Article
Reproductive Biology
Anastasia Weyrich, Markus Frericks, Michael Eichenlaub, Steffen Schneider, Thomas Hofmann, Steven Van Cruchten, Bennard van Ravenzwaay
Summary: This study compared the expression levels of xenobiotic transporters in liver, kidney, and placenta of human, Wistar rat, and New Zealand White rabbit during pre- and postnatal development, revealing significant differences in transporter expression in development and between species.
REPRODUCTIVE TOXICOLOGY
(2022)
Article
Pharmacology & Pharmacy
Kakeru Sato, Tatsuya Seki, Asuka Mizutani, Yuka Muranaka, Shiho Hirota, Kodai Nishi, Kana Yamazaki, Ryuichi Nishii, Takeo Nakanishi, Ikumi Tamai, Keiichi Kawai, Masato Kobayashi
Summary: Chemoradiotherapy is commonly used in cancer treatment, and stereotactic body radiotherapy (SBRT) is a high-dose radiotherapy used to treat various types of cancer. This study investigated the relationship between the accumulation of methotrexate and the expression levels of solute carrier (SLC) and ATP-binding cassette (ABC) transporters in cancer cells after high-dose X-ray irradiation. The results showed that gene expression levels of solute carrier transporters (OATP1B1/1B3/1B7) and ATP-binding cassette transporters (MRP1/2) were altered after irradiation, leading to a decrease in the accumulation of methotrexate in cancer cells.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Chih-hsuan Hsin, Annett Kuehne, Yi Gu, Gabriele Jedlitschky, Yohannes Hagos, Dirk Gruendemann, Uwe Fuhr
Summary: This study investigated the inhibitory effects of individual probe substrates on major transporters in vitro, using a clinically tested cocktail of adefovir, digoxin, metformin, sitagliptin, and pitavastatin. Only sitagliptin showed significant inhibition on several transporters, suggesting a need for dose reduction in the cocktail.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Review
Pharmacology & Pharmacy
Valerio Taggi, Mario Riera Romo, Micheline Piquette-Miller, Henriette E. Meyer zu Schwabedissen, Sibylle Neuhoff
Summary: Drug transporters are crucial for maintaining chemical balance and homeostasis in tissues, as well as for the absorption, distribution, and elimination of clinically important drugs. Diseases can alter the expression and function of drug transporters. However, there is limited knowledge on transporter regulation in critical protective barriers, which requires further research.
Article
Chemistry, Medicinal
Tomoko Yamaguchi, Daiki Sako, Toshiki Kurosawa, Misae Nishijima, Ayaka Miyano, Yoshiyuki Kubo, Sumio Ohtsuki, Kenji Kawabata, Yoshiharu Deguchi
Summary: MDR1-expressing hiPS-BMECs can be used as an in vitro model of the human blood-brain barrier, demonstrating good barrier function and MDR1-mediated efflux transport.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Article
Toxicology
Helen Hammer, Felix Schmidt, Philip Marx-Stoelting, Oliver Poetz, Albert Braeuning
Summary: Most drugs and xenobiotics are metabolized in the liver, where cytochrome P450 enzymes and transport proteins play a key role in the process. Variations in the levels of drug-metabolizing enzymes and transporters among different experimental systems determine the pharmacokinetic properties of a compound. By comparing the levels of key proteins in different experimental models, this study provides a comprehensive overview of the similarities and differences in drug metabolism-related proteins.
ARCHIVES OF TOXICOLOGY
(2021)
Article
Chemistry, Medicinal
Solene Marie, Irene Hernandez-Lozano, Marc Le Vee, Louise Breuil, Wadad Saba, Maud Goislard, Sebastien Goutal, Charles Truillet, Oliver Langer, Olivier Fardel, Nicolas Tournier
Summary: Endotoxemia-induced inflammation affects the activity of hepatocyte transporters, leading to changes in drug and bile acid elimination. Tc-99m-mebrofenin imaging is useful for studying disease-related alterations in hepatocyte transporter function.
