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https://www.readbyqxmd.com/read/28941201/synthesis-and-evaluation-of-in-vitro-biological-properties-of-ferrocenyl-side-chain-decorated-paclitaxel
#1
Damian Plażuk, Anna Wieczorek, Wojciech M Ciszewski, Karolina Kowalczyk, Andrzej Błauż, Sylwia Pawlędzio, Anna Makal, Chatchakorn Eurtivong, Homayon J Arabshahi, Jóhannes Reynisson, Christian G Hartinger, Błażej Rychlik
Taxanes, including paclitaxel, are widely used in cancer therapy. In an attempt to overcome some of the disadvantages entailed with taxane chemotherapy, we devised the synthesis of ferrocenyl-decorated paclitaxels and studied their biological properties. The cytotoxic activity was measured in a panel of human cancer cell lines of different tissue origin including also multidrug resistant ones. A structure-activity study of paclitaxel ferrocenylation revealed that the N-benzoyl ferrocenyl substituted derivative was the most cytotoxic...
September 21, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28938627/prostate-tumor-overexpressed-1-ptov1-promotes-docetaxel-resistance-and-survival-of-castration-resistant-prostate-cancer-cells
#2
Verónica Cánovas, Yolanda Puñal, Valentina Maggio, Enric Redondo, Mercedes Marín, Begoña Mellado, Mireia Olivan, Matilde Lleonart, Jacques Planas, Juan Morote, Rosanna Paciucci
Metastatic prostate cancer is presently incurable. The oncogenic protein PTOV1, first described in prostate cancer, was reported as overexpressed and significantly correlated with poor survival in numerous tumors. Here, we investigated the role of PTOV1 in prostate cancer survival to docetaxel and self-renewal ability. Transduction of PTOV1 in docetaxel-sensitive Du145 and PC3 cells significantly increased cell survival after docetaxel exposure and induced docetaxel-resistance genes expression (ABCB1, CCNG2 and TUBB2B)...
August 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28934955/the-drug-transporter-abcb1-c-3435c-t-snp-influences-artemether-lumefantrine-treatment-outcome
#3
Kinanga Kiaco, António Sebastião Rodrigues, Virgílio do Rosário, José Pedro Gil, Dinora Lopes
Malaria treatment performance is potentially influenced by pharmacogenetic factors. This study reports an association study between the ABCB1 c.3435C>T, CYP3A4*1B (g.-392A>G), CYP3A5*3 (g.6986A>G) SNPs and artemether + lumefantrine treatment outcome in 103 uncomplicated malaria patients from Angola. No significant associations with the CYP3A4*1B and CYP3A5*3 were observed, while a significant predominance of the ABCB1 c.3435CC genotype was found among the recurrent infection-free patients (p < 0...
September 21, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28928160/quantitative-and-mechanistic-understanding-of-azd1775-penetration-across-human-blood-brain-barrier-in-glioblastoma-patients-using-an-ivive-pbpk-modeling-approach
#4
Jing Li, Jianmei Wu, Xun Bao, Norissa Honea, Youming Xie, Seongho Kim, Alex Sparreboom, Nader Sanai
PURPOSE: AZD1775, a first-in-class, small molecule inhibitor of the Wee1 tyrosine kinase, is under evaluation as a potential chemo- and radio-sensitizer for treating glioblastoma. This study was to prospectively, quantitatively, and mechanistically investigate the penetration of AZD1775 across human blood-brain barrier (BBB). EXPERIMENTAL DESIGN: AZD1775 plasma and tumor pharmacokinetics were evaluated in 20 glioblastoma patients. The drug metabolism, transcellular passive permeability, and interactions with efflux and uptake transporters were determined using human derived in vitro systems...
September 19, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28921565/the-impact-of-p-glycoprotein-and-breast-cancer-resistance-protein-on-the-brain-pharmacokinetics-and-pharmacodynamics-of-a-panel-of-mek-inhibitors
#5
Mark C de Gooijer, Ping Zhang, Ruud Weijer, Levi C M Buil, Jos H Beijnen, Olaf van Tellingen
Mitogen/extracellular signal-regulated kinase (MEK) inhibitors have been tested in clinical trials for treatment of intracranial neoplasms, including glioblastoma (GBM), but efficacy of these drugs has not yet been demonstrated. The blood-brain barrier (BBB) is a major impediment to adequate delivery of drugs into the brain and may thereby also limit the successful implementation of MEK inhibitors against intracranial malignancies. The BBB is equipped with a range of ATP-dependent efflux transport proteins, of which P-gp (ABCB1) and BCRP (ABCG2) are the two most dominant for drug efflux from the brain...
