4 November 2009

Mohamed-Eslam F. Mohamed and Reginald F. Frye

Inhibition of intestinal and hepatic glucuronidation of mycophenolic acid by Ginkgo biloba extract and flavonoids
Published November 4, 2009; doi:10.1124/dmd.109.030080 [Abstract] [PDF]  

Annie Albin Lumen, Poulomi Acharya, Joseph W. Polli, Andy Ayrton, Harma Ellens, and Joe Bentz

If the KI is defined by the free energy of binding to P-gp, what kinetic parameters define the IC50 for the MDCKII-hMDR1 confluent cell monolayer?
Published November 4, 2009; doi:10.1124/dmd.109.029843 [Abstract] [PDF] [Data Supplement]  

Tsuyoshi Minematsu, Jennifer Lee, Jiuhong Zha, Selina Moy, Donna Kowalski, Katsuyuki Hori, Koji Ishibashi, Takashi Usui, and Hidetaka Kamimura

Time-dependent Inhibitory Effects of FK1706, a Novel Non-immunosuppressive Immunophilin Ligand, on CYP3A4/5 Activity in Humans in Vivo and in Vitro
Published November 4, 2009; doi:10.1124/dmd.109.029280 [Abstract] [PDF] [Data Supplement]  

2 November 2009

Christopher Marohnic, Satya P. Panda, Karen McCammon, Jose Rueff, Bettie Sue S. Masters, and Michel Kranendonk

Human Cytochrome P450 Oxidoreductase Deficiency Caused by the Y181D Mutation: Molecular Consequences & Rescue of Defect
Published November 2, 2009; doi:10.1124/dmd.109.030445 [Abstract] [PDF] [Data Supplement]  

Sara K Quinney, Xin Zhang, Aroonrut Lucksiri, J. Christopher Gorski, Lang Li, and Stephen D Hall

Physiologically-Based Pharmacokinetic Model of Mechanism-Based Inhibition of CYP3A by Clarithromycin
Published November 2, 2009; doi:10.1124/dmd.109.028746 [Abstract] [PDF]  

29 October 2009

Takao Watanabe, Hiroyuki Kusuhara, Kazuya Maeda, Hiroshi Kanamaru, Yoshikazu Saito, Zhuohan Hu, and Yuichi Sugiyama

Investigation of the Rate-determining Process in the Hepatic Elimination of HMG-CoA Reductase Inhibitors in Rats and Humans
Published October 29, 2009; doi:10.1124/dmd.109.030254 [Abstract] [PDF]  

Liyue Huang, Loren Berry, Sindhura Ganga, Brett Janosky, April Chen, Jonathan Roberts, Adria E Colletti, and Min-Hwa Jasmine Lin

Relationship between Passive Permeability, Efflux, and Predictability of Clearance from in vitro Metabolic Intrinsic Clearance
Published October 29, 2009; doi:10.1124/dmd.109.029066 [Abstract] [PDF] [Data Supplement]  

Florian Gillotin, Patrice Chiap, Michel Frederich, Jean-Claude Van Heugen, Pierre Francotte, Philippe Lebrun, Bernard Pirotte, and Pascal de Tullio

Coupling of LC-MS/MS and LC-SPE-NMR techniques for the structural identification of metabolites following in vitro biotransformation of SUR1-selective KATP channel openers
Published October 29, 2009; doi:10.1124/dmd.109.028928 [Abstract] [PDF]  

22 October 2009

Kay-Gunnar Stubenrauch, Uwe Wessels, Joerg Thomas Regula, Hubert Kettenberger, Julia Schleypen, and Ulrich Kohnert

Impact of molecular processing in the hinge region of therapeutic IgG4 antibodies on disposition profiles in cynomolgus monkeys
Published October 22, 2009; doi:10.1124/dmd.109.029751 [Abstract] [PDF]  

