Ganoci, Lana Trkulja, Vladimir Živković, Maja Božina, Tamara Šagud, Marina Lovrić, Mila Božina, Nada
Published in
Progress in neuro-psychopharmacology & biological psychiatry
The relevance of the multidrug resistance (ABCB1) and breast cancer resistance (ABCG2) protein transporter polymorphisms for treatment with long-acting intramuscular (LAI) risperidone is largely unknown. We explored the relationship between these polymorphisms and cytochrome P450 (CYP) 2D6 genotype-predicted phenotype in their effects on drug dispo...
Marques, Maiara Bernardes Machado, Ayane Pontes Santos, Priscila Antiqueira Carrett-Dias, Michele Araújo, Gabriela Soares Alves, Barbara da Silva de Oliveira, Bárbara Santos da Silva Júnior, Flavio M R Dora, Cristiana Lima Cañedo, Andrés Delgado
...
Published in
Anti-cancer agents in medicinal chemistry
The quercetin has potential against the multidrug resistance (MDR) phenotype, but with low bioavailability. The increase in the bioavailability can be obtained with nanostructures. To analyze the effects of quercetin and its nanoemulsion on MDR and non-MDR cells. We used: high pressure homogenization for nanoemulsion production; Trypan Blue for cyt...
Crowe, Andrew
Published in
SLAS discovery : advancing life sciences R & D
In drug discovery it is essential that one of the parameters tested for any new chemical entity is its affinity for human efflux systems, most notably P-glycoprotein (P-gp). These efflux systems affect not only rates of oral absorption but also rates of excretion through the liver, blood-brain barrier, and accumulation in potential target cells tha...
Huang, Ronglan Zhan, Qinghao Hu, Wenbin Yang, Renmin Cheng, Nan Han, Yongsheng Yue, Xiuyu
Published in
Genetic testing and molecular biomarkers
Objective: Osteonecrosis of the femoral head (ONFH) is a severe pathological state with multiple etiologies. Steroid hormone metabolism-related genes play an important role in ONFH. The aim of this study was to investigate the relationships between polymorphisms of the drug-metabolizing enzyme gene, cytochrome P450 (CYP450), and the drug transporte...
Williams, Mark S. Basma, Naseer J. Amaral, Fabio M. R. Williams, Gillian Weightman, John P. Breitwieser, Wolfgang Nelson, Louisa Taylor, Stephen S. Wiseman, Daniel H. Somervaille, Tim C. P.
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Published in
BMC Cancer
BackgroundResistance to chemotherapy is the most common cause of treatment failure in acute myeloid leukemia (AML) and the drug efflux pump ABCB1 is a critical mediator. Recent studies have identified promoter translocations as common drivers of high ABCB1 expression in recurrent, chemotherapy-treated high-grade serous ovarian cancer (HGSC) and bre...
Ji, Jin-Zi Li, Yi-Fei Jiang, Li-Ping Tai, Ting Ge, Peng-Xin Mi, Qiong-Yu Zhu, Ting Xie, Hong-Guang
Published in
Biochemical pharmacology
Variability in P-glycoprotein (P-gp) efflux transporting activity was supposed to be involved in altered intestinal absorption and bioavailability of clopidogrel in patients; however, reliable evidence is still lacking. In this study, we sought to determine whether P-gp could play an important role in the metabolic activation of and platelet respon...
Shin, Hyo-Bin Jung, Eui Hyun Kang, Pureum Lim, Chang Woo Oh, Kyung-Yul Cho, Chang-Keun Lee, Yun Jeong Choi, Chang-Ik Jang, Choon-Gon Lee, Seok-Yong
...
Published in
Archives of pharmacal research
Losartan has been shown to be a substrate of the drug-efflux transporter MDR1, encoded by the ABCB1 gene. ABCB1 c.2677G>T and c.3435C>T variants are known to be associated with reduced expression and function of P-glycoprotein (P-gp). We investigated the effects of ABCB1 diplotype on the pharmacokinetics of losartan. Thirty-eight healthy Korean vol...
Scholefield, Melissa Church, Stephanie J Xu, Jingshu Robinson, Andrew C Gardiner, Natalie J Roncaroli, Federico Hooper, Nigel M Unwin, Richard D Cooper, Garth J S
Published in
Metabolites
The use of post-mortem human tissue is indispensable in studies investigating alterations in metabolite levels in neurodegenerative conditions such as Alzheimer's disease (AD). However, variability between samples may have unknown effects on metabolite concentrations. The aim of this study was to characterize the impact of such variables. Cingulate...
Löscher, Wolfgang Gericke, Birthe
Published in
Pharmaceutics
The blood-brain barrier (BBB) limits the pharmacotherapy of several brain disorders. In addition to the structural and metabolic characteristics of the BBB, the ATP-driven, drug efflux transporter P-glycoprotein (Pgp) is a selective gatekeeper of the BBB; thus, it is a primary hindrance to drug delivery into the brain. Here, we review the complex r...
Gao, Hai-Ling Gupta, Pranav Cui, Qingbin Ashar, Yunali V. Wu, Zhuo-Xun Zeng, Leli Lei, Zi-Ning Teng, Qiu-Xu Ashby, Charles R. Jr. Guan, Yingjun
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Published in
Frontiers in Oncology
The efficacy of anti-cancer drugs in patients can be attenuated by the development of multi-drug resistance (MDR) due to ATP-binding cassette (ABC) transporters overexpression. In this in vitro study, we determined the reversal efficacy of the epidermal growth factor receptor (EFGR) inhibitor, saptinib, in SW620 and SW720/Ad300 colon cancer cells a...