September 16, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28919802/abcb1-and-abcc1-single-nucleotide-polymorphisms-in-patients-treated-with-clozapine
#6
Irina Piatkov, Dorgival Caetano, Yolinda Assur, Sue Lynn Lau, Trudi Jones, Steven C Boyages, Mark McLean
Clozapine (CZ) has superior efficacy to other antipsychotic agents in the treatment of schizophrenia and has been extensively used in clinical practice. ATP-binding cassette (ABC) transporter proteins are responsible for the distribution of various molecules as well as drugs across extracellular and intracellular membranes, including the blood-brain barrier. Genetic variations in these proteins can account for differences in treatment response. We investigated the influence of ABCB1 rs1045642 and ABCC1 rs212090 single-nucleotide polymorphisms (SNPs) on CZ serum level, clinical outcome, and changes in body mass index (BMI) in the first year of CZ treatment...
2017: Pharmacogenomics and Personalized Medicine
https://www.readbyqxmd.com/read/28914344/influence-of-genetic-co-factors-on-the-population-pharmacokinetic-model-for-clopidogrel-and-its-active-thiol-metabolite
#7
Dorota Danielak, Marta Karaźniewicz-Łada, Anna Komosa, Paweł Burchardt, Maciej Lesiak, Łukasz Kruszyna, Agnieszka Graczyk-Szuster, Franciszek Główka
PURPOSE: A high interindividual variability is observed in the pharmacokinetics of clopidogrel, a widely used antiplatelet drug. In the present study, a joint parent-metabolite population pharmacokinetic model was developed to adequately describe observed concentrations of clopidogrel and its active thiol metabolite (H4). METHODS: The study included 63 patients undergoing elective coronarography or percutaneous coronary intervention. The population pharmacokinetic model was developed in the NONMEM 7...
September 15, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28912477/brain-barriers-and-functional-interfaces-with-sequential-appearance-of-abc-efflux-transporters-during-human-development
#8
Kjeld Møllgård, Katarzyna M Dziegielewska, Camilla B Holst, Mark D Habgood, Norman R Saunders
Adult brain is protected from entry of drugs and toxins by specific mechanisms such as ABC (ATP-binding Cassette) efflux transporters. Little is known when these appear in human brain during development. Cellular distribution of three main ABC transporters (ABCC1, ABCG2, ABCB1) was determined at blood-brain barriers and interfaces in human embryos and fetuses in first half of gestation. Antibodies against claudin-5 and -11 and antibodies to α-fetoprotein were used to describe morphological and functional aspects of brain barriers...
September 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28912036/dual-effects-of-the-pi3k-inhibitor-zstk474-on-multidrug-efflux-pumps-in-resistant-cancer-cells
#9
Divya Muthiah, Richard Callaghan
ZSTK474 is a potent phosphoinositide 3-kinase (PI3K) inhibitor that reduces cell proliferation via G1-arrest. However, there is little information on the susceptibility of this anticancer drug to resistance conferred by the multidrug pumps P-glycoprotein (ABCB1) and ABCG2. We have demonstrated that ZSTK474 generated cytotoxicity in cells over-expressing either pump with potency similar to that in drug sensitive cells. In addition, the co-administration of ZSTK474 with the cytotoxic anti-cancer drugs vinblastine and mitoxantrone caused a potentiated cytotoxic effect in both drug sensitive and efflux pump expressing cells...
September 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28904007/synthetic-analogs-of-curcumin-modulate-the-function-of-multidrug-resistance-linked-abc-transporter-abcg2
#10
Megumi Murakami, Shinobu Ohnuma, Michihiro Fukuda, Eduardo E Chufan, Katsuyoshi Kudoh, Keigo Kanehara, Norihiko Sugisawa, Masaharu Ishida, Takeshi Naitoh, Hiroyuki Shibata, Yoshiharu Iwabuchi, Suresh V Ambudkar, Michiaki Unno
Multidrug resistance (MDR) caused by the overexpression of ATP-binding cassette (ABC) transporters in cancer cells is a major obstacle in cancer chemotherapy. Previous studies have shown that curcumin, a natural product and a dietary constituent of turmeric, inhibits the function of MDR-related ABC transporters, including ABCB1, ABCC1, and especially ABCG2. However, the limited bioavailability of curcumin prevents its use for modulation of the function of these transporters in the clinical setting. In this study, we investigated the effects of twenty-four synthetic curcumin analogs with increased bioavailability on the transport function of ABCG2...