Yong Liu, Jacqueline Ramirez, Larry House, and Mark J. Ratain

COMPARISON OF THE DRUG-DRUG INTERACTIONS POTENTIAL OF ERLOTINIB AND GEFITINIB VIA INHIBITION OF UDP-GLUCURONOSYLTRANSFERASES
Published October 22, 2009; doi:10.1124/dmd.109.029660 [Abstract] [PDF]  

19 October 2009

Miho Kazui, Yumi Nishiya, Tomoko Ishizuka, Katsunobu Hagihara, Nagy A Farid, Osamu Okazaki, Toshihiko Ikeda, and Atsushi Kurihara

Identification of the human cytochrome P450 enzymes involved in the two oxidative steps in the bioactivation of clopidogrel to its pharmacologically active metabolite
Published October 19, 2009; doi:10.1124/dmd.109.029132 [Abstract] [PDF]  

Ying Wang, Jordan C Bell, Diane S Keeney, and Henry W. Strobel

Gene Regulation of CYP4F11 in Human Keratinocyte HaCaT Cells
Published October 19, 2009; doi:10.1124/dmd.109.029025 [Abstract] [PDF] [Data Supplement]  

Souzan B. Yanni, Pieter P. Annaert, Patrick Augustijns, Joseph G. Ibrahim, Daniel K. Benjamin, and Dhiren R. Thakker

In Vitro Hepatic Metabolism Explains Higher Clearance of Voriconazole in Children versus Adults: Role of CYP2C19 and FMO3
Published October 19, 2009; doi:10.1124/dmd.109.029769 [Abstract] [PDF]  

Koukeb ROUGUIEG, Nicolas PICARD, Francois-Ludovic SAUVAGE, Jean-michel GAULIER, and Pierre MARQUET

Contribution of the different UDP-glucuronosyltransferase (UGT) isoforms to buprenorphine and norbuprenorphine metabolism and relationship with the main UGT polymorphisms in a bank of human liver microsomes.
Published October 19, 2009; doi:10.1124/dmd.109.029546 [Abstract] [PDF]  

15 October 2009

Atsushi Ose, Hiroyuki Kusuhara, Chihiro Endo, Kimio Tohyama, Mari Miyajima, Satoshi Kitamura, and Yuichi Sugiyama

Functional characterization of mouse Oatp1a4 in the uptake and efflux of drugs across the blood–brain barrier
Published October 15, 2009; doi:10.1124/dmd.109.029454 [Abstract] [PDF]  

Xiaoliang Zhuo, Richard A Hartz, Joanne J Bronson, Harvey Wong, Vijay T Ahuja, Vivekananda M Vrudhula, John E Leet, Stella Huang, John E Macor, and Yue-Zhong Shu

COMPARATIVE BIOTRANSFORMATION OF PYRAZINONE-CONTAINING CORTICOTROPIN-RELEASING FACTOR RECEPTOR-1 (CRF-R1) ANTAGONISTS: MINIMIZING THE REACTIVE METABOLITE FORMATION
Published October 15, 2009; doi:10.1124/dmd.109.028910 [Abstract] [PDF]  

Tsuyoshi Minematsu, Megumi Iwai, Ken-ichi Umehara, Takashi Usui, and Hidetaka Kamimura

Characterization of human organic cation transporter 1 (OCT1/SLC22A1)-, and OCT2 (SLC22A2)-mediated transport of YM155 monobromide, a novel survivin suppressant
Published October 15, 2009; doi:10.1124/dmd.109.028142 [Abstract] [PDF]  

Sean Kim, Joseph E Dinchuk, Monique Anthony, Tami Orcutt, Mary E Zoeckler, Mary B Sauer, Kathleen W Mosure, Ragini Vuppugalla, James E Grace, Jean Simmermacher, Heidi Dulac, Jennifer Pizzano, and Michael Sinz

Evaluation of Cynomolgus Monkey PXR, Primary Hepatocyte and In Vivo Pharmacokinetic Changes in Predicting Human CYP3A4 Induction
Published October 15, 2009; doi:10.1124/dmd.109.029637 [Abstract] [PDF] [Data Supplement]  

