4.4 Review

Special Section on New Era of Transporter Science: Unraveling the Functional Role of Orphan Transporters-Minireview Transcriptional Regulation of Solute Carrier Drug Transporters

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Article Pharmacology & Pharmacy

Intestinal P-gp and Putative Hepatic OATP1B Induction: International Transporter Consortium Perspective on Drug Development Implications

Maciej J. Zamek-Gliszczynski et al.

Summary: The increasing interest in transporter induction highlights the importance of P-glycoprotein and OATP1B in drug absorption and disposition, as well as the potential for drug-drug interactions. Further research is needed to fully understand the clinical relevance and mechanisms of these interactions in order to inform drug development strategies.

CLINICAL PHARMACOLOGY & THERAPEUTICS (2021)

Article Biochemistry & Molecular Biology

A guide to plasma membrane solute carrier proteins

Mattia D. Pizzagalli et al.

Summary: This review provides an overview of the SLC superfamily of transporter proteins and their roles in regulating metabolism and environmental conditions at the cell surface, with a focus on their involvement in cancer development and progression.

FEBS JOURNAL (2021)

Review Biochemistry & Molecular Biology

Circadian regulation of transporter expression and implications for drug disposition

Jiri Pacha et al.

Summary: This review provides an overview of the circadian rhythmicity of drug transporters and their molecular mechanisms of circadian control, discussing evidence for coupling drug transporters to circadian oscillators and potential candidates for conveying circadian clock signals to target drug transporters, particularly transcription factors as the output of clock genes.

EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY (2021)

Article Oncology

Regulation of OATP1B1 Function by Tyrosine Kinase-mediated Phosphorylation

Elizabeth R. Hayden et al.

Summary: OATP1B1 is a major drug uptake transporter in the liver, and its activity can be significantly inhibited by various TKIs. The inhibition of OATP1B1 by TKIs can lead to reduced phosphorylation levels, affecting its transport function and pharmacokinetics of substrates like rosuvastatin. Identified Src kinase LYN as a potential regulator of OATP1B1 activity, highly sensitive to inhibition by clinically relevant concentrations of TKIs.

CLINICAL CANCER RESEARCH (2021)

Article Pharmacology & Pharmacy

Upregulation of histone acetylation reverses organic anion transporter 2 repression and enhances 5-fluorouracil sensitivity in hepatocellular carcinoma

Yingying Wang et al.

Summary: Hepatocellular carcinoma (HCC) is a common malignant tumor globally, with chemotherapy resistance often attributed to abnormal drug transporters. The study identified histone hypoacetylation as the mechanism behind OAT2 downregulation in HCC, and demonstrated that histone deacetylases inhibitor can reverse this state, enhancing drug uptake and sensitivity to chemotherapy in HCC cells.

BIOCHEMICAL PHARMACOLOGY (2021)

Article Cell Biology

Epigenetic regulation of intestinal peptide transporter PEPT1 as a potential strategy for colorectal cancer sensitization

Yanhong Wang et al.

Summary: The repression of PEPT1 in human colorectal cancer is due to DNA methylation mediated by DNMT1 and histone deacetylation mediated by HDAC1, which plays a vital role in the poor response of CRC to the common treatment ubenimex.

CELL DEATH & DISEASE (2021)

Review Pharmacology & Pharmacy

Organic Cation Transporters in Health and Disease

Hermann Koepsell

PHARMACOLOGICAL REVIEWS (2020)

Review Biochemistry & Molecular Biology

Role of SLC transporters in toxicity induced by anticancer drugs

Kevin M. Huang et al.

EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY (2020)

Review Neurosciences

The Role of the SLC Transporters Protein in the Neurodegenerative Disorders

Asli Aykac et al.

CLINICAL PSYCHOPHARMACOLOGY AND NEUROSCIENCE (2020)

Article Biochemistry & Molecular Biology

Farnesoid X Receptor Activation Stimulates Organic Cations Transport in Human Renal Proximal Tubular Cells

Teerasak Wongwan et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

Article Biochemistry & Molecular Biology

PPAR-alpha Deletion Attenuates Cisplatin Nephrotoxicity by Modulating Renal Organic Transporters MATE-1 and OCT-2

Leandro Ceotto Freitas-Lima et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

Article Biochemistry & Molecular Biology

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

Qianying Zhu et al.