September 13, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28893612/tyrphostin-rg14620-selectively-reverses-abcg2-mediated-multidrug-resistance-in-cancer-cell-lines
#11
Chung-Pu Wu, Sung-Han Hsiao, Megumi Murakami, Ming-Jie Lu, Yan-Qing Li, Chia-Hung Hsieh, Suresh V Ambudkar, Yu-Shan Wu
The multidrug resistance (MDR) phenotype associated with the overexpression of ATP-binding cassette (ABC) drug transporters ABCB1, ABCC1 and ABCG2 is a major obstacle in cancer chemotherapy. Numerous epidermal growth factor receptor (EGFR) inhibitors have previously been shown capable of reversing MDR in ABCG2-overexpressing cancer cells. However, most of them are not transporter-specific due to the substantial overlapping substrate specificity among the transporters. In this study, we investigated the interaction between ABCG2 and tyrphostin RG14620, an EGFR inhibitor of the tyrphostin family, in multidrug-resistant cancer cell lines...
September 8, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28882946/pharmacokinetics-of-morphine-in-rats-with-adjuvant-induced-arthritis
#12
Yoshiaki Kimura, Mika Shibata, Mika Tamada, Noriyuki Ozaki, Kunizo Arai
We investigated the in vivo dynamics and analgesic effect of morphine using an adjuvant-induced arthritis (AA) rat as a model of chronic inflammation. Morphine generally binds to μ-opioid receptors in the brain to exert its effects. After several minutes, it is metabolized by glucuronidation via a UDP-glucuronosyltransferase (UGT). Here, we showed that in AA rats, UGT activity in liver microsomes was reduced. Morphine-free serum fractions in AA rats were also decreased (control, 84.9%; AA, 63.9%) and the expression of ATP-binding cassette, sub-family B (MDR/TAP), member 1 (ABCB1), which plays a crucial role in morphine bile excretion, decreased to 23...
September 2017: In Vivo
https://www.readbyqxmd.com/read/28882804/abcb1-and-abcc1-like-transporters-in-immune-system-cells-from-sea-urchins-echinometra-lucunter-and-echinus-esculentus-and-oysters-crassostrea-gasar-and-crassostrea-gigas
#13
Luis Fernando Marques-Santos, Hélène Hégaret, Leonardo Lima-Santos, Fernando Ramos Queiroga, Patricia Mirella da Silva
ABC transporters activity and expression have been associated with the multixenobiotic resistance phenotype (MXR). The activity of these proteins leads to a reduction in the intracellular concentration of several xenobiotics, thus reducing their toxicity. However, little attention has been given to the expression of ABC transporters in marine invertebrates and few studies have investigated their role in immune system cells of sea urchins and shellfish bivalves. The aim of the present study was to investigate the activity of the ABC transporters ABCB1 and ABCC1 in immune system cells of sea urchins (coelomocytes) and oysters (hemocytes) from different climatic regions (Brazil and France)...
September 5, 2017: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/28882160/intrinsic-fluorescence-of-the-clinically-approved-multikinase-inhibitor-nintedanib-reveals-lysosomal-sequestration-as-resistance-mechanism-in-fgfr-driven-lung-cancer
#14
Bernhard Englinger, Sebastian Kallus, Julia Senkiv, Daniela Heilos, Lisa Gabler, Sushilla van Schoonhoven, Alessio Terenzi, Patrick Moser, Christine Pirker, Gerald Timelthaler, Walter Jäger, Christian R Kowol, Petra Heffeter, Michael Grusch, Walter Berger
BACKGROUND: Studying the intracellular distribution of pharmacological agents, including anticancer compounds, is of central importance in biomedical research. It constitutes a prerequisite for a better understanding of the molecular mechanisms underlying drug action and resistance development. Hyperactivated fibroblast growth factor receptors (FGFRs) constitute a promising therapy target in several types of malignancies including lung cancer. The clinically approved small-molecule FGFR inhibitor nintedanib exerts strong cytotoxicity in FGFR-driven lung cancer cells...
September 7, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28881781/twist1-confers-multidrug-resistance-in-colon-cancer-through-upregulation-of-atp-binding-cassette-transporters
#15
Yan-Rong Liu, Lan Liang, Jian Min Zhao, Yang Zhang, Min Zhang, Wei-Long Zhong, Qiang Zhang, Jun-Jie Wei, Meng Li, Jie Yuan, Shuang Chen, Shu-Min Zong, Hui-Juan Liu, Jing Meng, Yuan Qin, Bo Sun, Lan Yang, Hong-Gang Zhou, Tao Sun, Cheng Yang
Multidrug resistance is a major problem in colon cancer treatment. However, its molecular mechanisms remain unclear. Recently, the epithelial-mesenchymal transition (EMT) in anticancer drug resistance has attracted increasing attention. This study investigated whether vincristine treatment induces EMT and promotes multidrug resistance in colon cancer. The result showed that vincristine treatment increases the expression of several ATP-binding cassette transporters in invasive human colon adenocarcinoma cell line (HCT-8)...
