Dissertations / Theses on the topic 'ABCG2 inhibitors'
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Fischer, Carolin [Verfasser], and Burkhard [Akademischer Betreuer] König. "New inhibitors for the ABCG2 transporter / Carolin Fischer. Betreuer: Burkhard König." Regensburg : Universitätsbibliothek Regensburg, 2011. http://d-nb.info/1023312131/34.
Full textLi, Jiyang [Verfasser]. "Investigation of Phthalazine, Quinazoline and Pyrimidine Derivatives as ABCG2 Inhibitors / Jiyang Li." Bonn : Universitäts- und Landesbibliothek Bonn, 2018. http://d-nb.info/1167857135/34.
Full textOchoa, Puentes Cristian [Verfasser], and Burkhard [Akademischer Betreuer] König. "Potent and selective ABCG2 inhibitors derived from tariquidar / Cristian Ochoa Puentes. Betreuer: Burkhard König." Regensburg : Universitätsbibliothek Regensburg, 2012. http://d-nb.info/1033688312/34.
Full textMacalou, Sira. "Le transporteur ABCG2 de multiples drogues : rôle d’une séquence spécifique et recherche d’inhibiteurs sélectifs." Thesis, Lyon 1, 2009. http://www.theses.fr/2009LYO10301.
Full textDuring chemotherapy, cancer cells frequently succeed to escape the toxic effects of drugs by developing mechanisms of chemoresistance which often result from the presence of an efflux system of these drugs. Such a chemoresistance is correlated to the MDR (MultiDrug Resistance) phenotype and associated to overexpression of membrane ATPases belonging to the ABC (ATP-Binding Cassette) transporters. The ABCG2 transporter belongs to this large family of proteins. Sequence alignment allowed the identification of a specific (LSGGE) sequence in ABCG2, which is quite similar to the canonical sequence signature (VSGGE) of all ABC transporters. Point mutation of these residues into alanine produced a loss of function in L352A and S353A mutants, as observed in transport and on ATPase activity. Structure-activity relationships drawn from some compounds among the family of flavonoids allowed the identification of MBLI 97, boeravinone G, MHT and ABI as potent and ABCG2-specific inhibitors, able to revert multidrug resistance and chemosensitize cell growth. The study of specific sequences and use of specific inhibitors of these transporters constitute strategies to abolish cancer cell chemoresistance and to increase the efficiency of chemotherapeutic treatments
Krapf, Michael [Verfasser]. "Investigation of Quinazoline Derivatives as Inhibitors of Breast Cancer Resistance Protein (BCRP/ABCG2) / Michael Krapf." Bonn : Universitäts- und Landesbibliothek Bonn, 2018. http://d-nb.info/1160594155/34.
Full textArnaud, Ophélie. "Étude fonctionnelle de la région intracellulaire d’ABCG2 et modulation d’ABCG2 et ABCB1 humains par des petidomimétiques non compétitifs." Thesis, Lyon 1, 2011. http://www.theses.fr/2011LYO10091/document.
Full textResistance to chemotherapy is partly due to efflux pumps expressed in the plasma membrane which prevent the accumulation of anticancer drugs in the tumour cells. Three human ATP-binding Cassette (ABC) transporters are particularly involved in this phenotype: P-gp/ABCB1, MRP1/ABCC1, and the last discovered BCRP/ABCG2. Because of their involvement in chemoresistance, it is critical to understand the mechanism by which those ABC transporters recognize and transport drugs. The mutagenesis study of the intracellular loops, ICL0 and 1 shows that these loops are involved in this mechanism. Two amino acids were particularly remarkable: W379 which act as a substrate filter and H457 which can be involved in substrate recognition and binding. In order to restore the cancer cell sensitivity to chemotherapeutic drugs, we have developed a new class of peptide inhibitors, specific to one transporter. A structure-activity relationship study has been performed and made it possible to develop a second generation of molecules. The most efficient compound inhibiting ABCB1 (CT1347) or ABCG2 (CT1364) have none or limitated cytotoxic effects. These compounds restore the activity of chemotherapeutic drugs and act as non competitive inhibitors. Moreover, CT1364 inhibits the ATP hydrolysis activity and lead to a rapid reduction of ABCG2 expression. Initial in vivo tests that have been carried out with CT1364 associated with irinotecan allow to observe a growth reduction of small mice xenografts
Antoni, Frauke [Verfasser], and Günther [Akademischer Betreuer] Bernhardt. "Design, Synthesis and Characterization of ABCG2 Inhibitors with a Focus on Water Solubility and Stability in Plasma / Frauke Antoni ; Betreuer: Günther Bernhardt." Regensburg : Universitätsbibliothek Regensburg, 2021. http://d-nb.info/1225121493/34.
