The development of MDR (multidrug resistance) in yeast is due to a number of mechanisms. The most documented mechanism is enhanced extrusion of drugs mediated by efflux pump proteins belonging to either the ABC (ATP-binding cassette) superfamily or MFS (major facilitator superfamily). These drug-efflux pump proteins are localized on the plasma membrane, and the milieu therein affects their proper functioning. Several recent studies demonstrate that fluctuations in membrane lipid composition affect the localization and proper functioning of the MDR efflux pump proteins. Interestingly, the efflux pumps of the ABC superfamily are particularly susceptible to imbalances in membrane-raft lipid constituents. This review focuses on the importance of the membrane environment in functioning of the drug-efflux pumps and explores a correlation between MDR and membrane lipid homoeostasis.
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http://dx.doi.org/10.1042/BSR20080071 | DOI Listing |
Sci Rep
January 2025
Department of Gastroenterology, Affiliated Changzhou No. 2 People's Hospital of Nanjing Medical University, Changzhou Medical Center, Nanjing Medical University, 68 Gehu Middle Road, Wujing District, Changzhou, 213000, Jiangsu, China.
Patients with diabetes have a high risk of failure of H. pylori eradication therapy. The present study aims to evaluate the efficacy and safety of vonoprazan-amoxicillin (VA) dual therapy for the treatment of H.
View Article and Find Full Text PDFACS Appl Mater Interfaces
January 2025
Key Laboratory of Analytical Chemistry for Life Science of Shaanxi Province, School of Chemistry and Chemical Engineering, Key Laboratory of Applied Surface and Colloid Chemistry, Ministry of Education, Shaanxi Normal University, Xi'an 710119, P. R. China.
High expression of drug efflux pump makes antibiotics ineffective against bacteria, leading to drug-resistant strains and even the emergence of "superbugs". Herein, we design and synthesize a dual functional o-nitrobenzene (NB)-modified conjugated oligo-polyfluorene vinylene (OPFV) photosensitizer, OPFV-NB, which can depress efflux pump activity and also possesses photodynamic therapy (PDT) for synergistically overcoming drug-resistant bacteria. Upon light irradiation, the OPFV-NB can produce aldehyde active groups to covalently bind outer membrane proteins, such as tolerant colicin (TolC), blocking drug efflux of bacteria.
View Article and Find Full Text PDFToxicol Sci
January 2025
Takeda Development Center Americas, Inc, Cambridge, MA, USA.
The frequency of drug-induced liver injury (DILI) in clinical trials remains a challenge for drug developers despite advances in human hepatotoxicity models and improvements in reducing liver-related attrition in preclinical species. TAK-994, an oral orexin receptor 2 agonist, was withdrawn from phase II clinical trials due to the appearance of severe DILI. Here, we investigate the likely mechanism of TAK-994 DILI in hepatic cell culture systems examined cytotoxicity, mitochondrial toxicity, impact on drug transporter proteins, and covalent binding.
View Article and Find Full Text PDFNagoya J Med Sci
November 2024
Department of Anesthesiology, Nagoya University Graduate School of Medicine, Nagoya, Japan.
Postoperative atrial fibrillation complicates 15-40% of cardiac surgery cases and is associated with various adverse health outcomes including high mortality. Although vasopressin administration decreases postoperative atrial fibrillation in on-pump coronary artery bypass grafting, its use in off-pump coronary artery bypass grafting has not been investigated. Therefore, we evaluated the effect of vasopressin use in off-pump coronary artery bypass grafting.
View Article and Find Full Text PDFJ Ethnopharmacol
January 2025
Department of Pharmacology, Shaanxi University of Chinese Medicine, No. 1 Middle Section of Century Avenue, Xianyang 712046, People's Republic of China. Electronic address:
Ethnopharmacological Relevance: Dioscorea bulbifera L. (DBL) was a traditional Chinese medicine commonly used to treat goitre and cancer. Nevertheless, its clinical application may lead to liver injury.
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