Review
Biology
Lorena Pochini, Michele Galluccio
Summary: For over 20 years, yeast has been widely used for expressing human membrane transporters, particularly the SLC superfamily, which plays crucial roles in maintaining cellular homeostasis. However, many SLCs remain poorly understood in terms of substrate specificity and function, and their 3D structure is largely unknown. Understanding protein expression in systems that allow functional production of SLCs is essential for filling these knowledge gaps and potentially impacting human health.
Article
Physiology
Riccardo F. Romersi, Sascha C. T. Nicklisch
Summary: An organism's diet plays a crucial role in its exposure to beneficial nutrients and harmful environmental chemicals. Transporters in the intestine prevent the uptake of xenobiotics from dietary sources. While some chemicals induce the expression of defense transporters in fish and aquatic invertebrates, others can bind to and inhibit certain transporters, leading to toxic accumulations. The molecular interactions between xenobiotics and transporters are poorly understood in aquatic organisms, highlighting the need for further research.
FRONTIERS IN PHYSIOLOGY
(2022)
Article
Health Care Sciences & Services
Miriam Saiz-Rodriguez, Dolores Ochoa, Pablo Zubiaur, Marcos Navares-Gomez, Manuel Roman, Paola Camargo-Mamani, Sergio Luquero-Bueno, Gonzalo Villapalos-Garcia, Raquel Alcaraz, Gina Mejia-Abril, Estefania Santos-Mazo, Francisco Abad-Santos
Summary: For patients with type 2 diabetes, the drug metformin is commonly prescribed, but the response to this drug varies greatly among individuals. In order to study the impact of transporter variations on metformin pharmacokinetics, a study was conducted on healthy participants without confounding factors. This study is the first of its kind to consider demographic characteristics and all transporters involved in metformin distribution. The pharmacokinetic parameters of metformin were found to be influenced by age, sex, ethnicity, and several transporter polymorphisms.
JOURNAL OF PERSONALIZED MEDICINE
(2023)
Article
Chemistry, Medicinal
Toshiki Kurosawa, Yuma Tega, Daiki Sako, Tatsuki Mochizuki, Tomoko Yamaguchi, Kenji Kawabata, Katsuhisa Inoue, Naoki Ito, Hiroyuki Kusuhara, Yoshiharu Deguchi
Summary: This study investigated the transport mechanism of 6-mercaptopurine (6-MP) across the blood-brain barrier (BBB) using human induced pluripotent stem cell-derived microvascular endothelial cells (hiPSBMECs). The results showed that uptake of 6-MP was significantly influenced by ENBT1 and MRP5 proteins, with different inhibition profiles observed in different directions of transport.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Hiroyuki Sasabe, Toshihisa Koga, Masayuki Furukawa, Masayuki Matsunaga, Katsunori Sasahara, Kenta Hashizume, Yoshihiro Oozone, Immaculate Amunom, Mikako Torii, Ken Umehara, Eiji Kashiyama, Kenji Takeuchi
Summary: The in vitro study on brexpiprazole showed weak inhibitory effects on CYP enzymes and transporters, indicating unlikely clinically relevant drug interactions.
Review
Biochemistry & Molecular Biology
Michele Galluccio, Lara Console, Lorena Pochini, Mariafrancesca Scalise, Nicola Giangregorio, Cesare Indiveri
Summary: Membrane transport systems play a crucial role in maintaining cell homeostasis and drug interactions. E. coli is a preferred host for expressing human membrane proteins, but their hydrophobicity and structural differences pose challenges. This review summarizes various strategies for expressing human transport systems in bacteria.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Yen T. K. Nguyen, Hoa T. T. Ha, Tra H. Nguyen, Long N. Nguyen
Summary: The brain exchanges nutrients and small molecules with blood through the blood-brain barrier, and glucose plays a critical role in providing energy for the brain. The brain also takes up various substances through different transport systems, and unraveling these mechanisms is key in understanding the brain's nutritional requirements and potential therapeutic interventions for neurological disorders.
CELLULAR AND MOLECULAR LIFE SCIENCES
(2022)
Review
Biology
Lara Console, Mariafrancesca Scalise
Summary: Extracellular vesicles, including exosomes, play a crucial role in promoting chemoresistance in cancer cells through various mechanisms.
