Article
Pharmacology & Pharmacy
Eva Bakos, Orsolya Nemet, Nora Kucsma, Natalia Tokesi, Bruno Stieger, Elisabeth Rushing, Anna-Maria Tokes, Peter Kele, Gabor E. Tusnady, Csilla Ozvegy-Laczka
Summary: In this study, the cloning and functional characterization of a third isoform of OATP3A1, OATP3A1_V3, was described. OATP3A1_V3 showed widespread expression in human organs, with the highest expression in the brain and testis. Immunostaining and functional assays confirmed the expression of OATP3A1_V3 in the human choroid plexus, neurons, and both germ and Sertoli cells of the testis, and identified dehydroepiandrosterone sulfate as a novel OATP3A1 substrate.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Medicine, Research & Experimental
Christine C. Orozco, Mikko Neuvonen, Yi-An Bi, Matthew A. Cerny, Sumathy Mathialagan, Laurie Tylaska, Brian Rago, Chester Costales, Amanda King-Ahmad, Mikko Niemi, A. David Rodrigues
Summary: This study found that sulfated bile acids (BA-S) can potentially serve as clinical biomarkers for OATP1B1/3. The BA-S substrates were observed in OATP1B1, OATP1B3, and NTCP transfected into human embryonic kidney 293 cells, with minimal uptake in other solute carriers (SLCs). Inhibition of BA-S uptake in human hepatocytes was greater with rifampicin (OATP1B1/3 selective inhibitor) than other inhibitors.
MOLECULAR PHARMACEUTICS
(2023)
Article
Chemistry, Medicinal
Katherine D. Lynch, Michelle L. Montonye, Dan-Dan Tian, Tarana Arman, Victoria O. Oyanna, Baron J. Bechtold, Tyler N. Graf, Nicholas H. Oberlies, Mary F. Paine, John D. Clarke
Summary: Silymarin, derived from milk thistle seeds, contains flavonolignans that are substrates for OATPs/Oatps. Research shows that OATPs/Oatps play a role in flavonolignan cellular uptake, and mediate interactions between silymarin and diseases like NASH on drug exposure.
PHYTOTHERAPY RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Yi-Hsueh Lee, Menq-Rong Wu, Jong-Kai Hsiao
Summary: This study confirmed the uptake capability of OATP1B1 for both MR agents and NIR fluorescent dyes, while demonstrating that OATP1B3 exhibits superior ICG uptake capability.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Mikko Neuvonen, Aleksi Tornio, Paivi Hirvensalo, Janne T. Backman, Mikko Niemi
Summary: The study found that plasma CPI performs better than CPIII in detecting altered OATP1B1 function, but GCDCA-3G is an even more sensitive OATP1B1 biomarker than CPI.
CLINICAL PHARMACOLOGY & THERAPEUTICS
(2021)
Article
Agriculture, Multidisciplinary
Kengo Sakurai, Jun Abe, Kota Hirasawa, Hayato Takeuchi, Sachiko Kitamoto
Summary: A study examined the metabolic fate of a newly developed herbicide epyrifenacil in rats, finding that it was rapidly metabolized to M1 and mainly excreted through bile. The parent compound was not detected in plasma, tissues, or urine. M1 was predominantly found in the liver, with a significant sex-related difference observed in urinary excretion. The study suggests that organic anion-transporting polypeptide (OATP) may play a role in the active transport of M1 in the liver and kidney.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Jieru Chen, Yuanping Xue, Xiaoyu Shuai, Chunxu Ni, Zihui Fang, Ling Ye, Mei Hong
Summary: This study investigated the inhibitory effects of major components of Triptergium wilfordii Hook. f. (TWHF) on the function of organic anion transporting polypeptide 1B1 (OATP1B1), which plays a crucial role in drug pharmacokinetics. The results showed that the tested TWHF components, especially the alkaloids Wilforine and Wilforgine, significantly inhibited OATP1B1 activity. The co-incubation and pre-incubation of these components had different effects on the function of OATP1B1.