August 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28880088/brain-accumulation-of-ponatinib-and-its-active-metabolite-n-desmethyl-ponatinib-is-limited-by-p-glycoprotein-p-gp-abcb1-and-breast-cancer-resistance-protein-bcrp-abcg2
#16
Anita Kort, Stephanie van Hoppe, Rolf W Sparidans, Els Wagenaar, Jos H Beijnen, Alfred H Schinkel
Ponatinib is an oral BCR-ABL1 inhibitor for treatment of advanced leukemic diseases that carry the Philadelphia chromosome, specifically containing the T315I mutation yielding resistance to previously approved BCR-ABL1 inhibitors. Using in vitro transport assays and knockout mouse models, we investigated whether the multidrug efflux transporters ABCB1 and ABCG2 transport ponatinib and whether they, or the drug-metabolizing enzyme CYP3A, affect the oral availability and brain accumulation of ponatinib and its active N-desmethyl metabolite (DMP)...
September 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28867064/increased-dna-methylation-of-abcb1-cyp2d6-and-oprm1-genes-in-newborn-infants-of-methadone-maintained-opioid-dependent-mothers
#17
Poppy McLaughlin, Helen Mactier, Cheryl Gillis, Tamas Hickish, Anton Parker, Wei-Jun Liang, M David Osselton
OBJECTIVE: To investigate whether in utero opioid exposure, which has been linked to adverse neurodevelopmental and social outcomes, is associated with altered DNA methylation of opioid-related genes at birth. STUDY DESIGN: Observational cohort study of 21 healthy methadone-maintained opioid-dependent mother-infant dyads consecutively delivered at >36 weeks of gestation, and 2 comparator groups: smoking, "deprived" opioid-naïve mother-infant dyads (n = 17) and nonsmoking, "affluent" opioid-naïve mother-infant dyads (n = 15)...
August 31, 2017: Journal of Pediatrics
https://www.readbyqxmd.com/read/28865123/kaempferol-increases-apoptosis-in-human-acute-promyelocytic-leukemia-cells-and-inhibits-multidrug-resistance-genes
#18
Maliheh Moradzadeh, Alijan Tabarraei, Hamid Reza Sadeghnia, Ahmad Ghorbani, Ashraf Mohamadkhani, Saiedeh Erfanian, Amirhossein Sahebkar
Acute promyelocytic leukemia (APL) is one of the most life-threatening hematological malignancies. Defects in the cell growth and apoptotic pathways are responsible for both disease pathogenesis and treatment resistance. Therefore, pro-apoptotic agents are potential candidates for APL treatment. Kaempferol is a flavonoid with antioxidant and anti-tumor properties. This study was designed to investigate the cytotoxic, pro-apoptotic and differentiation-inducing effects of kaempferol on HL-60 and NB4 leukemia cells...
September 2, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28865089/impact-of-enzalutamide-and-its-main-metabolite-n-desmethyl-enzalutamide-on-pharmacokinetically-important-drug-metabolizing-enzymes-and-drug-transporters
#19
Johanna Weiss, Jutta Kocher, Corina Mueller, Stephanie Rosenzweig, Dirk Theile
Enzalutamide is a new drug against castration-resistant prostate cancer. Recent data indicate profound induction of drug metabolizing enzymes (e.g. cytochrome P450 isoenzyme (CYP) 3A4) but comprehensive in vitro data on other CYP enzymes, drug conjugating enzymes or drug transporters is scarce. Moreover, mechanisms of induction are poorly investigated and the effects of the active metabolite N-desmethyl enzalutamide are unknown. Using LS180 cells as an induction model and quantitative real-time reverse transcription polymerase chain reaction, our study demonstrated a concentration-dependent induction of CYP1A1, CYP1A2, CYP3A5, CYP3A4, UGT1A3, UGT1A9, ABCB1, ABCC2, and ABCG2 mRNA...
September 1, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28858994/high-plasma-concentrations-of-dolutegravir-in-patients-with-abcg2-genetic-variants
#20
Kiyoto Tsuchiya, Tsunefusa Hayashida, Akinobu Hamada, Sakurako Oki, Shinichi Oka, Hiroyuki Gatanaga
The ATP-binding cassette transporters B1 (ABCB1) and G2 (ABCG2) are both expressed in the intestine and known as efflux transporters of drugs. Dolutegravir was identified recently as a substrate of both ABCB1 and ABCG2. This study aimed to determine the relations between single-nucleotide polymorphisms of ABCB1 and ABCG2 genes and plasma dolutegravir concentrations. Plasma samples were obtained from 42 HIV-1-infected patients treated with dolutegravir-containing regimens 0.5-4 h after dolutegravir dosing...
August 29, 2017: Pharmacogenetics and Genomics
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