EPIGENETICS (2019)

Article Multidisciplinary Sciences

Remote sensing and signaling in kidney proximal tubules stimulates gut microbiome-derived organic anion secretion

Jitske Jansen et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)

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OATP1B3-1B7, a novel organic anion transporting polypeptide, is modulated by FXR ligands and transports bile acids

Vanessa Malagnino et al.

AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY (2019)

Review Pharmacology & Pharmacy

The SLC22 Transporter Family: A Paradigm for the Impact of Drug Transporters on Metabolic Pathways, Signaling, and Disease

Sanjay K. Nigam

ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 58 (2018)

Review Biochemistry & Molecular Biology

The Human Transcription Factors

Samuel A. Lambert et al.

Review Pharmacology & Pharmacy

Molecular Modeling of Drug-Transporter Interactions-An International Transporter Consortium Perspective

Avner Schlessinger et al.

CLINICAL PHARMACOLOGY & THERAPEUTICS (2018)

Review Gastroenterology & Hepatology

The molecular functions of hepatocyte nuclear factors - In and beyond the liver

Hwee Hui Lau et al.

JOURNAL OF HEPATOLOGY (2018)

Review Pharmacology & Pharmacy

Post-translational modifications of transporters

Lindsay C. Czuba et al.

PHARMACOLOGY & THERAPEUTICS (2018)

Review Biochemistry & Molecular Biology

Transcriptional Regulation by Nrf2

Claudia Tonelli et al.

ANTIOXIDANTS & REDOX SIGNALING (2018)

Review Biophysics

Chromatin-remodeling for transcription

Yahli Lorch et al.

QUARTERLY REVIEWS OF BIOPHYSICS (2017)

Review Pharmacology & Pharmacy

Classification Systems of Secondary Active Transporters

Emelie Perland et al.

TRENDS IN PHARMACOLOGICAL SCIENCES (2017)

Review Pharmacology & Pharmacy

Loops and layers of post-translational modifications of drug transporters

Da Xu et al.

ADVANCED DRUG DELIVERY REVIEWS (2017)

Article Pharmacology & Pharmacy

Potentiating SLC transporter activity: Emerging drug discovery opportunities

Marie-Laure Rives et al.

BIOCHEMICAL PHARMACOLOGY (2017)

Review Biochemistry & Molecular Biology

The role and regulation of the peroxisome proliferator activated receptor alpha in human liver

Sander Kersten et al.

BIOCHIMIE (2017)

Article Biochemistry & Molecular Biology

Fluid shear stress stimulates MATE2-K expression via Nrf2 pathway activation

Yasunori Fukuda et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2017)

Review Biochemistry & Molecular Biology

SLC transporters as a novel class of tumour suppressors: identity, function and molecular mechanisms

Yangzom D. Bhutia et al.

BIOCHEMICAL JOURNAL (2016)

Review Biochemistry & Molecular Biology

The Functions of Histone Modification Enzymes in Cancer

Ruilin Wang et al.

CURRENT PROTEIN & PEPTIDE SCIENCE (2016)

Review Developmental Biology

ATP-dependent chromatin remodeling during mammalian development

Swetansu K. Hota et al.

DEVELOPMENT (2016)

Review Biochemistry & Molecular Biology

The regulation of human hepatic drug transporter expression by activation of xenobiotic-sensing nuclear receptors

David E. Amacher

EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY (2016)

Article Cell Biology

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

Yanqing Liu et al.

SCIENCE TRANSLATIONAL MEDICINE (2016)

Article Pharmacology & Pharmacy

Rifampin Regulation of Drug Transporters Gene Expression and the Association of MicroRNAs in Human Hepatocytes

Eric A. Benson et al.

FRONTIERS IN PHARMACOLOGY (2016)

Article Medicine, Research & Experimental

Effect of DNA methylation profile on OATP3A1 and OATP4A1 transcript levels in colorectal cancer

Agnieszka Anna Rawluszko-Wieczorek et al.

BIOMEDICINE & PHARMACOTHERAPY (2015)

Review Biochemistry & Molecular Biology

A Call for Systematic Research on Solute Carriers

Adrian Cesar-Razquin et al.

