Transporters in drug discovery and development detailed concepts and best practice 1st Edition by Yurong Lai 190881828X 9781908818287

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ISBN 10: 190881828X 

ISBN 13: 9781908818287

Author: Yurong Lai

Written by a leading researcher in the field, Transporters in Drug Discovery and Development provides a comprehensive and practical guide to drug transporter families that are the most important for drug discovery and development. It covers: an overview of transporter families and organ distribution; clinical relevant drug-drug interaction; clinical relevant polymorphism; drug transporter related pharmacokinetic, pharmacodynamics and toxicity; in vitro/in vivo probes of drug transport studies; the practical methodologies of industrial transporter screening and translational aspect in drug discovery and developments.

Transporters in drug discovery and development detailed concepts and best practice 1st Table of contents:

1. Membrane Transporters and Diseases Related to Functional Defects

• 1.1 Introduction
• 1.2 Ion Channels
• 1.3 Transporters
• 1.4 References

2. P-Glycoprotein (P-gp/MDR1)/ABCB1

• 2.1 Introduction
• 2.2 Molecular Characteristics and Transport Mechanisms
• 2.3 Tissue Expression of P-gp
• 2.4 Genetic Polymorphism of ABCB1
• 2.5 Substrates and Inhibitors
• 2.6 P-gp Functional Modulation and Clinical Implications
• 2.7 References

3. Multidrug Resistance-Associated Protein 2 (MRP2/ABCC2)

• 3.1 Introduction
• 3.2 Molecular Characteristics and Transport Mechanisms
• 3.3 Organ Expression of MRP2
• 3.4 Genetic Polymorphisms of ABCC2
• 3.5 Substrates and Inhibitors of MRP2/ABCC2
• 3.6 MRP2 Functional Modulation and Clinical Implications
• 3.7 References

4. Breast Cancer Resistance Protein (BCRP)/ABCG2

• 4.1 Introduction
• 4.2 Molecular Characteristics and Transport Mechanisms
• 4.3 Tissue Expression of BCRP
• 4.4 Genetic Polymorphisms of ABCG2
• 4.5 Substrates and Inhibitors
• 4.6 BCRP Functional Modulation and Clinical Implications
• 4.7 References

5. The Bile Salt Export Pump (BSEP/ABCB11)

• 5.1 Introduction
• 5.2 Molecular Characteristics and Transport Mechanisms
• 5.3 BSEP Expression and Drug-Induced Cholestasis
• 5.4 Genetic Polymorphisms of ABCB11
• 5.5 Substrates and Inhibitors of BSEP and Clinical Implications
• 5.6 References

6. Organic Anion-Transporting Polypeptides (OATPs/SLCOs)

• 6.1 Introduction
• 6.2 Molecular Characteristics and Transport Mechanisms
• 6.3 Organ Expression of OATP Transporters
• 6.4 Genetic Polymorphisms of SLCO Genes
• 6.5 OATP Functional Modulation and Clinical Implications
• 6.6 Substrates and Inhibitors of OATP Transporters
• 6.7 References

7. Organic Anion, Organic Cation, and Zwitterion Transporters of the SLC22 and SLC47 Superfamily (OATs, OCTs, OCTNs, and MATEs)

• 7.1 Introduction
• 7.2 Molecular Characteristics and Transport Mechanisms
• 7.3 Tissue Expression of Organic Anion, Organic Cation, and Zwitterion Transporters
• 7.4 Genetic Polymorphisms
• 7.5 Substrates and Inhibitors
• 7.6 Transporter Functional Modulation and Clinical Implications
• 7.7 References

8. Drug Transporters in Drug Discovery and Development

• 8.1 Introduction
• 8.2 Transporter Effects in Organ Barriers
• 8.3 Transporters as Pharmacological Targets
• 8.4 Transporter-Related Organ Toxicity
• 8.5 Enzyme-Transporter Interplay in the Liver
• 8.6 Transporter Assessment in Drug Discovery and Development
• 8.7 References

9. Transporter Study Methodologies

• 9.1 Introduction
• 9.2 Membrane-Based Systems
• 9.3 Cell-Based Transporter Assays
• 9.4 In Situ Perfused Organ and Ex Vivo Incubation Systems
• 9.5 Transporter Characterization in Animal Models
• 9.6 In Silico Computational and Mathematical Models

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