Full textGauthier, Charlotte. "Identification et mécanisme d'action de modulateurs sélectifs du transporteur ABCG2 responsable de la chimiorésistance de cellules cancéreuses." Phd thesis, Université Claude Bernard - Lyon I, 2014. http://tel.archives-ouvertes.fr/tel-00995077.
Full textGomes, Guilherme Wataru. "Expressão gênica dos transportadores de membrana ABCB1,ABCG2, SLC22A1 e SLCO1A2 em linhagens celulares tratadas com inibidor comercial da via JAK-STAT." Universidade de São Paulo, 2015. http://www.teses.usp.br/teses/disponiveis/9/9136/tde-16032016-095918/.
Full textBACKGROUND: JAK-STAT pathway signaling disregulation is a hallmark of myeloproliferative neoplasms (MPN), hematopoietic stem cell clonal diseases, among which is myelofibrosis (MF). Several JAK inhibitors have been developed for MF treatment and are found in different stages of clinical development. Because the recent development of these compounds, the role of drug transporters in their pharmacokinetics is poorly understood. These proteins perform celular influx and effux of endogenous substrates and xenobiotics, and changes in the expression of these drugs transporters may affect the response to these drugs. AIM: To evaluate the effect of a JAK-STAT pathway commercial inhibitor in gene expression of drug transporters ABCB1, ABCG2, SLC22A1 and SLCO1A2 in HepG2, Caco-2 and HEL92.1.7 cells. METHODS: Hepatocellular carcinoma cell line HepG2, colorectal adenocarcinoma cell line Caco-2 and human erythroleukemia homozygous JAK2V617F cell line HEL92.1.7 were grown and treated with the JAK-STAT pathway inhibitor JAK Inhibitor I. In order to determine the optimal concentration for treatment with the inhibitor, cells were treated with several concentrations of JAK inhibitor by 24 hours, and cell viability and DNA fragmentation tests were performed. Once the treatment conditions were standardized, total RNA were obtained from the cells, and cDNA was synthesized in order to evaluate the mRNA expression of ABCB1, ABCG2, SLC22A1 and SLCO1A2 genes, performed by real time PCR. We also evaluate the expression of drug efflux transporters ABCB1 and ABCG2 by flow cytometry, using primary antibodies directed to these proteins. RESULTS: In HepG2 cells, it was observed an increase in ABCB1 mRNA expression in cells treated with 4,00 µM of JAK inhibitor, when compared with controls (cells exposed only to the vehicle) (P=0.041). There was no change in ABCB2 and SLC22A1 mRNA expression with the treatment with JAK inhibitor in this cell line (P>0.05); SLCO1A2 mRNA was not detected in this cell line. In Caco-2 cells, ABCB1, ABCG2, SLC22A1 and SLCO1A2 mRNA expression did not change with treatment with the JAK inhibitor at the concentrations used (0.25 µM to 1.00 µM) by 24 hours (P>0.05). In HEL92.1.7 cells, it was not observed differences in ABCB1, ABCG2 and SLC22A1 mRNA expression with the treatment with 1 µM of JAK inhibitor by 24 hours when compared with controls (P>0.05); in this cell line, SLCO1A2 mRNA was not detected. Protein expression of ABCB1 and ABCG2 drug transporters has not changed with treatment with the JAK inhibitor under the conditions used in the three cell lines studied. CONCLUSIONS: Only HepG2 cells presented an increase in mRNA expression of drug efflux transporter ABCB1 in presence of high levels of JAK inhibitor, suggesting that JAK inhibitors could modulate this transporter gene expression in liver. Treatment with JAK-STAT pathway inhibitor was not associated with changes in ABCB1 and ABCG2 protein expression in all cell lines studied.
