Preface

Studies of membrane transporters have had a great impact on our understanding of human diseases and the design of effective drugs. About 30 of current clinically marketed drugs are targeting membrane transporters or channels. This book provides various practical methodologies of the ongoing research on membrane transporters, especially applications of transporter technologies in drug discovery and development. To provide readers the most up-to-date information, new and useful fields and...

Info

Dipeptides, tripeptides, -lactam antibiotics, (19,42,121) ACE inhibitors, bestatin, valacyclovir Dipeptides, tripeptides, -lactam antibiotics, (199-202) ACE inhibitors, bestatin, valacyclovir Bile salts, hormones, statins, cardiac glycosides, (203-207) methotrexate, rifampicin -lactam antibiotics, probenecid, loop and (208-212) thiazide diuretics, ACE inhibitors, NSAIDs, and methotrexate, cyclic nucleotides, prostaglandins, folate, neurotransmitter-metabolites, and hormone-conjugates Metformin,...

Multidrug Resistance Phylogenetic Characterization of Superfamilies of Secondary Carriers that Include Drug Exporters

Chen, Jose L. Marquez, Eric I. Sun, and Milton H. Saier We here describe the application of novel programs that allow definition of phylogenetic relationships in transport protein superfamilies. These programs are used to provide information about the four major superfamilies of secondary carriers that include members that export hydrophobic and amphipathic compounds including drugs. These novel programs must be used when sequence divergence among super-family members...

The Resistance Nodulation

All RND superfamily proteins (17) were analyzed using the SFT1 program (Fig. 3.3a) and the SFT2 program (Fig. 3.3b). The SFT1 tree reveals that the members of the two eukaryotic families (EST and Dispatched) cluster together. The many members of the eukaryotic sterol transporter (EST) family group together, while the Dispatched protein branches from a point near the center of the tree (center right). Closest to this branch is one bearing the HAE2 lipid exporters of Gram-positive bacteria, the...

Tap1

Isoleucine-333 valine asp-637 glycine central part ofpharmacogenomics. Pharmacogenomics represents studies on the essential gene-drug interactions through genetic mechanisms and the functional pharmacological context, in cooperation with clinical studies. When drugs enter the human body, their fate is affected by uptake, binding, distribution, biotransformation, and excretion. On a molecular basis, the efficacy of a drug is influenced by the alterations in receptor affinity, transporters, or...

Slc01b3

Ingenuity pathways analysis version 7.1 was used to create a network of direct interacting transporter genes around the nuclear receptor PXR NR1I2 in human. Other smaller scale experimental studies have shown that the bile salt export pump in human hepatocytes is regulated by FXR and not LXR, as it was inducible by 22 R -hydroxycholesterol and appeared to have different ligand binding determinants in the receptor than chenodeoxycholic acid 191 . FXR has also been suggested to regulate...