7 October 2009

Tove Johansson, Lars Weidolf, Friedrich Popp, Reinhold Tacke, and Ulrik Jurva

In vitro metabolism of haloperidol and sila-haloperidol - new metabolic pathways resulting from carbon/silicon exchange
Published October 7, 2009; doi:10.1124/dmd.109.028449 [Abstract] [PDF] [Data Supplement]  

Helen L Andersson, Malin Helmestam, Anna Zebrowska, Matts Olofsson, and Eva Brittebo

Tamoxifen-induced adduct formation and cell stress in human endometrial glands
Published October 7, 2009; doi:10.1124/dmd.109.029488 [Abstract] [PDF]  

Jian Yu, Donald E Mathisen, Doug Burdette, Dean G Brown, Christopher Becker, and David Aharony

Identification of Multiple Glutathione Conjugates of Nomifensine in Liver Microsomes and Hepatocyte Preparations: Evidence of the Bioactivation of Nomifensine
Published October 7, 2009; doi:10.1124/dmd.109.028803 [Abstract] [PDF] [Data Supplement]  

1 October 2009

Thomas J Bateman, John S Debenham, Christina Madsen-Duggan, Richard B Toupence, Thomas F Walsh, Quang Truong, Scott A Bradley, George A Doss, Sanjeev Kumar, and Vijay Bhasker G Reddy

Glutathione S-transferase Catalyzed Desulfonylation of a Sulfonylfuropyridine
Published October 1, 2009; doi:10.1124/dmd.109.029801 [Abstract] [PDF]  

Bryn M Owen, Alexandra Milona, Saskia van Mil, Peter Clements, Julie Holder, Mohamed Boudjelal, William Cairns, Malcolm Parker, Roger White, and Catherine Williamson

Intestinal Detoxification Limits the Activation of Hepatic PXR by Lithocholic Acid.
Published October 1, 2009; doi:10.1124/dmd.109.029306 [Abstract] [PDF] [Data Supplement]  

Loren M Berry, Jonathan Roberts, Xuhai Be, Zhiyang Zhao, and Min-Hwa Jasmine Lin

Prediction of Vss from in vitro tissue binding studies
Published October 1, 2009; doi:10.1124/dmd.109.029629 [Abstract] [PDF]  

Xin Zhang, Raymond E. Galinsky, Robert E. Kimura, Sara K Quinney, David R. Jones, and Stephen D. Hall

Inhibition of CYP3A by Erythromycin: In Vitro-In Vivo Correlation in Rats
Published October 1, 2009; doi:10.1124/dmd.109.028290 [Abstract] [PDF]  

Britta K Bonn, Collen M Masimirembwa, and Neal Castagnoli

Exploration of catalytic properties of CYP2D6 and CYP3A4 through metabolic studies of levorphanol and levallorphan
Published October 1, 2009; doi:10.1124/dmd.109.028670 [Abstract] [PDF] [Data Supplement]  

Abhishek Srivastava, Lu-Yun Lian, James L Maggs, Masautso Chaponda, Munir Pirmohamed, Dominic Paul Williams, and B. Kevin Park

Quantifying the Metabolic Activation of Nevirapine in Patients by Integrated Applications of NMR and Mass Spectrometries
Published October 1, 2009; doi:10.1124/dmd.109.028688 [Abstract] [PDF] [Data Supplement]  

Junko Sugatani, Makoto Osabe, Masatoshi Kurosawa, Naomi Kitamura, Akira Ikari, and Masao Miwa

Induction of UGT1A1 and CYP2B6 by an antimitogenic factor in HepG2 cells is mediated through suppression of cyclin-dependent kinase 2 activity: Cell-cycle dependent expression
Published October 1, 2009; doi:10.1124/dmd.109.029785 [Abstract] [PDF]  

