Regulation of Drug Transport Proteins—From Mechanisms to Clinical Impact: A White Paper on Behalf of the International Transporter Consortium

Regulation of OATP1B1 function by tyrosine kinase-mediated phosphorylation

(2021) Elizabeth Hayden et al.   CLINICAL CANCER RESEARCH

Molecular Regulation of Canalicular ABC Transporters

(2021) Amel Ben Saad et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Influence of YES1 Kinase and Tyrosine Phosphorylation on the Activity of OCT1

(2021) Muhammad Erfan Uddin et al.   Frontiers in Pharmacology

Exploring the Use of Serum‐Derived Small Extracellular Vesicles as Liquid Biopsy to Study the Induction of Hepatic Cytochromes P450 and Organic Anion Transporting Polypeptides

(2021) A. David Rodrigues et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

RNA editing enzyme ADAR1 governs the circadian expression of P-glycoprotein in human renal cells by regulating alternative splicing of the ABCB1 gene

(2021) Yuji Omata et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mapping the miRNA‐mRNA Interactome in Human Hepatocytes and Identification of Functional mirSNPs in Pharmacogenes

(2021) Nicholas R. Powell et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Expression and Function of Organic Anion Transporting Polypeptides in the Human Brain: Physiological and Pharmacological Implications

(2021) Anima M. Schäfer et al.   Pharmaceutics

Pre-incubation with OATP1B1 and OATP1B3 inhibitors potentiates inhibitory effects in physiologically relevant sandwich-cultured primary human hepatocytes

(2021) Taleah Farasyn et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Protein kinase C regulates organic anion transporter 1 through phosphorylating ubiquitin ligase Nedd4–2

(2021) Zhou Yu et al.   BMC Molecular and Cell Biology

Unraveling pleiotropic effects of rifampicin by using physiologically based pharmacokinetic modeling: Assessing the induction magnitude of P‐glycoprotein–cytochrome P450 3A4 dual substrates

(2021) Xian Pan et al.   CPT-Pharmacometrics & Systems Pharmacology

Alternative Splicing of the SLCO1B1 Gene: An Exploratory Analysis of Isoform Diversity in Pediatric Liver

(2020) Bianca D. Groen et al.   CTS-Clinical and Translational Science

S-Acylation modulates the function of the apical sodium-dependent bile acid transporter in human cells

(2020) Alexander L Ticho et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Intestinal P‐gp and Putative Hepatic OATP1B Induction: ITC Perspective on Drug Development Implications

(2020) Maciej J. Zamek‐Gliszczynski et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Proteasome Inhibitors Bortezomib and Carfilzomib Stimulate the Transport Activity of Human Organic Anion Transporter 1

(2020) Yunzhou Fan et al.   MOLECULAR PHARMACOLOGY

Short-chain fatty acids exert opposite effects on the expression and function of p-glycoprotein and breast cancer resistance protein in rat intestine

(2020) Qiu-shi Xie et al.   ACTA PHARMACOLOGICA SINICA

A Microdose Cocktail to Evaluate Drug Interactions in Patients with Renal Impairment

(2020) Daniel A. Tatosian et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Gestational Age–Dependent Abundance of Human Placental Transporters as Determined by Quantitative Targeted Proteomics

(2020) Olena Anoshchenko et al.   DRUG METABOLISM AND DISPOSITION

Regulation of Organic Anion Transporting Polypeptide 2B1 Expression by MicroRNA in the Human Liver

(2020) Ayaka Tajiri et al.   MOLECULAR PHARMACEUTICS

Post-transcriptional regulation of OATP2B1 transporter by a microRNA, miR-24

(2020) Weiyi Liu et al.   Drug Metabolism and Pharmacokinetics

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

(2020) Dominique A. Garrison et al.   Pharmaceutics

Ubiquitin-specific peptidase 8 regulates the trafficking and stability of the human organic anion transporter 1

(2020) Jinghui Zhang et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Assessing Transporter‐Mediated Natural Product‐Drug Interactions Via In vitro ‐ In Vivo Extrapolation: Clinical Evaluation With a Probe Cocktail

(2020) James T. Nguyen et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Clinical Aspects of Transporter-Mediated Drug-Drug Interactions

(2019) Arne Gessner et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

The impact of cigarette smoke exposure, COPD, or asthma status on ABC transporter gene expression in human airway epithelial cells

(2019) Jennifer A. Aguiar et al.   Scientific Reports

Activation of Protein Kinase A Stimulates SUMOylation, Expression, and Transport Activity of Organic Anion Transporter 3

(2019) Haoxun Wang et al.   AAPS Journal

Regulation of OCT2 transcriptional repression by histone acetylation in renal cell carcinoma

