjugated bilirubin in the blood, resulting in jaundice. The mechanistic basis of bilirubin excretion and hyperbilirubinemia syndromes is largely u...
    Author: Evita van de S…
    Published: 2012/02/02
    Publication: J Clin Inv…
    PubMed
    Role of the liver-specific transporters OATP1B1 and OATP1B3 in governing drug elimination
    Members of the organic anion transporting polypeptide (OATP) family are responsible for the cellular uptake of a broad range of endogenous compounds and xenobiotics in multiple tissues. This review focuses on OATP1B1 and -1B3, which are specifically expressed in the liver and considered to be of par...
    Author: Nicola F Smith
    Published: 2005/10
    Keywords: National In…
  8. PubMed
    https://pubmed.ncbi.nlm.nih.gov/21297316

    Clinical importance of OATP1B1 and OATP1B3 in drug-drug

    Tags:
    Oatp1b1 and Oatp1b3
    Oatp1b1 Drugs
    Yoshihisa Shitara
    Publish Year:2011
  9. National Center for Biotechnology Information
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7750294

    Assessing OATP1B1- and OATP1B3-mediated drug-drug …

    Tags:
    Organic anion
    Presidential Memorial Certificate
    Oatp Drugs
    Publish Year:2021
  10. Taylor & Francis Online
    https://www.tandfonline.com/doi/full/10.10…

    The role of OATP1B1 and OATP1B3 transporter …

    WEBAug 30, 2022 · OATP1B1 and OATP1B3 are important members of the SLC superfamily of transporters, and polymorphic variants of these proteins have profound implications for the pharmacokinetic profile of an increasingly …

    Tags:
    Oatp1b1 and Oatp1b3
    Oatp1b1 Drugs
    Oatp1b1 Transporter
  11. Nature
    https://www.nature.com/articles/s41467-023-41552-8.pdf
    [PDF]

    Structure of human drug transporters OATP1B1 and OATP1B3

    Tags:
    Oatp1b1 and Oatp1b3
    Oatp1b1 Drugs
    Organic anion
  12. PubMed
    https://pubmed.ncbi.nlm.nih.gov/32916864

    Role of OATP1B1 and OATP1B3 in Drug-Drug Interactions …

    Tags:
    Oatp1b1 and Oatp1b3
    Publish Year:2020
  13. MDPI
    https://www.mdpi.com/1999-4923/12/9/856

    Role of OATP1B1 and OATP1B3 in Drug-Drug Interactions …

    Tags:
    Oatp1b1 Drugs
    Publish Year:2020
    Clinical Drug Interaction Oatp1b3
  14. ACS Publications
    https://pubs.acs.org/doi/10.1021/acs.molp…

    Preclinical Mouse Models To Study Human OATP1B1

    WEBOct 16, 2015 · OATP1B1 and OATP1B3 are human hepatic uptake transporters that can mediate liver uptake of a wide variety of drugs. Recently, we generated transgenic mice with liver-specific expression of …

    Tags:
    Oatp1b1 and Oatp1b3
    Mice Oatp1b1
    Clinical Drug Interaction Oatp1b3
  15. Wikipedia
    https://en.wikipedia.org/wiki/Organo_anion_transporter_family

    Organo anion transporter family - Wikipedia

    Tags:
    Oatp1b1 and Oatp1b3
    Oatps
  16. ScienceDirect
    https://www.sciencedirect.com/science/article/pii/S1347436715305759

    Clinical Importance of OATP1B1 and OATP1B3 in Drug

    Tags:
    Oatp1b1 and Oatp1b3
    Oatp1b1 Drugs
    Yoshihisa Shitara
    Publish Year:2011
  17. Nature
    https://www.nature.com/articles/s41422-023-00870-8

    Cryo-EM structures of human organic anion transporting …

    Tags:
    Organic anion-transporting polypeptide
    Cryo-electron microscopy
  18. ScienceDirect
    https://www.sciencedirect.com/science/article/pii/S0041008X20301630

    Elucidation of OATP1B1 and 1B3 transporter function using …

    Tags:
    Oatp1b1 and Oatp1b3
    Publish Year:2020
    Oatp1b1 Transporter
    Mice Oatp1b1
  19. J-Stage
    https://www.jstage.jst.go.jp/article/dmpk/26/3/26_DMPK-10-RV-094/_pdf
    [PDF]

    Clinical Importance of OATP1B1 and OATP1B3 in Drug Drug …

    Tags:
    Oatp1b1 and Oatp1b3
    Oatp1b1 Drugs
    Yoshihisa Shitara
    Publish Year:2011
  20. PubMed
    https://pubmed.ncbi.nlm.nih.gov/37723174

    Structure of human drug transporters OATP1B1 and OATP1B3

    Tags:
    Oatp1b1 and Oatp1b3
    Oatp1b1 Drugs
    Organic anion
  21. National Center for Biotechnology Information
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2765590

    Impact of OATP transporters on pharmacokinetics - PMC

    Tags:
    Oatp1b1 and Oatp1b3
    Organic anion
    Oatp Drugs
    Oatp1b1 Gene
  22. National Center for Biotechnology Information
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10507018

    Structure of human drug transporters OATP1B1 and OATP1B3

    Tags:
    Oatp1b1 and Oatp1b3
    Oatp1b1 Drugs
    Organic anion
  23. ACS Publications
    https://pubs.acs.org/doi/10.1021/jm300212s

    Classification of Inhibitors of Hepatic Organic Anion Transporting ...

    Tags:
    Organic anion
    Publish Year:2012
    Oatp1b1 Transporter
    Biological classification
  24. PubMed
    https://pubmed.ncbi.nlm.nih.gov/25747975

    Organic anion transporting polypeptide (OATP)1B1 and …

    Tags:
    Oatp1b1 and Oatp1b3
    Oatp1b1 Drugs
    Oatp Drugs
    Oatp1b1 Mutation
  25. National Center for Biotechnology Information
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3372714

    OATPs, OATs and OCTs: the organic anion and cation …

    Tags:
    Oatp1b1 and Oatp1b3
    Organic anion
    Presidential Memorial Certificate
  26. National Center for Biotechnology Information
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3266790

    Complete OATP1B1 and OATP1B3 deficiency causes human …

    Tags:
    Oatp1b1 and Oatp1b3
    Presidential Memorial Certificate
    Publish Year:2012
  27. PubMed
    https://pubmed.ncbi.nlm.nih.gov/16863454

    Role of the liver-specific transporters OATP1B1 and OATP1B3 in …

    Tags:
    Oatp1b1 and Oatp1b3
    Publish Year:2005