TOXICOLOGY AND APPLIED PHARMACOLOGY
(2022)
Article
Multidisciplinary Sciences
Lewis Hun, Naoki Okamoto, Eisuke Imura, Roilea Maxson, Riyan Bittar, Naoki Yamanaka
Summary: The primary insect steroid hormone ecdysone requires a membrane transporter to enter its target cells. Although an organic anion-transporting polypeptide (OATP) named Ecdysone Importer (EcI) serves this role in the fruit fly Drosophila melanogaster and most likely in other arthropod species, this highly conserved transporter is apparently missing in mosquitoes. Here we report three additional OATPs that facilitate cellular incorporation of ecdysone in Drosophila and the yellow fever mosquito Aedes aegypti. These additional ecdysone importers (EcI-2, -3, and -4) are dispensable for development and reproduction in Drosophila, consistent with the predominant role of Ed. In contrast, in Aedes, EcI-2 is indispensable for ecdysone-mediated development, whereas EcI-4 is critical for vitellogenesis induced by ecdysone in adult females. Altogether, our results indicate unique and essential functions of these additional ecdysone importers in mosquito development and reproduction, making them attractive molecular targets for species- and stage-specific control of ecdysone signaling in mosquitoes.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Chemistry, Medicinal
Youmna Ali, Tahiatul Shams, Zhengqi Cheng, Yue Li, Chelsea Siu-Wai Chun, Wenying Shu, Xiaofeng Bao, Ling Zhu, Michael Murray, Fanfan Zhou
Summary: This study evaluated the regulatory actions of Wnt inhibitors on human renal Organic anion transporters and Organic anion transporting polypeptides, showing that these inhibitors significantly decrease the activities and membrane expression of multiple transporters. The findings suggest that Wnt inhibitors may have unexpected effects on drug entry into cells.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Chemistry, Medicinal
Azusa Futatsugi, Yusuke Masuo, Yukio Kato
Summary: The study showed that PBD increased plasma concentrations of four endogenous substrates in rats, but reduced the liver-to-plasma and kidney-to-plasma concentration ratios of HDA and TDA. PBD mainly affected the renal contribution to the disposition of HDA, ODA, and TDA.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Plant Sciences
Ruifeng Liang, Wenjing Ge, Bingjie Li, Weifeng Cui, Xiaofan Ma, Yuying Pan, Gengsheng Li
Summary: The study showed that evodiamine reduced the systemic exposure of pravastatin in NASH rats by enhancing the uptake and distribution in the liver. This was achieved by up-regulating the expression of OATPs. Additionally, evodiamine also decreased the levels of pro-inflammatory cytokines in NASH rats.
PHARMACEUTICAL BIOLOGY
(2022)
Article
Environmental Sciences
Ning Guo, Zoe Disdier, Emilie Thory, Jean-Charles Robinet, Romain V. H. Dagnelie
Summary: The migration of organic compounds in soils is a major concern in environmental issues. Studies have shown that the retention mechanism of hydrophobic compounds by natural organic matter is well known, while the retention of ionizable compounds is mainly related to oxides and clay minerals. The dataset provides insights into the general scheme for assessing the migration of a wide variety of organic compounds, with potential applications in predictive modeling of organic compounds' fate in environmental media.
Article
Biochemistry & Molecular Biology
Santosh Kumar Adla, Arun Kumar Tonduru, Thales Kronenberger, Eva Kudova, Antti Poso, Kristiina M. Huttunen
Summary: In this study, synthetic neurosteroids were delivered into MCF-7 cells via OATPs to investigate structural components necessary for cellular uptake and understand brain drug delivery. The research identified key structural features that improve the affinity of neurosteroids and interact with specific amino acids, providing insights for potential drug delivery strategies across the blood-brain barrier.
Article
Entomology
Janin Roesner, Johanne Tietmeyer, Hans Merzendorfer
Summary: This study identified highly expressed OATP genes in relevant tissues of the red flour beetle, Tribolium castaneum, and showed their involvement in insecticide tolerance through RNAi experiments. The upregulation of certain genes in response to insecticide treatment and increased mortalities after gene silencing suggest the role of OATPs in insecticide resistance, highlighting the importance of studying these transporters in agricultural and forestry practices.
JOURNAL OF PEST SCIENCE
(2021)
Review
Biochemistry & Molecular Biology
Thays Calista Santiago, Larissa Parra, Joao V. Nani, Thiago M. Fidalgo, Nicholas J. Bradshaw, Mirian A. F. Hayashi
Summary: The renin-angiotensin system (RAS) has recently been recognized for its potential roles in the brain, with angiotensin-converting enzyme (ACE) and other RAS components implicated in brain disorders. This review identifies the functions of the RAS and ACEs in the brain, and their association with neurodegenerative and psychiatric illnesses. The findings suggest that ACE inhibitors and angiotensin receptor blockers could be valuable as a novel integrated treatment approach for various brain disorders, particularly psychiatric illnesses.