(2019) Qianying Zhu et al.   Epigenetics

Preincubation With Everolimus and Sirolimus Reduces Organic Anion-Transporting Polypeptide (OATP)1B1- and 1B3-Mediated Transport Independently of mTOR Kinase Inhibition: Implication in Assessing OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions

(2019) Taleah Farasyn et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Characterization of Plasma Membrane Localization and Phosphorylation Status of Organic Anion Transporting Polypeptide (OATP) 1B1 c.521 T>C Nonsynonymous Single-Nucleotide Polymorphism

(2019) Alexandra Crowe et al.   PHARMACEUTICAL RESEARCH

Toward a Consensus on Applying Quantitative Liquid Chromatography‐Tandem Mass Spectrometry Proteomics in Translational Pharmacology Research: A White Paper

(2019) Bhagwat Prasad et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

TRANSCRIPTIONAL AND POSTTRANSCRIPTIONAL REGULATION OF DUODENAL P-GLYCOPROTEIN AND MRP2 IN HEALTHY HUMAN SUBJECTS AFTER CHRONIC TREATMENT WITH RIFAMPIN AND CARBAMAZEPINE

(2019) Susanne Brueck et al.   MOLECULAR PHARMACEUTICS

Insulin-like Growth Factor 1 Modulates the Phosphorylation, Expression, and Activity of Organic Anion Transporter 3 through Protein Kinase A Signaling Pathway

(2019) Jinghui Zhang et al.   Acta Pharmaceutica Sinica B

microRNA‐206 modulates the hepatic expression of the organic anion‐transporting polypeptide 1B1

(2019) Tämer El Saadany et al.   LIVER INTERNATIONAL

Organic Anion-Transporting Polypeptide Genes Are Not Induced by the Pregnane X Receptor Activator Rifampin: Studies in Hepatocytes In Vitro and in Monkeys In Vivo

(2019) Congrong Niu et al.   DRUG METABOLISM AND DISPOSITION

Intestinal breast cancer resistance protein (BCRP) requires Janus kinase 3 activity for drug efflux and barrier functions in obesity

(2019) Jayshree Mishra et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Alternative polyadenylation of ABC-transporters of the C-family (ABCC1, ABCC2, ABCC3) and implications on post-transcriptional micro-RNA regulation

(2019) Oliver Bruhn et al.   MOLECULAR PHARMACOLOGY

Long-noncoding RNAs (lncRNAs) in drug metabolism and disposition, implications in cancer chemo-resistance

(2019) Yue Wang et al.   Acta Pharmaceutica Sinica B

Stimulatory effect on the transport mediated by organic anion transporting polypeptide 2B1

(2019) Jiro Ogura et al.   Asian Journal of Pharmaceutical Sciences

Induction of Human Intestinal and Hepatic Organic Anion Transporting Polypeptides: Where Is the Evidence for Its Relevance in Drug-Drug Interactions?

(2019) A. David Rodrigues et al.   DRUG METABOLISM AND DISPOSITION

Suppression of P-glycoprotein by cigarette smoke extract in human lung-derived A549/P-gp cells

(2019) Mikihisa Takano et al.   Drug Metabolism and Pharmacokinetics

Profiling of Drug-Metabolizing Enzymes and Transporters in Human Tissue Biopsy Samples: A Review of the Literature

(2019) A. David Rodrigues et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

LST-3TM12 is a member of the OATP1B family and a functional transporter

(2018) Vanessa Malagnino et al.   BIOCHEMICAL PHARMACOLOGY

Cytochrome P450 3A Induction Predicts P-glycoprotein Induction; Part 2: Prediction of Decreased Substrate Exposure After Rifabutin or Carbamazepine

(2018) Justin D. Lutz et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Cytochrome P450 3A Induction Predicts P-glycoprotein Induction; Part 1: Establishing Induction Relationships Using Ascending Dose Rifampin

(2018) Justin D. Lutz et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Transporter-Mediated Alterations in Patients With NASH Increase Systemic and Hepatic Exposure to an OATP and MRP2 Substrate

(2018) Izna Ali et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Disease-Associated Changes in Drug Transporters May Impact the Pharmacokinetics and/or Toxicity of Drugs: A White Paper From the International Transporter Consortium

(2018) Raymond Evers et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Beyond Competitive Inhibition: Regulation of ABC Transporters by Kinases and Protein-Protein Interactions as Potential Mechanisms of Drug-Drug Interactions

(2018) Rebecca R. Crawford et al.   DRUG METABOLISM AND DISPOSITION

Glucocorticoids modulate multidrug resistance transporters in the first trimester human placenta

