of impact of selected polymorphisms in genes encoding dr...
16 Chapter 19TABLE 19.1 Tissue‐specific maturation patterns for ABC transporters TABLE 19.2 Tissue‐specific maturation patterns for SLC transporters
17 Chapter 20TABLE 20.1 Experimental techniques used to study drug transporters
18 Chapter 22TABLE 22.1 Comparison of SHH and PHH for evaluation of hepatic uptake/efflu...TABLE 22.2 Reported inhibitors for which preincubation with cells potentiat...
19 Chapter 23TABLE 23.1 Common problems in deriving key parameters in Transporter IVIVE‐...TABLE 23.2 Archetypal transporter‐IVIVE scalars, with their incorporation in...
20 Chapter 24TABLE 24.1 SLC transporters as targets in disease TABLE 24.2 ABC transporters as targets in disease
21 Chapter 25TABLE 25.1 Effects of dietary supplements on drug transporters TABLE 25.2 Chemical structures of subclasses of flavonoids TABLE 25.3 Interactions of flavonoids with P‐gp TABLE 25.4 Interactions of flavonoids with MRPs TABLE 25.5 Interactions of flavonoids with BCRP TABLE 25.6 Interactions of flavonoids with OATPs TABLE 25.7 Interactions of isothiocyanates with transporters
List of Illustrations
1 Chapter 2FIGURE 2.1 Tissue distribution and membrane localization of organic cation a...FIGURE 2.2 (a) Alternating‐access transport model for translocation of subst...FIGURE 2.3 Predicted secondary structure of OCT1 with most common (GAF > 0.0...
2 Chapter 3FIGURE 3.1 Mate transporters across species and localization. (a) Phylogenic...FIGURE 3.2 Examples of MATE inhibitors. Structures of chemical inhibitors we...FIGURE 3.3 Predicted structure of the human MATE1 transporter. The membrane ...
3 Chapter 4FIGURE 4.1 Schematic illustrating the transmembrane topology of organic anio...FIGURE 4.2 Post‐translational modifications of OATs. Ubiquitination an...FIGURE 4.3 ABC and SLC transporters contribute to remote sensing and signali...
4 Chapter 6FIGURE 6.1 This schematic illustrates the potential parallel/competing pathw...FIGURE 6.2 The effective permeability of the physiological barrier is a func...FIGURE 6.3 This schematic demonstrates the potential pathways of saquinavir ...
5 Chapter 7FIGURE 7.1 (a) The proposed secondary structure model of SMCTs. The 13 putat...FIGURE 7.2 The phylogenetic tree of human MCT family members. The bar indica...FIGURE 7.3 Lactate shuttling pathway in glycolytic and oxidative cancer cell...
6 Chapter 8FIGURE 8.1 Core chemical structures of a purine nucleoside (a) and a pyrimid...FIGURE 8.2 Substrate selectivity and localization of hCNTs and hENTs in pola...FIGURE 8.3 Membrane topology and secondary structure of hCNT3 (a) and hENT1 ...
7 Chapter 9FIGURE 9.1 Bile acid synthesis. Primary bile acids, cholic acid (CA), and ch...FIGURE 9.2 The enterohepatic circulation (EHC) of bile acids. Bile acids are...
8 Chapter 10FIGURE 10.1 Atomic structures of human P‐gp solved with ligand bound in the ...FIGURE 10.2 Proposed transport cycle of P‐gp. The ligand (in this case pacli...FIGURE 10.3 Chemical structures of selected repurposed drugs used as modulat...
9 Chapter 11FIGURE 11.1 (a) Topology of the “long” human ABBC/MRP subfamily members ABCC...FIGURE 11.2 Expression of ABCC/MRP transporters in 32 human cancers from the...
10 Chapter 12FIGURE 12.1 Structural characterization of ABCG2. (a) ATP‐hydrolysis‐depende...FIGURE 12.2 Expression of ABCG2 and ABCB1 in tumor samples. Data retrieved f...
11 Chapter 13FIGURE 13.1 In vivo architecture of the liver (a)and localization of sel...
12 Chapter 14FIGURE 14.1 Localization of selective ABC and SLC transporters at the blood–...FIGURE 14.2 Localization of selective ABC and SLC transporters in neurons, m...
13 Chapter 15FIGURE 15.1 Schematic representation of the basic functional unit of the kid...
14 Chapter 16FIGURE 16.1 Schematic overview of clinically relevant ATP‐binding cassette (...FIGURE 16.2 Mean relative protein abundance of clinically relevant intestina...FIGURE 16.3 Different possible scenarios of intestinal drug–drug interaction...
15 Chapter 17FIGURE 17.1 A schematic illustration of cellular localization of major drug ...
16 Chapter 20FIGURE 20.1 Schematic diagram for transcellular transport study in polarized...
17 Chapter 21FIGURE 21.1 Relationship between rat biliary excretion (%) and physicochemic...FIGURE 21.2 Principal component analysis of compounds with rat biliary excre...FIGURE 21.3 Physicochemical trends of human renal clearance. Relationship be...FIGURE 21.4 (a) Extended clearance classification system (ECCS) and the majo...FIGURE 21.5 View of the distance of partial residues of P‐gp‐MDR1 the interf...FIGURE 21.6 Schematic depiction of ECCS‐informed approach for ADCE and pharm...FIGURE 21.7 Structures and pharmacological activity of systemic and hepatose...FIGURE 21.8 Structures of third‐generation P‐gp inhibitor tariquidar and the...
18 Chapter 22FIGURE 22.1 Schematic diagram of the methods for estimating the contribution...FIGURE 22.2 Contribution of each transporter isoform to the overall uptake o...FIGURE 22.3 Comparison of pharmacokinetic parameters for several compounds o...FIGURE 22.4 Comparison between the uptake clearance (f B PS u,inf ) at 0% HS...FIGURE 22.5 Relationship between the observed and predicted renal uptake cle...FIGURE 22.6 Substrate dependence of IC 50 values of OATP1B1 inhibitors (cycl...FIGURE 22.7 Structures of physiologically based pharmacokinetic models of ri...
19 Chapter 23FIGURE 23.1 Schematic depicting the central role of IVIVE (in vitro—in vivo...FIGURE 23.2 The schematic provides examples of key permeability‐limited orga...FIGURE 23.3 Part (a) is a schematic of the PBPK/PD model accounting for the ...
20 Chapter 25FIGURE 25.1 Structure of common isothiocyanates.
Guide
7 PREFACE