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Drug Transporters

:	Martin F. Fromm, Richard B. Kim
:	Martin F. Fromm, Richard B. Kim
:	Drug Transporters
:	Springer-Verlag
:	9783642145414
:	1
:	CHF 275.70
:

:	Pharmazie
:	English

:	454
:	Wasserzeichen/DRM
:	PC/MAC/eReader/Tablet
:	PDF

It is increasingly recognized that various transporter proteins are expressed throughout the body and determine absorption, tissue distribution, biliary and renal elimination of endogenous compounds and drugs and drug effects. This book will give an overview on the transporter families which are most important for drug therapy. Most chapters will focus on one transporter family highlighting tissue expression, substrates, inhibitors, knock-out mouse models and clinical studies.

	Preface	6
	Reference	7
	Contents	8
	Contributors	10
	Uptake Transporters of the Human OATP Family	12
	1 Introduction	13
	2 The Human OATP Family	14
	2.1 Molecular Characteristics of Human OATP Family Members	14
	2.2 Substrate Spectrum of Human OATP Family Members	19
	2.3 Hepatic OATPs and Drug Drug Interactions	22
	2.4 Functional Consequences of Genetic Variations in Transporter Genes	26
	2.4.1 Pharmacogenomics of OATP1B1	26
	2.4.2 Pharmacogenomics of Other Human OATP Family Members	30
	3 Conclusions	32
	References	33
	In Vitro and In Vivo Evidence of the Importance of Organic Anion Transporters (OATs) in Drug Therapy	40
	1 Organic Anion Transporters Within the SLC22A Gene Family	42
	2 Organic Anion Transporter 1 (OAT1/Oat1	Gene name SLC22A6/Slc22a6)43
	2.1 Cloning, Structure	43
	2.2 Tissue Distribution of mRNA	45
	2.3 Immunolocalization of OAT1/Oat1 Protein	47
	2.4 Species Differences, Age and Gender Dependence of Expression	47
	2.5 Factors Influencing Activity and Abundance of OAT1/Oat1	48
	2.6 Substrates	50
	2.6.1 Endogenous Substrates of OAT1/Oat1	51
	2.6.2 Drugs	53
	2.7 Inhibitors	60
	2.8 Drug/Drug Interactions	61
	2.9 Pharmacogenomics	62
	3 Organic Anion Transporter 2 (OAT2/Oat2, Gene Name SLC22A7/Slc22a7)	63
	3.1 Cloning, Structure	63
	3.2 Tissue Distribution of mRNA	63
	3.3 Immunolocalization of OAT2/Oat2 Protein	64
	3.4 Species Differences, Age and Gender Dependence of Expression	64
	3.5 Factors Influencing Activity and Abundance of OAT2/Oat2	65
	3.6 Substrates	65
	3.6.1 Endogenous Substrates	66
	3.6.2 Drugs	66
	3.7 Inhibitors	69
	3.8 Drug/Drug Interactions	69
	3.9 Pharmacogenomics	69
	4 Organic Anion Transporter 3 (OAT3/Oat3, Gene Name SLC22A8/Slc22a8)	69
	4.1 Cloning, Structure	69
	4.2 Tissue Distribution of mRNA	70
	4.3 Immunolocalization of OAT3/Oat3 Protein	70
	4.4 Species Differences, Age and Gender Dependence of Expression	71
	4.5 Factors Influencing Activity and Abundance of OAT3/Oat3	71
	4.6 Substrates	72
	4.6.1 Endogenous Substrates	73
	4.6.2 Drugs	75
	4.7 Inhibitors	80
	4.8 Drug/Drug Interactions	80
	4.9 Pharmacogenomics	82
	5 Organic Anion Transporter 4 (OAT4, Gene Name SLC22A11)	82
	5.1 Cloning, Structure	82
	5.2 Tissue Distribution of mRNA	83
	5.3 Immunolocalization of OAT4 Protein	83
	5.4 Species Differences, Age and Gender Dependence of Expression	84
	5.5 Factors Influencing Activity and Abundance of OAT4	84
	5.6 Substrates	84
	5.6.1 Endogeneous Substrates	84
	5.6.2 Drugs	85
	5.7 Inhibitors	89
	5.8 Drug/Drug Interactions	89
	5.9 Pharmacogenomics	89
	6 Urate Transporter 1 (URAT1	Urat1/Rst, Gene Name SLC22A12/Slc22a12)89
	6.1 Cloning, Structure	89
	6.2 Tissue Distribution of mRNA	90
	6.3 Immunolocalization of URAT1/Urat1/Rst Protein	90
	6.4 Species Differences, Age and Gender Dependence of Expression	91
	6.5 Factors Influencing Activity and Abundance of URAT1/Urat1/Rst	91
	6.6 Substrates	91
	6.6.1 Endogenous Substrates	92
	6.6.2 Drugs	92
	6.7 Inhibitors	93
	6.8 Drug/Drug Interactions	93
	6.9 Pharmacogenomics	94
	7 Organic Anion Transporter 10 (OAT10/ORCTL3, Gene Name SLC22A13)	94
	7.1 Cloning, Structure	94
	7.2 Tissue Distribution of mRNA	94
	7.3 Immunolocalization of OAT10 Protein, Gender Differences	95
	7.4 Substrates	95
	7.4.1 Endogenous Substrates (Bahn et al. 2008)	95
	7.4.2 Drugs (Bahn et al. 2008)	96
	7.5 Inhibitors, Drug/Drug Interactions, Pharmacogenomics	96
	8 Organic Anion Transporter 5 (Oat5, Gene Name Slc22a19)	96
	8.1 Cloning, Structure	96
	8.2 Tissue Distribution of mRNA, Immunolocalization, Gender Differences	96
	8.3 Substrates	97
	8.3.1 Endogenous Substrates	97
	8.3.2 Drugs (Rat Oat5: Anzai et al. 2005	Mouse Oat5: Youngblood and Sweet 2004)97
	8.4 Inhibitors, Drug/Drug Interactions, Pharmacogenomics	97
	9 Organic Anion Transporter 6 (Oat6, Gene Name Slc22a20)	98
	9.1 Cloning, Structure, Tissue Distribution	98
	9.2 Species Differences, Age and Gender D