(2018) Phetcharawan Lye et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Farnesoid X Receptor Agonists Obeticholic Acid and Chenodeoxycholic Acid Increase Bile Acid Efflux in Sandwich-Cultured Human Hepatocytes: Functional Evidence and Mechanisms

(2018) Cen Guo et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Genetic variations of the xenoreceptors NR1I2 and NR1I3 and their effect on drug disposition and response variability

(2018) Litaty Céphanoée Mbatchi et al.   PHARMACOGENOMICS

Post-translational modifications of transporters

(2018) Lindsay C. Czuba et al.   PHARMACOLOGY & THERAPEUTICS

Expression of clinically relevant drug-metabolizing enzymes along the human intestine and their correlation to drug transporters and nuclear receptors: an intra-subject analysis

(2018) Anja Fritz et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

JNK-AKT-NF-κB controls P-glycoprotein expression to attenuate the cytotoxicity of deoxynivalenol in mammalian cells

(2018) Xiaoming Li et al.   BIOCHEMICAL PHARMACOLOGY

Transporters in Drug Development: 2018 ITC Recommendations for Transporters of Emerging Clinical Importance

(2018) Maciej J. Zamek-Gliszczynski et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Can BSEP Inhibition Testing In Drug Discovery And Development Reduce Liver Injury Risk? - An International Transporter Consortium Perspective

(2018) J Gerry Kenna et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Dysregulation of mucosal membrane transporters and drug metabolizing enzymes in ulcerative colitis

(2018) Pascal Erdmann et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Role of N-glycosylation in the expression of human SLC26A2 and A3 anion transport membrane glycoproteins

(2018) Chloe L. Rapp et al.   Biochemistry and Cell Biology

From Endogenous Compounds as Biomarkers to Plasma‐Derived Nanovesicles as Liquid Biopsy; Has the Golden Age of Translational PK ‐ ADME ‐ DDI Science Finally Arrived?

(2018) David Rodrigues et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Protein Kinases C-Mediated Regulations of Drug Transporter Activity, Localization and Expression

(2017) Abdullah Mayati et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Impaired N-linked glycosylation of uptake and efflux transporters in human non-alcoholic fatty liver disease

(2017) John D. Clarke et al.   LIVER INTERNATIONAL

Clinically Relevant Multidrug Transporters Are Regulated by microRNAs along the Human Intestine

(2017) Henrike Bruckmueller et al.   MOLECULAR PHARMACEUTICS

Relationship between DNA Methylation in the 5′ CpG Island of theSLC47A1(Multidrug and Toxin Extrusion Protein MATE1) Gene and Interindividual Variability in MATE1 Expression in the Human Liver

(2017) Toshihiro Tanaka et al.   MOLECULAR PHARMACOLOGY

Preincubation-dependent and long-lasting inhibition of organic anion transporting polypeptide (OATP) and its impact on drug-drug interactions

(2017) Yoshihisa Shitara et al.   PHARMACOLOGY & THERAPEUTICS

N-linked glycans do not affect plasma membrane localization of multidrug resistance protein 4 (MRP4) but selectively alter its prostaglandin E2 transport activity

(2016) M. Fahad Miah et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Expression of organic cation transporter 1 (OCT1): unique patterns of indirect regulation by nuclear receptors and hepatospecific gene regulation

(2016) Lucie Hyrsova et al.   DRUG METABOLISM REVIEWS

Epigenetic regulation of drug transporter expression in human tissues

(2016) Takeshi Hirota et al.   Expert Opinion on Drug Metabolism & Toxicology

A novel miR-203-DNMT3b-ABCG2 regulatory pathway predisposing colorectal cancer development

(2016) Kenneth K.W. To et al.   MOLECULAR CARCINOGENESIS

Epigenetic activation of the drug transporter OCT2 sensitizes renal cell carcinoma to oxaliplatin

(2016) Yanqing Liu et al.   Science Translational Medicine

A phosphotyrosine switch regulates organic cation transporters

(2016) Jason A. Sprowl et al.   Nature Communications

Protein kinase C affects the internalization and recycling of organic anion transporting polypeptide 1B1

(2015) Mei Hong et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Regulation of ABC efflux transporters at blood-brain barrier in health and neurological disorders

(2015) Hisham Qosa et al.   BRAIN RESEARCH

Exploiting a novel miR-519c–HuR–ABCG2 regulatory pathway to overcome chemoresistance in colorectal cancer

(2015) Kenneth K.W. To et al.   EXPERIMENTAL CELL RESEARCH

Regulation of the expression of renal drug transporters in KEAP1-knockdown human tubular cells

(2015) Hyuk-Sang Jeong et al.   TOXICOLOGY IN VITRO

Nuclear Receptors, RXR, and the Big Bang

(2014) Ronald M. Evans et al.   CELL

What do drug transporters really do?

