1;Preface;6 1.1;Reference;7 2;Contents;8 3;Contributors;10 4;Uptake Transporters of the Human OATP Family;12 4.1;1 Introduction;13 4.2;2 The Human OATP Family;14 4.2.1;2.1 Molecular Characteristics of Human OATP Family Members;14 4.2.2;2.2 Substrate Spectrum of Human OATP Family Members;19 4.2.3;2.3 Hepatic OATPs and Drug-Drug Interactions;22 4.2.4;2.4 Functional Consequences of Genetic Variations in Transporter Genes;26 4.2.4.1;2.4.1 Pharmacogenomics of OATP1B1;26 4.2.4.2;2.4.2 Pharmacogenomics of Other Human OATP Family Members;30 4.3;3 Conclusions;32 4.4;References;33 5;In Vitro and In Vivo Evidence of the Importance of Organic Anion Transporters (OATs) in Drug Therapy;40 5.1;1 Organic Anion Transporters Within the SLC22A Gene Family;42 5.2;2 Organic Anion Transporter 1 (OAT1/Oat1; Gene name SLC22A6/Slc22a6)43 5.2.1;2.1 Cloning, Structure;43 5.2.2;2.2 Tissue Distribution of mRNA;45 5.2.3;2.3 Immunolocalization of OAT1/Oat1 Protein;47 5.2.4;2.4 Species Differences, Age and Gender Dependence of Expression;47 5.2.5;2.5 Factors Influencing Activity and Abundance of OAT1/Oat1;48 5.2.6;2.6 Substrates;50 5.2.6.1;2.6.1 Endogenous Substrates of OAT1/Oat1;51 5.2.6.2;2.6.2 Drugs;53 5.2.7;2.7 Inhibitors;60 5.2.8;2.8 Drug/Drug Interactions;61 5.2.9;2.9 Pharmacogenomics;62 5.3;3 Organic Anion Transporter 2 (OAT2/Oat2, Gene Name SLC22A7/Slc22a7);63 5.3.1;3.1 Cloning, Structure;63 5.3.2;3.2 Tissue Distribution of mRNA;63 5.3.3;3.3 Immunolocalization of OAT2/Oat2 Protein;64 5.3.4;3.4 Species Differences, Age and Gender Dependence of Expression;64 5.3.5;3.5 Factors Influencing Activity and Abundance of OAT2/Oat2;65 5.3.6;3.6 Substrates;65 5.3.6.1;3.6.1 Endogenous Substrates;66 5.3.6.2;3.6.2 Drugs;66 5.3.7;3.7 Inhibitors;69 5.3.8;3.8 Drug/Drug Interactions;69 5.3.9;3.9 Pharmacogenomics;69 5.4;4 Organic Anion Transporter 3 (OAT3/Oat3, Gene Name SLC22A8/Slc22a8);69 5.4.1;4.1 Cloning, Structure;69 5.4.2;4.2 Tissue Distribution of mRNA;70 5.4.3;4.3 Immunolocalization of OAT3/Oat3 Protein;70 5.4.4;4.4 Species Differences, Age and Gender Dependence of Expression;71 5.4.5;4.5 Factors Influencing Activity and Abundance of OAT3/Oat3;71 5.4.6;4.6 Substrates;72 5.4.6.1;4.6.1 Endogenous Substrates;73 5.4.6.2;4.6.2 Drugs;75 5.4.7;4.7 Inhibitors;80 5.4.8;4.8 Drug/Drug Interactions;80 5.4.9;4.9 Pharmacogenomics;82 5.5;5 Organic Anion Transporter 4 (OAT4, Gene Name SLC22A11);82 5.5.1;5.1 Cloning, Structure;82 5.5.2;5.2 Tissue Distribution of mRNA;83 5.5.3;5.3 Immunolocalization of OAT4 Protein;83 5.5.4;5.4 Species Differences, Age and Gender Dependence of Expression;84 5.5.5;5.5 Factors Influencing Activity and Abundance of OAT4;84 5.5.6;5.6 Substrates;84 5.5.6.1;5.6.1 Endogeneous Substrates;84 5.5.6.2;5.6.2 Drugs;85 5.5.7;5.7 Inhibitors;89 5.5.8;5.8 Drug/Drug Interactions;89 5.5.9;5.9 Pharmacogenomics;89 5.6;6 Urate Transporter 1 (URAT1; Urat1/Rst, Gene Name SLC22A12/Slc22a12)89 5.6.1;6.1 Cloning, Structure;89 5.6.2;6.2 Tissue Distribution of mRNA;90 5.6.3;6.3 Immunolocalization of URAT1/Urat1/Rst Protein;90 5.6.4;6.4 Species Differences, Age and Gender Dependence of Expression;91 5.6.5;6.5 Factors Influencing Activity and Abundance of URAT1/Urat1/Rst;91 5.6.6;6.6 Substrates;91 5.6.6.1;6.6.1 Endogenous Substrates;92 5.6.6.2;6.6.2 Drugs;92 5.6.7;6.7 Inhibitors;93 5.6.8;6.8 Drug/Drug Interactions;93 5.6.9;6.9 Pharmacogenomics;94 5.7;7 Organic Anion Transporter 10 (OAT10/ORCTL3, Gene Name SLC22A13);94 5.7.1;7.1 Cloning, Structure;94 5.7.2;7.2 Tissue Distribution of mRNA;94 5.7.3;7.3 Immunolocalization of OAT10 Protein, Gender Differences;95 5.7.4;7.4 Substrates;95 5.7.4.1;7.4.1 Endogenous Substrates (Bahn et al. 2008);95 5.7.4.2;7.4.2 Drugs (Bahn et al. 2008);96 5.7.5;7.5 Inhibitors, Drug/Drug Interactions, Pharmacogenomics;96 5.8;8 Organic Anion Transporter 5 (Oat5, Gene Name Slc22a19);96 5.8.1;8.1 Cloning, Structure;96 5.8.2;8.2 Tissue Distribution of mRNA, Immunolocalization, Gender Differences;96 5.8.3;8.3 Substrates;97 5.8.3.1;8.3.1 Endogenous Substrates;