28 September 2009

Mark P. Grillo, Jill C. M. Wait, Michelle Tadano Lohr, Smriti Khera, and Leslie Z. Benet

Stereoselective Flunoxaprofen-S-Acyl-Glutathione Thioester Formation Mediated by Acyl-CoA Formation in Rat Hepatocytes
Published September 28, 2009; doi:10.1124/dmd.109.029371 [Abstract] [PDF] [Data Supplement]  

Hazem E Hassan, Alan Myers, Insong Lee, Hegang Chen, Andrew Coop, and Natalie D. Eddington

Regulation of Gene Expression in Brain Tissues of Rats Chronically Treated by The Highly Abused Opioid Agonist, Oxycodone: Microarray Profiling and Gene Mapping Analysis
Published September 28, 2009; doi:10.1124/dmd.109.029199 [Abstract] [PDF]  

Houfu Liu, Junling Yang, Feifei Du, Xiumei Gao, Xutao Ma, Yuhong Huang, Fang Xu, Wei Niu, Fengqing Wang, Yu Mao, Yan Sun, Tong Lu, Changxiao Liu, Boli Zhang, and Chuan Li

Absorption and disposition of ginsenosides after oral administration of Panax notoginseng extract to rats
Published September 28, 2009; doi:10.1124/dmd.109.029819 [Abstract] [PDF]  

Yoshihisa Kato, Koichi Haraguchi, Makiko Kubota, Yoshiki Seto, Takashi Okura, Shin-ichi Ikushiro, Nobuyuki Koga, Shizuo Yamada, and Masakuni Degawa

A Possible Mechanism for the Decrease in Serum Thyroxine Level by a TCDD-Like PCB Congener, 3,3',4,4',5-Pentachlorobiphenyl in Mice
Published September 28, 2009; doi:10.1124/dmd.109.029348 [Abstract] [PDF]  

Jennifer Q. Dong and Philip C. Smith

Glucuronidation and Covalent Protein Binding of Benoxaprofen and Flunoxaprofen in Sandwich-Cultured Rat and Human Hepatocytes
Published September 28, 2009; doi:10.1124/dmd.109.028944 [Abstract] [PDF]  

22 September 2009

Janne T. Backman, Johanna Honkalammi, Mikko Neuvonen, Kaisa J. Kurkinen, Aleksi Tornio, Mikko Niemi, and Pertti J. Neuvonen

CYP2C8 Activity Recovers Within 96 Hours After Gemfibrozil Dosing: Estimation of CYP2C8 Half-life Using Repaglinide as an In Vivo Probe
Published September 22, 2009; doi:10.1124/dmd.109.029728 [Abstract] [PDF]  

Francois Marceau, Marie-Therese Bawolak, Johanne Bouthillier, and Guillaume Morissette

Vacuolar ATPase-mediated cellular concentration and retention of quinacrine: a model for the distribution of lipophilic cationic drugs to autophagic vacuoles
Published September 22, 2009; doi:10.1124/dmd.109.028480 [Abstract] [PDF]  

Hirohisa Nagahori, Koichi Saito, Yoshitaka Tomigahara, Naohiko Isobe, and Hideo Kaneko

Metabolism of Pyridalyl in Rats
Published September 22, 2009; doi:10.1124/dmd.109.028878 [Abstract] [PDF]  

Lilly Xu, Yuping Chen, Yvonne Pan, Gary L Skiles, and Magang Shou

Prediction of Human Drug and Drug Interactions from Time-Dependent Inactivation of CYP3A4 in Primary Hepatocytes Using a Population-Based Simulator
Published September 22, 2009; doi:10.1124/dmd.108.025494 [Abstract] [PDF]  

Ebba Bergman, Anna Lundahl, Patrik Fridblom, Mikael Hedeland, Ulf Bondesson, Lars Knutson, and Hans Lennernas

The Enterohepatic Disposition of Rosuvastatin in Pigs and The Impact of Concomitant Dosing with Cyclosporine and Gemfibrozil
Published September 22, 2009; doi:10.1124/dmd.109.029363 [Abstract] [PDF]  

