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Whole Issue (PDF) DrugDrug DiscoveriesDiscoveries && TherapeuticsTherapeutics ISSN 1881-7831 Online ISSN 1881-784X Volume 2, Number 6, December 2008 www.ddtjournal.com Astrocyte Microglia Tight junction Brain PgP MRP1 MRP2 BCRP Mrp4 Mrp5 Blood Shandong University China-Japan Cooperation Center for Drug Discovery & Screen International Advancement Center for Medicine & Health Research Drug Discoveries & Therapeutics Editor-in-Chief: Kazuhisa SEKIMIZU (The University of Tokyo, Tokyo, Japan) Associate Editor: Norihiro KOKUDO (The University of Tokyo, Tokyo, Japan) Drug Discoveries & Therapeutics is a peer-reviewed international journal published bimonthly by Shandong University China-Japan Cooperation Center for Drug Discovery & Screen (SDU-DDSC) and International Advancement Center for Medicine & Health Research Co., Ltd. (IACMHR Co., Ltd.). Drug Discoveries & Therapeutics mainly publishes articles related to basic and clinical pharmaceutical research such as pharmaceutical and therapeutical chemistry, pharmacology, pharmacy, pharmacokinetics, industrial pharmacy, pharmaceutical manufacturing, pharmaceutical technology, drug delivery, toxicology, and traditional herb medicine. Studies on drug-related fields such as biology, biochemistry, physiology, microbiology, and immunology are also within the scope of this journal. Subject Coverage: Basic and clinical pharmaceutical research including Pharmaceutical and therapeutical chemistry, Pharmacology, Pharmacy, Pharmacokinetics, Industrial pharmacy, Pharmaceutical manufacturing, Pharmaceutical technology, Drug delivery, Toxicology, and Traditional herb medicine. Language: English Issues/Year: 6 Published by: IACMHR and SDU-DDSC ISSN: 1881-7831 (Online ISSN 1881-784X) Editorial and Head Office Wei TANG, MD PhD Secretary-in-General TSUIN-IKIZAKA 410 2-17-5 Hongo, Bunkyo-ku Tokyo 113-0033, Japan Tel: 03-5840-9697 Fax: 03-5840-9698 E-mail: office@ddtjournal.com IACMHR CO., LTD. URL: www.ddtjournal.com www.ddtjournal.com i Drug Discoveries & Therapeutics Editorial Board Editor-in-Chief: Kazuhisa SEKIMIZU (The University of Tokyo, Tokyo, Japan) Associate Editor: Norihiro KOKUDO (The University of Tokyo, Tokyo, Japan) Secretary-in-General: Wei TANG (The University of Tokyo, Tokyo, Japan) Offi ce Manager: Munehiro NAKATA (Tokai University, Kanagawa, Japan) Web Editor: Yu CHEN (The University of Tokyo, Tokyo, Japan) English Editor: Curtis BENTLEY (Roswell, GA, USA) China Offi ce: Wenfang XU (Shandong University, Shandong, China) Editors: Yoshihiro ARAKAWA (Tokyo, Japan) Hongxiang LOU (Jinan, China) Santad CHANPRAPAPH (Bangkok, Thailand) Ken-ichi MAFUNE (Tokyo, Japan) Fen Er CHEN (Shanghai, China) Norio MATSUKI (Tokyo, Japan) Zilin CHEN (Wuhan, China) Tohru MIZUSHIMA (Kumamoto, Japan) Guanhua DU (Beijing, China) Abdulla M. MOLOKHIA (Alexandria, Egypt) Chandradhar DWIVEDI (Brookings, SD, USA) Masahiro MURAKAMI (Osaka, Japan) Mohamed F. EL-MILIGI (Cairo, Egypt) Yoshinobu NAKANISHI (Ishikawa, Japan) Harald HAMACHER (Tuebingen, Germany) Yutaka ORIHARA (Tokyo, Japan) Hiroshi HAMAMOTO (Tokyo, Japan) Xiao-Ming OU (Jackson, MS, USA) Xiao-Jiang HAO (Kunming, China) Wei-San PAN (Shenyang, China) Langchong HE (Xi'an, China) Shafi qur RAHMAN (Brookings, SD, USA) David A. HORNE (Duarte, CA, USA) Adel SAKR (Cincinnati, OH, USA) Yongzhou HU (Hangzhou, China) Abdel Aziz M. SALEH (Cairo, Egypt) Wei HUANG (Shanghai, China) Tomofumi SANTA (Tokyo, Japan) Yu HUANG (Hong Kong, China) Yasufumi SAWADA (Tokyo, Japan) Hans E. JUNGINGER (Phitsanulok, Thailand) Brahma N. SINGH (Commack, NY, USA) Toshiaki KATADA (Tokyo, Japan) Hongbin SUN (Nanjing, China) Ibrahim S. KHATTAB (Safat, Kuwait) Benny K. H. TAN (Singapore, Singapore) Hiromichi KIMURA (Tokyo, Japan) Ren-Xiang TAN (Nanjing, China) Shiroh KISHIOKA (Wakayama, Japan) Murat TURKOGLU (Istanbul, Turkey) Kam Ming KO (Hong Kong, China) Stephen G. WARD (Bath, UK) Nobuyuki KOBAYASHI (Nagasaki, Japan) Takako YOKOZAWA (Toyama, Japan) Toshiro KONISHI (Tokyo, Japan) Liangren ZHANG (Beijing, China) Masahiro KUROYANAGI (Hiroshima, Japan) Jian-Ping ZUO (Shanghai, China) Chun Guang LI (Victoria, Australia) Hongmin LIU (Zhengzhou, China) (as of December 20, 2008) Ji-Kai LIU (Kunming, China) ii www.ddtjournal.com CONTENTS Volume 2, Number 6, 2008 Reviews 305 - 332 Role of multidrug resistance associated proteins in drug development. Shu-Feng Zhou 333 - 338 Pharmacogenomics-based clinical studies using a novel, fully automated genotyping system. Setsuo Hasegawa, Sayaka Kimura, Ai Kobayashi, Naoko Imanishi Brief Report 339 - 343 Apoptosis-inducing effect of cinobutacini, Bufo bufo gargarizans Cantor skin extract, on human hepatoma cell line BEL-7402. Fanghua Qi, Anyuan Li, Hong Lv, Lin Zhao, Jijun Li, Bo Gao, Wei Tang Original Articles 344 - 352 Part 2. Long term in vivo/in vitro