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.
Review
Pharmacology & Pharmacy
Lenka Hruba, Viswanath Das, Marian Hajduch, Petr Dzubak
Summary: Nucleoside-based drugs, widely used in the treatment of various diseases, have been hindered by drug resistance. This review explores the mechanisms of resistance, including changes in membrane transporters, activating kinases, drug elimination strategies, and DNA damage repair mechanisms. The critical analysis in this review points towards novel therapeutic strategies such as targeted therapies, new nucleoside analogs, and synergistic drug combinations to overcome resistance and improve patient outcomes.
BIOCHEMICAL PHARMACOLOGY
(2023)
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)
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)
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)
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)
Review
Pharmacology & Pharmacy
Patrick T. Ronaldson, Thomas P. Davis
Summary: Ischemic stroke is a major cause of morbidity and mortality globally. Despite positive results in preclinical studies, only one compound has advanced to Phase III clinical trial evaluation. This may be due to the neglect of transport mechanisms at the blood-brain barrier and neurovascular unit. This review highlights the role of BBB transporters in drug delivery and their expression in different brain cell types.
Review
Biology
Lara Console, Mariafrancesca Scalise
Summary: Extracellular vesicles, including exosomes, play a crucial role in promoting chemoresistance in cancer cells through various mechanisms.
Article
Neurosciences
Elena Puris, Seppo Auriola, Sabrina Petralla, Robin Hartman, Mikko Gynther, Elizabeth C. M. de Lange, Gert Fricker
Summary: There is evidence that membrane transporters expressed at the blood-brain barrier and brain parenchymal cells play a role in Alzheimer's disease development. This study examined changes in transporter protein expression in the brain of TgF344AD rats compared to wild-type animals and found significant alterations. These findings provide insight into the molecular mechanisms of AD and the use of the TgF344AD rat model in drug development research.
NEUROBIOLOGY OF DISEASE
(2022)
Article
Pharmacology & Pharmacy
Craig Russell, Majad Hussain, David Huen, Ayesha S. Rahman, Afzal R. Mohammed
Summary: This study explores the use of DNA microarrays as a high throughput screening tool to identify markers for predicting bioavailability and formulation-driven physiological responses. Significant changes in gene expression were found as a result of formulation exposure, including genes related to drug transport and metabolism.
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
(2021)
Review
Chemistry, Medicinal
Rachel L. Mynott, Craig T. Wallington-Beddoe
Summary: The review evaluates the resistance of multiple myeloma patients to novel therapies, particularly focusing on the mechanisms of resistance to proteasome inhibitors and immunomodulatory drugs, as well as the role of transporters in drug resistance.
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE
(2021)
Review
Biochemistry & Molecular Biology
Joanna Lapczuk-Romanska, Maria Drozdzik, Stefan Oswald, Marek Drozdzik
Summary: The kidney is not only involved in metabolite elimination, but also plays a critical role in pharmacotherapy. Membrane carriers and transporters expressed in kidney tubule epithelial cells are important in drug elimination, determining drug nephrotoxicity and drug-drug interactions, as well as serving as direct drug targets. This review discusses these aspects of kidney transport proteins.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
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
C. Goldeman, M. Andersen, A. Al-Robai, T. Buchholtz, N. Svane, B. Ozgur, B. Holst, E. Shusta, V. J. Hall, L. Saaby, P. Hyttel, B. Brodin
Summary: This study investigated the differentiation of human induced pluripotent stem cells (hiPSCs) into brain capillary endothelial-like cells (BCEC) for potential use in drug delivery research. The results demonstrated that the BCEC monolayers exhibited properties of the blood-brain barrier, including barrier tightness, high dynamic range, and functional transport capabilities.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Lyndsey L. Anderson, Maia G. Etchart, Laura MacNair, M. Hunter Land, Irina A. Mosesova, Marcel O. Bonn-Miller, Jonathon C. Arnold
Summary: The legalization of medicinal cannabis has led to increased use of commercial cannabis-based products, which can potentially interact with other drugs. This study evaluated the inhibitory potential of three commercially available cannabis-based products on human transporters and found that some of these products can inhibit transporter function.
CANNABIS AND CANNABINOID RESEARCH
(2022)