Review Biotechnology & Applied Microbiology

SLC transporters as therapeutic targets: emerging opportunities

Lawrence Lin et al.

NATURE REVIEWS DRUG DISCOVERY (2015)

Review Cell Biology

Transcriptional regulation of hepatic lipogenesis

Yuhui Wang et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2015)

Review Physiology

THE ORGANIC ANION TRANSPORTER (OAT) FAMILY: A SYSTEMS BIOLOGY PERSPECTIVE

Sanjay K. Nigam et al.

PHYSIOLOGICAL REVIEWS (2015)

Article Biochemistry & Molecular Biology

Nrf2 regulates the expression of the peptide transporter PEPT1 in the human colon carcinoma cell line Caco-2

Kerstin E. Geillinger et al.

BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS (2014)

Review Biochemistry & Molecular Biology

Pregnane X receptor and drug-induced liver injury

Yue-Ming Wang et al.

EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY (2014)

Review Oncology

Aryl hydrocarbon receptor ligands in cancer: friend and foe

Iain A. Murray et al.

NATURE REVIEWS CANCER (2014)

Article Pharmacology & Pharmacy

Renal Circadian Clock Regulates the Dosing-Time Dependency of Cisplatin-Induced Nephrotoxicity in Mice

Masayuki Oda et al.

MOLECULAR PHARMACOLOGY (2014)

Article Physiology

Transcriptional regulation of human organic anion transporter 1 by B-cell CLL/lymphoma 6

Waja Wegner et al.

AMERICAN JOURNAL OF PHYSIOLOGY-RENAL PHYSIOLOGY (2014)

Article Gastroenterology & Hepatology

Long-Term Cisplatin Exposure Promotes Methylation of the OCT1 Gene in Human Esophageal Cancer Cells

Rui Lin et al.

DIGESTIVE DISEASES AND SCIENCES (2013)

Review Pharmacology & Pharmacy

Nuclear-receptor-mediated regulation of drug- and bile-acid-transporter proteins in gut and liver

Jeff L. Staudinger et al.

DRUG METABOLISM REVIEWS (2013)

Article Oncology

An in vivo hypoxia metagene identifies the novel hypoxia inducible factor target gene SLCO1B3

Anassuya Ramachandran et al.

EUROPEAN JOURNAL OF CANCER (2013)

Article Pharmacology & Pharmacy

Differential regulation of drug transporter expression by all-trans retinoic acid in hepatoma HepaRG cells and human hepatocytes

Marc Le Vee et al.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2013)

Review Neurosciences

DNA Methylation and Its Basic Function

Lisa D. Moore et al.

NEUROPSYCHOPHARMACOLOGY (2013)

Article Chemistry, Multidisciplinary

Epigenetic Regulation of Organic Anion Transporting Polypeptide 1B3 in Cancer Cell Lines

Satoki Imai et al.

PHARMACEUTICAL RESEARCH (2013)

Article Genetics & Heredity

Genetic and epigenetic regulation of the organic cation transporter 3, SLC22A3

L. Chen et al.

PHARMACOGENOMICS JOURNAL (2013)

Article Pharmacology & Pharmacy

DNA Methylation and Histone Modification Profiles of Mouse Organic Anion Transporting Polypeptides

Satoki Imai et al.

DRUG METABOLISM AND DISPOSITION (2013)

Article Pharmacology & Pharmacy

Atorvastatin Treatment Induces Uptake and Efflux Transporters in Human Liver

Linda Bjorkhem-Bergman et al.

DRUG METABOLISM AND DISPOSITION (2013)

Review Pharmacology & Pharmacy

OATPs, OATs and OCTs: the organic anion and cation transporters of the SLCO and SLC22A gene superfamilies

Megan Roth et al.

BRITISH JOURNAL OF PHARMACOLOGY (2012)

Article Biochemistry & Molecular Biology

Human OCTN2 (SLC22A5) is down-regulated in virus- and nonvirus-mediated cancer

Mariafrancesca Scalise et al.

CELL BIOCHEMISTRY AND FUNCTION (2012)

Review Biochemistry & Molecular Biology

Role of CAR and PXR in xenobiotic sensing and metabolism

Yue-Ming Wang et al.

EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY (2012)

Article Physiology

Liver X receptor activation downregulates organic anion transporter 1 (OAT1) in the renal proximal tubule

Suticha Kittayaruksakul et al.

AMERICAN JOURNAL OF PHYSIOLOGY-RENAL PHYSIOLOGY (2012)

Article Pharmacology & Pharmacy

Regulation of Tissue-Specific Expression of Renal Organic Anion Transporters by Hepatocyte Nuclear Factor 1 α/β and DNA Methylation

Li Jin et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2012)

Article Pharmacology & Pharmacy

Rifampin Enhances the Glucose-Lowering Effect of Metformin and Increases OCT1 mRNA Levels in Healthy Participants

S. K. Cho et al.

CLINICAL PHARMACOLOGY & THERAPEUTICS (2011)

Review Biochemistry & Molecular Biology

Organic Anion Transporting Polypeptides (OATPs): Regulation of Expression and Function

Martin Svoboda et al.

CURRENT DRUG METABOLISM (2011)

Article Pharmacology & Pharmacy

Transporter Pharmacogenetics and Statin Toxicity

M. Niemi

CLINICAL PHARMACOLOGY & THERAPEUTICS (2010)

Article Gastroenterology & Hepatology

Liver X Receptor α and Farnesoid X Receptor Are Major Transcriptional Regulators of OATP1B1

Henriette E. Meyer Zu Schwabedissen et al.

HEPATOLOGY (2010)

Review Biotechnology & Applied Microbiology

Membrane transporters in drug development

Kathleen M. Giacomini et al.

NATURE REVIEWS DRUG DISCOVERY (2010)

Review Physiology

Hijacking Solute Carriers for Proton-Coupled Drug Transport

Catriona M. H. Anderson et al.

PHYSIOLOGY (2010)

Article Chemistry, Multidisciplinary

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

Sayaka Ichihara et al.

PHARMACEUTICAL RESEARCH (2010)

Review Pharmacology & Pharmacy

Xenobiotic, Bile Acid, and Cholesterol Transporters: Function and Regulation

Curtis D. Klaassen et al.

PHARMACOLOGICAL REVIEWS (2010)

Article Biochemistry & Molecular Biology

Organic cation/carnitine transporter OCTN3 is present in astrocytes and is up-regulated by peroxisome proliferators-activator receptor agonist

Elzbieta Januszewicz et al.

INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY (2009)

Article Biochemistry & Molecular Biology

Carnitine synthesis and uptake into cells are stimulated by fasting in pigs as a model of nonproliferating species

Robert Ringseis et al.

JOURNAL OF NUTRITIONAL BIOCHEMISTRY (2009)

Article Urology & Nephrology

SLCO4C1 Transporter Eliminates Uremic Toxins and Attenuates Hypertension and Renal Inflammation

Takafumi Toyohara et al.

JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY (2009)

Review Medicine, Research & Experimental

Hepatic OATP1B Transporters and Nuclear Receptors PXR and CAR: Interplay, Regulation of Drug Disposition Genes, and Single Nucleotide Polymorphisms

Henriette E. Meyer Zu Schwabedissen et al.

MOLECULAR PHARMACEUTICS (2009)

Article Pharmacology & Pharmacy

Analysis of DNA Methylation and Histone Modification Profiles of Liver-Specific Transporters

Satoki Imai et al.

MOLECULAR PHARMACOLOGY (2009)

Article Biotechnology & Applied Microbiology

Identification and characterization of novel polymorphisms in the basal promoter of the human transporter, MATE1

Ji Ha Choi et al.

PHARMACOGENETICS AND GENOMICS (2009)

Article Gastroenterology & Hepatology

Regulatory mechanism governing the diurnal rhythm of intestinal H+/peptide cotransporter 1 (PEPT1)

Hirofumi Saito et al.

AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY (2008)

Article Gastroenterology & Hepatology

Regulation of basal core promoter activity of human organic cation transporter 1 (OCT1/SLC22A1)

Moto Kajiwara et al.

AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY (2008)

Article Pharmacology & Pharmacy

Regulation of Octn2 transporter (SLC22A5) by peroxisome proliferator activated receptor alpha

Tomoji Maeda et al.