JOURNAL OF NEUROCHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Dallas Bednarczyk, Carri Boiselle
Article
Biochemical Research Methods
Dallas Bednarczyk
ANALYTICAL BIOCHEMISTRY
(2010)
Article
Chemistry, Multidisciplinary
Maria Luisa Lucero, Ana Gonzalo, Alvaro Ganza, Nerea Leal, Itziar Soengas, Eniko Ioja, Szilvia Gedey, Mirza Jahic, Dallas Bednarczyk
DRUG AND CHEMICAL TOXICOLOGY
(2012)
Article
Chemistry, Medicinal
Jiping Fu, Meiliana Tjandra, Christopher Becker, Dallas Bednarczyk, Michael Capparelli, Robert Elling, Imad Hanna, Roger Fujimoto, Markus Furegati, Subramanian Karur, Theresa Kasprzyk, Mark Knapp, Kwan Leung, Xiaolin Li, Peichao Lu, Wosenu Mergo, Charlotte Miault, Simon Ng, David Parker, Yunshan Peng, Silvio Roggo, Alexey Rivkin, Robert L. Simmons, Michael Wang, Brigitte Wiedmann, Andrew H. Weiss, Linda Xiao, Lili Xie, Wenjian Xu, Aregahegn Yifru, Shengtian Yang, Bo Zhou, Zachary K. Sweeney
JOURNAL OF MEDICINAL CHEMISTRY
(2014)
Article
Chemistry, Medicinal
Callum J. Dickson, Viktor Hornak, Dallas Bednarczyk, Jose S. Duca
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2019)
Article
Pharmacology & Pharmacy
Dallas Bednarczyk, Menaka Sanghvi
Article
Pharmacology & Pharmacy
Dallas Bednarczyk
Summary: The study illustrates that the cellular accumulation of highly permeable low-molecular-weight acidic drugs is more influenced by passive influx and ion trapping than the previously proposed mechanism of OAT2-mediated transport.
DRUG METABOLISM AND DISPOSITION
(2021)
Article
Multidisciplinary Sciences
Joshua Pottel, Duncan Armstrong, Ling Zou, Alexander Fekete, Xi-Ping Huang, Hayarpi Torosyan, Dallas Bednarczyk, Steven Whitebread, Barun Bhhatarai, Guiqing Liang, Hong Jin, S. Nassir Ghaemi, Samuel Slocum, Katalin V. Lukacs, John J. Irwin, Ellen L. Berg, Kathleen M. Giacomini, Bryan L. Roth, Brian K. Shoichet, Laszlo Urban
Article
Pharmacology & Pharmacy
Joe Bentz, Michael P. O'Connor, Dallas Bednarczyk, JoAnn Coleman, Caroline Lee, Johan Palm, Y. Anne Pak, Elke S. Perloff, Eric Reyner, Praveen Balimane, Marie Brannstrom, Xiaoyan Chu, Christoph Funk, Ailan Guo, Imad Hanna, Krisztina Heredi-Szabo, Kate Hillgren, Libin Li, Evelyn Hollnack-Pusch, Masoud Jamei, Xuena Lin, Andrew K. Mason, Sibylle Neuhoff, Aarti Patel, Lalitha Podila, Emile Plise, Ganesh Rajaraman, Laurent Salphati, Eric Sands, Mitchell E. Taub, Jan-Shiang Taur, Dietmar Weitz, Heleen M. Wortelboer, Cindy Q. Xia, Guangqing Xiao, Jocelyn Yabut, Tetsuo Yamagata, Lei Zhang, Harma Ellens
DRUG METABOLISM AND DISPOSITION
(2013)
Article
Pharmacology & Pharmacy
Harma Ellens, Shibing Deng, JoAnn Coleman, Joe Bentz, Mitchell E. Taub, Isabelle Ragueneau-Majlessi, Sophie P. Chung, Krisztina Heredi-Szabo, Sibylle Neuhoff, Johan Palm, Praveen Balimane, Lei Zhang, Masoud Jamei, Imad Hanna, Michael O'Connor, Dallas Bednarczyk, Malin Forsgard, Xiaoyan Chu, Christoph Funk, Ailan Guo, Kathleen M. Hillgren, LiBin Li, Anne Y. Pak, Elke S. Perloff, Ganesh Rajaraman, Laurent Salphati, Jan-Shiang Taur, Dietmar Weitz, Heleen M. Wortelboer, Cindy Q. Xia, Guangqing Xiao, Tetsuo Yamagata, Caroline A. Lee
DRUG METABOLISM AND DISPOSITION
(2013)
Article
Pharmacology & Pharmacy
D Bednarczyk, S Ekins, JH Wikel, SH Wright
MOLECULAR PHARMACOLOGY
(2003)
Article
Physiology
D Bednarczyk, EA Mash, BR Aavula, SH Wright
PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY
(2000)