evaluation of the Cholecystokinin antagonists: N-(5-methyl-3-oxo-1,2-diphenyl-2,3-dihydro-1H-pyrazol-4- yl)-N'-phenylurea MPP and carboxamide MPM. Eric Lattmann, Yodchai Boonprakob, Jintana Sattayasai 353 - 356 Pioglitazone attenuates tactile allodynia and microglial activation in mice with peripheral nerve injury. Shigeki Iwai, Takehiko Maeda, Norikazu Kiguchi, Yuka Kobayashi, Yohji Fukazawa, Masanobu Ozaki, Shiroh Kishioka 357 - 367 Phenolphthalein treatment in pregnant women and congenital abnormalities in their offspring: A population-based case-control study. Ferenc Bánhidy, Nándor Ács, Erzsébet H. Puhó, Andrew E. Czeizel www.ddtjournal.com iii CONTENTS (Continued) Index 368 - 371 Author Index 372 - 378 Subject Index Guide for Authors Copyright iv www.ddtjournal.com Drug Discov Ther 2008; 2(6):305-332. 305 Review Role of multidrug resistance associated proteins in drug development Shu-Feng Zhou* School of Health Sciences, RMIT University, Bundoora, Victoria, Australia. ABSTRACT: The multidrug resistance associated include the active extrusion of xenobiotics by commonly proteins (MRP1, MRP2, MRP3, MRP4, MRP5, shared transport proteins, mainly located in kidney, MRP6, MRP7, MRP8 and MRP9) belongs to the liver and intestine. The ATP-binding cassette (ABC) ATP-binding cassette superfamily (ABCC family) superfamily of transporters consist of a large number of transporters expressed differentially in the liver, of functionally diverse transmembrane proteins which kidney, intestine and blood-brain barrier. MRPs have been subdivided into seven families designated A transport a structurally diverse array of endo- and through G (1-4). Members of this transport superfamily xenobiotics and their metabolites (in particular display high amino acid similarity of the 200 amino acids conjugates) and are subject to induction and surrounding the ATP-binding folds. Approximately 1,100 inhibition by a variety of compounds. An increased ABC transporters are known at this time. Traffic ATPases efflux of natural product anticancer drugs and and P-glycoproteins (PgPs) are other names used for this other anticancer agents by MRPs in cancer cells is family. The family includes bacterial transporters, the associated with tumor resistance. These transporting cystic fibrosis transmembrane conductance regulator, the proteins play a role in the absorption, distribution and Plasmodium falciparum drug-resistance gene, and genes elimination of various compounds in the body. There apparently involved in peptide transport during antigen are increased reports on the clinical impact of genetic presentation. mutations of genes encoding MRP1-9. Therefore, In humans, members of this family serve a variety MRPs have an important role in drug development, of physiological roles in transmembrane transport and and a better understanding of their function and cell signalling, many of which are associated with regulating mechanism can help minimize and avoid disease phenotypes such as multidrug resistance, cystic drug toxicity, unfavourable drug-drug interactions, fibrosis, Tangier disease, adrenoleukodystrophy and and to overcome drug resistance. Zellwegers' syndrome (1,2,4). The available outline of the human genome contains 48 ABC genes (5); 16 of Keywords: MRP, Drug development, Single nucleotide these have a known function and 14 are associated with a polymorphism, Toxicity, Pharmacokinetics, Blood-brain defined human disease (6). ABC transporters that pump barrier, Biliary excretion, Intestinal absorption, Drug cytotoxic drugs from the cell are also present in micro- transport organisms, and this is one of the main mechanisms by which pathogenic species can resist antibiotic treatment. The human family of ABC transporters includes at least 48 members with 7 subfamilies (4). They facilitate 1. Introduction unidirectional translocation of chemically diverse substrates including amino acids, lipids, inorganic The human body is continuously exposed to a great ions, peptides, saccharides, metals, drugs, and proteins. variety of xenobiotics via food, drugs, occupation and Energy derived from the hydrolysis of ATP is used to environment. Evolution has equipped the body with a transport the substrate across the membrane against a plethora of protecting systems to defend itself against the concentration gradient (7). These transporters are present potentially harmful effects of these compounds. One of in almost all tissues and cell types in different amounts. A the important and clinically relevant defense mechanisms typical ABC transporter is characterized by the presence of three peptide motifs: Walker A and B sequences and *Correspondence to: Dr. Shu-Feng Zhou, School of the so-called ABC-signature sequence ("ALSGGQ") Health Sciences, RMIT University, Bundoora,
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