BIOLOGICAL & PHARMACEUTICAL BULLETIN (2008)

Article Oncology

Regulation of Prostaglandin Transporters in Colorectal Neoplasia

Vijaykumar R. Holla et al.

CANCER PREVENTION RESEARCH (2008)

Article Physiology

Kidney-specific expression of human organic cation transporter 2 (OCT2/SLC22A2) is regulated by DNA methylation

Masayo Aoki et al.

AMERICAN JOURNAL OF PHYSIOLOGY-RENAL PHYSIOLOGY (2008)

Article Pharmacology & Pharmacy

Transcriptional regulation of human and mouse organic anion transporter 1 by hepatocyte nuclear factor 1 α/β

Takami Saji et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2008)

Article Pharmacology & Pharmacy

PPARα agonists positively and negatively regulate the expression of several nutrient/drug transporters in mouse small intestine

Toshitake Hirai et al.

BIOLOGICAL & PHARMACEUTICAL BULLETIN (2007)

Article Biochemistry & Molecular Biology

PPARα-activation results in enhanced carnitine biosynthesis and OCTN2-mediated hepatic carnitine accumulation

Naomi van Vlies et al.

BIOCHIMICA ET BIOPHYSICA ACTA-BIOENERGETICS (2007)

Article Pharmacology & Pharmacy

Effect of pregnane X receptor ligand on pharmacokinetics of substrates of organic cation transporter Oct1 in rats

Tomoji Maeda et al.

DRUG METABOLISM AND DISPOSITION (2007)

Article Physiology

Clofibrate causes an upregulation of PPAR-α target genes but does not alter expression of SREBP target genes in liver and adipose tissue of pigs

Sebastian Luci et al.

AMERICAN JOURNAL OF PHYSIOLOGY-REGULATORY INTEGRATIVE AND COMPARATIVE PHYSIOLOGY (2007)

Article Physiology

Hepatocyte nuclear factor-4α regulates the human organic anion transporter 1 gene in the kidney

Ken Ogasawara et al.

AMERICAN JOURNAL OF PHYSIOLOGY-RENAL PHYSIOLOGY (2007)

Article Biochemistry & Molecular Biology

Feeding oxidized fat during pregnancy up-regulates expression of PPARα-responsive genes in the liver of rat fetuses

Robert Ringseis et al.

LIPIDS IN HEALTH AND DISEASE (2007)

Article Biochemical Research Methods

Transcriptional regulation at a glance

Silke Sperling

BMC BIOINFORMATICS (2007)

Review Biochemistry & Molecular Biology

Principles of hepatic organic anion transporter regulation during cholestasis, inflammation and liver regeneration

Andreas Geier et al.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH (2007)

Article Biochemistry & Molecular Biology

PPARα agonists up-regulate organic cation transporters in rat liver cells

Sebastian Luci et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2006)

Article Gastroenterology & Hepatology

Induction of intestinal peptide transporter 1 expression during fasting is mediated via peroxisome proliferator-activated receptor α

Jin Shimakura et al.

AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY (2006)

Article Pharmacology & Pharmacy

Transcriptional profiling of genes induced in the livers of patients treated with carbamazepine

Mikael Oscarson et al.

CLINICAL PHARMACOLOGY & THERAPEUTICS (2006)

Article Pharmacology & Pharmacy

The human organic cation transporter-1 gene is transactivated by hepatocyte nuclear factor-4α

M Saborowski et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2006)

Article Endocrinology & Metabolism

The pregnane X receptor regulates gene expression in a ligand- and promoter-selective fashion

H Masuyama et al.

MOLECULAR ENDOCRINOLOGY (2005)

Article Gastroenterology & Hepatology

Characterization of the human peptide transporter PEPT1 promoter: Sp1 functions as a basal transcriptional regulator of human PEPT1

J Shimakura et al.

AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY (2005)

Review Gastroenterology & Hepatology

Enterohepatic bile salt transporters in normal physiology and liver disease

GA Kullak-Ublick et al.

GASTROENTEROLOGY (2004)

Article Gastroenterology & Hepatology

Effect of phenobarbital on the expression of bile salt and organic anion transporters of rat liver

N Hagenbuch et al.

JOURNAL OF HEPATOLOGY (2001)