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Drug Transporters


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HEPATIC TRANSPORT PROTEINS AS DETERMINANTS OF DRUG TOXICITY 13.11 THE FUTURE OF HEPATIC DRUG TRANSPORT ACKNOWLEDGMENTS REFERENCES

      21  14 DRUG TRANSPORT IN THE BRAIN 14.1 INTRODUCTION 14.2 PHYSIOLOGY OF THE BRAIN BARRIERS AND BRAIN PARENCHYMA 14.3 FUNCTIONAL EXPRESSION AND LOCALIZATION OF DRUG TRANSPORTERS IN THE BRAIN 14.4 RELEVANCE OF DRUG TRANSPORTERS IN CNS DISORDERS 14.5 CONCLUSION REFERENCES

      22  15 DRUG TRANSPORT IN THE KIDNEY 15.1 KIDNEY STRUCTURE AND FUNCTION 15.2 MAJOR DRUG TRANSPORTERS EXPRESSED IN HUMAN KIDNEY 15.3 TARGETED PROTEOMICS OF HUMAN RENAL TRANSPORTERS 15.4 HUMAN TRANSPORTERS IN RENAL INJURY AND DISEASE 15.5 CONCLUSIONS AND FUTURE PERSPECTIVES REFERENCES

      23  16 DRUG TRANSPORTERS IN THE HUMAN INTESTINE 16.1 INTRODUCTION 16.2 INTESTINAL ABC TRANSPORTERS (EXPRESSION, LOCALIZATION, FUNCTION) 16.3 INTESTINAL SLC TRANSPORTERS (EXPRESSION, LOCALIZATION, FUNCTION) 16.4 INTERPLAY OF APICAL AND BASOLATERAL TRANSPORTERS 16.5 VARIABILITY OF INTESTINAL TRANSPORTERS 16.6 DRUG–DRUG INTERACTIONS INVOLVING INTESTINAL TRANSPORTERS 16.7 LIMITATIONS OF AVAILABLE RESEARCH MODELS FOR THE HUMAN INTESTINE 16.8 CONCLUSIONS AND FUTURE PERSPECTIVES REFERENCES

      24  17 DRUG TRANSPORT IN THE PLACENTA 17.1 INTRODUCTION 17.2 BLOOD–PLACENTAL BARRIER RELEVANT TO DRUG PERMEABILITY AND TRANSPORT 17.3 DRUG TRANSPORTERS IN HUMAN PLACENTA 17.4 METHODS TO STUDY PLACENTAL DRUG TRANSPORT 17.5 CONCLUSIONS AND FUTURE PERSPECTIVES REFERENCES

      25  18 POLYMORPHISMS OF DRUG TRANSPORTERS AND CLINICAL RELEVANCE 18.1 INTRODUCTION 18.2 GENETIC VARIATION IN DRUG TRANSPORTERS LEADING TO ALTERED EFFECT 18.3 DISCUSSION 18.4 PERSPECTIVES REFERENCES

      26  19 ONTOGENY OF DRUG TRANSPORTERS 19.1 INTRODUCTION 19.2 TRANSPORTER ONTOGENY 19.3 CHALLENGES IN ASSESSING TRANSPORTER ONTOGENY 19.4 CONCLUSIONS AND FUTURE PERSPECTIVES REFERENCES

      27  20 EXPERIMENTAL APPROACHES FOR STUDYING DRUG TRANSPORTERS 20.1 INTRODUCTION 20.2 GENETICALLY MODIFIED AND HUMAN‐XENOGRAFT MODEL ANIMALS 20.3 IN VIVO EXPERIMENTS 20.4 ISOLATED TISSUE METHODS 20.5 PRIMARY CELL CULTURES, ESTABLISHED MODEL CELL LINES, AND THEIR COMBINATION 20.6 ANALYSIS OF THE TRANSPORT, INHIBITION, INDUCTION, AND DOWNREGULATION OF TRANSPORTERS 20.7 MEMBRANE VESICLES 20.8 PERSPECTIVES REFERENCES

      28  21 TRANSPORTERS‐MEDIATED DRUG DISPOSITION—PHYSIOCHEMISTRY AND IN SILICO APPROACHES 21.1 INTRODUCTION 21.2 PHYSICOCHEMICAL DETERMINANTS OF HEPATOBILIARY TRANSPORT 21.3 IN SILICO MODELS FOR BILIARY ELIMINATION 21.4 PHYSICOCHEMICAL DETERMINANTS OF RENAL ELIMINATION 21.5 IN SILICO MODELS FOR RENAL ELIMINATION OR RENAL CLEARANCE 21.6 FRAMEWORK TO PREDICT TRANSPORTER‐MEDIATED CLEARANCE MECHANISM—EXTENDED CLEARANCE CLASSIFICATION SYSTEM (ECCS) 21.7 IN SILICO APPROACHES AND SAR OF CLINICALLY RELEVANT TRANSPORTERS 21.8 STRATEGIES TO ASSESS TRANSPORTER INVOLVEMENT DURING DRUG DISCOVERY 21.9 TARGETING DRUG TRANSPORTERS: CASE EXAMPLES 21.10 CONCLUSIONS