Ida Rudberg, J Leon E Reubsaet, Monica Hermann, Helge Refsum, and Espen Molden

Identification of a novel CYP2C19-mediated metabolic pathway of S-citalopram in vitro
Published September 22, 2009; doi:10.1124/dmd.109.029355 [Abstract] [PDF]  

David E Moody, Wenfang B Fang, Shen-Nan Lin, Denise M Weyant, Stephen C Strom, and Curtis J Omiecinski

The effect of rifampin and nelfinavir on the metabolism of methadone and buprenorphine in primary cultures of human hepatocytes
Published September 22, 2009; doi:10.1124/dmd.109.028605 [Abstract] [PDF]  

14 September 2009

Robert A.B. van Waterschoot, Rogier W. Rooswinkel, Rolf W. Sparidans, Antonius E. van Herwaarden, Jos H. Beijnen, and Alfred H. Schinkel

Inhibition and stimulation of intestinal and hepatic CYP3A activity: studies in humanized CYP3A4 transgenic mice using triazolam
Published September 14, 2009; doi:10.1124/dmd.109.029397 [Abstract] [PDF] [Data Supplement]  

9 September 2009

Joshua F Alfaro, Carolyn A Joswig-Jones, Wenyun Ouyang, Joseph Nichols, Gregory J. Crouch, and Jeffrey P. Jones

PURIFICATION AND MECHANISM OF HUMAN ALDEHYDE OXIDASE (AOX1) EXPRESSED IN E. COLI.
Published September 9, 2009; doi:10.1124/dmd.109.029520 [Abstract] [PDF]  

Ruben J. Boado and William M. Pardridge

Comparison of Blood-Brain Barrier Transport of GDNF and an IgG-GDNF Fusion Protein in the Rhesus Monkey
Published September 9, 2009; doi:10.1124/dmd.109.028787 [Abstract] [PDF]  

Gustav Ahlin, Constanze Hilgendorf, Cristina Al-Khalili Szigyarto, Mathias Uhlen, Johan E Karlsson, and Per Artursson

Endogenous gene and protein expression of drug transporting proteins in cell lines routinely used in drug discovery programs.
Published September 9, 2009; doi:10.1124/dmd.109.028654 [Abstract] [PDF] [Data Supplement]  

Tian Lan, Anuradha Rao, Jamie Haywood, Charles B. Davis, Chao Han, Eric Garver, and Paul A. Dawson

Interaction of Macrolide Antibiotics with Intestinally Expressed Human and Rat Organic Anion Transporting Polypeptides
Published September 9, 2009; doi:10.1124/dmd.109.028522 [Abstract] [PDF] [Data Supplement]  

Leen Lootens, Peter Van Eenoo, Philip Meuleman, Geert Leroux-Roels, and Frans T Delbeke

uPA^+/+-SCID mouse with humanized liver as a model for in vivo metabolism of 4-androstene-3,17-dione.
Published September 9, 2009; doi:10.1124/dmd.109.028183 [Abstract] [PDF]  

Li Lai, Haiping Hao, Qiong Wang, Chaonan Zheng, Fang Zhou, Yitong Liu, Yuxin Wang, Guo Yu, An Kang, Ying Peng, Guangji Wang, and Xijing Chen

Effects of Short-term and Long-term Pretreatment of Schisandra Lignans on Regulating Hepatic and Intestinal CYP3A in Rats
Published September 9, 2009; doi:10.1124/dmd.109.027433 [Abstract] [PDF]  

31 August 2009

Toru Usui, Masashi Mise, Takanori Hashizume, Masashi Yabuki, and Setsuko Komuro

Evaluation of the potential for drug-induced liver injury based on in vitro covalent binding to human liver proteins
Published August 31, 2009; doi:10.1124/dmd.109.028860 [Abstract] [PDF] [Data Supplement]  

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