(2014) Sanjay K. Nigam   NATURE REVIEWS DRUG DISCOVERY

MicroRNAs as regulators of drug transporters, drug-metabolizing enzymes, and tight junctions: Implication for intestinal barrier function

(2014) Kenji Ikemura et al.   PHARMACOLOGY & THERAPEUTICS

FBXO15 regulates P-glycoprotein/ABCB1 expression through the ubiquitin-proteasome pathway in cancer cells

(2013) Kazuhiro Katayama et al.   CANCER SCIENCE

Signaling Pathways that Regulate Basal ABC Transporter Activity at the Blood- Brain Barrier

(2013) David Miller et al.   CURRENT PHARMACEUTICAL DESIGN

MiR-223 modulates multidrug resistance via downregulation of ABCB1 in hepatocellular carcinoma cells

(2013) Tao Yang et al.   EXPERIMENTAL BIOLOGY AND MEDICINE

Posttranslational Modifications of GLUT4 Affect Its Subcellular Localization and Translocation

(2013) Jessica Sadler et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Application of permeability‐limited physiologically-based pharmacokinetic models: Part II-prediction of p‐glycoprotein mediated drug–drug interactions with digoxin

(2013) Sibylle Neuhoff et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Modeling of Rifampicin-Induced CYP3A4 Activation Dynamics for the Prediction of Clinical Drug-Drug Interactions from In Vitro Data

(2013) Fumiyoshi Yamashita et al.   PLoS One

Impact of Efavirenz on Intestinal Metabolism and Transport: Insights From an Interaction Study With Ezetimibe in Healthy Volunteers

(2012) S Oswald et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Species differences in drug transporters and implications for translating preclinical findings to humans

(2012) Xiaoyan Chu et al.   Expert Opinion on Drug Metabolism & Toxicology

A Cancer-Specific Variant of the SLCO1B3 Gene Encodes a Novel Human Organic Anion Transporting Polypeptide 1B3 (OATP1B3) Localized Mainly in the Cytoplasm of Colon and Pancreatic Cancer Cells

(2012) Nilay Thakkar et al.   MOLECULAR PHARMACEUTICS

ABC drug transporter and nuclear receptor expression in human cytotrophoblasts: Influence of spontaneous syncytialization and induction by glucocorticoids

(2012) S. Manceau et al.   PLACENTA

N-glycosylation Dictates Proper Processing of Organic Anion Transporting Polypeptide 1B1

(2012) Juan Yao et al.   PLoS One

Interactions of Tyrosine Kinase Inhibitors with Organic Cation Transporters and Multidrug and Toxic Compound Extrusion Proteins

(2011) T. Minematsu et al.   MOLECULAR CANCER THERAPEUTICS

DNA methylation is associated with downregulation of the organic cation transporter OCT1 (SLC22A1) in human hepatocellular carcinoma

(2011) Elke Schaeffeler et al.   Genome Medicine

Up-regulation of connexin 32 gene by 5-aza-2′-deoxycytidine enhances vinblastine-induced cytotoxicity in human renal carcinoma cells via the activation of JNK signalling

(2010) Y. Takano et al.   BIOCHEMICAL PHARMACOLOGY

Liver X receptor α and farnesoid X receptor are major transcriptional regulators of OATP1B1

(2010) Henriette E. Meyer zu Schwabedissen et al.   HEPATOLOGY

Rapid Modulation of the Organic Anion Transporting Polypeptide 2B1 (OATP2B1, SLCO2B1) Function by Protein Kinase C-mediated Internalization

(2010) Kathleen Köck et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Membrane transporters in drug development

(2010)   NATURE REVIEWS DRUG DISCOVERY

DNA Methylation Profiles of Organic Anion Transporting Polypeptide 1B3 in Cancer Cell Lines

(2010) Sayaka Ichihara et al.   PHARMACEUTICAL RESEARCH

Pathophysiological regulation of renal SLC22A organic ion transporters in acute kidney injury: Pharmacological and toxicological implications

(2009) Hideyuki Saito   PHARMACOLOGY & THERAPEUTICS

Posttranslational regulation of Abcc2 expression by SUMOylation system

(2008) Satoko Minami et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Missense mutations and single nucleotide polymorphisms in ABCB11 impair bile salt export pump processing and function or disrupt pre-messenger RNA splicing

(2008) Jane A. Byrne et al.   HEPATOLOGY