Turner, Joel G. "Drug resistance to topoisomerase directed chemotherapy in human multiple myeloma." [Tampa, Fla] : University of South Florida, 2008. http://purl.fcla.edu/usf/dc/et/SFE0002446.
Full textNguyen, Kim-Anh. "Synthèse de nouveaux détergents extractants et stabilisants des protéines membranaireset synthèse de dérivés d'aurones comme inhibiteurs d'ABCC2." Thesis, Université Grenoble Alpes (ComUE), 2017. http://www.theses.fr/2017GREAV043/document.
Full textUnderstanding of tridimensional structure of membrane proteins (MPs) is crucial in medicinal chemistry and biochemistry. To maintain them in solution and consequently to prevent them from aggregation for structural and functional studies, utilization of detergents is indispensable. However, the conformation of MPs in complex with detergents could be very different from its membrane-embedded one. We synthetized new family of detergents, in which the incorporated carboxylates could generate a network of salt-bridges with basic-residue-enriched region of MPs, confer tighter interactions which could preserve their structural integrity. The detergents in which the glycoconjugation was achieved by Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction showed remarkable capacity to extract, stabilize and crystallize studied PMs. On the other hand, novel inhibitors of ABCC2, a non-crystallized MP to date, were identified by screening: the 2-indolylmethylenebenzofuranones. Such compounds could be considered as useful tools to further investigate the role of ABCC2 in the pharmacokinetics of drugs
Spindler, Anna [Verfasser]. "Synthese und Untersuchung neuer ABCG2 Inhibitoren / Anna Spindler." Bonn : Universitäts- und Landesbibliothek Bonn, 2017. http://d-nb.info/1130704688/34.
Full textWillmes, Thomas [Verfasser]. "Synthese, Testung und 3D-QSAR von ABCG2-Inhibitoren / Thomas Willmes." Bonn : Universitäts- und Landesbibliothek Bonn, 2021. http://d-nb.info/1240761309/34.
Full textKöhler, Sebastian Christoph [Verfasser]. "Über ABCG2-Inhibitoren mit Heteroaryl-phenylamid- und Carborancarboxamid-Grundstruktur / Sebastian Christoph Köhler." Bonn : Universitäts- und Landesbibliothek Bonn, 2017. http://d-nb.info/1159955212/34.
Full textKraege, Stefanie [Verfasser]. "Design, Synthese und Biologische Testung neuartiger Chalkon-Derivate als ABCG2 Inhibitoren / Stefanie Kraege." Bonn : Universitäts- und Landesbibliothek Bonn, 2017. http://d-nb.info/1132711290/34.
Full textPozza, Alexandre. "Surexpression hétérologue et purification du transporteur membranaire ABCG2 : mécanisme d'interaction avec des substrats et des inhibiteurs spécifiques." Lyon 1, 2007. http://www.theses.fr/2007LYO10327.
Full textABCG2 is an ABC half-transporter involved in multidrug resistance of cancer cells. Our aim is to understand the mechanism of transport and of interaction with specific inhibitors. After some unsuccessful attempts in bacteria, ABCG2 was functionally overexpressed with the insect cells/baculovirus system. The effects of some inhibitors on ATPase activity were studied, as well as the capacity of binding to the purified transporter. This allowed to bring evidence for a different inhibition mechanism for the same inhibitor between the wild-type and R482T mutant of the transporter. The difference in transport-substrate spectrum induced by the mutation is not due to binding, but more likely related to membrane translocation. The recombinant protein appears as two bands, the difference of which is probably of conformational origin
Arnaud, Ophélie. "Étude fonctionnelle de la région intracellulaire d'ABCG2 et modulation d'ABCG2 et ABCB1 humains par des petidomimétiques non compétitifs." Phd thesis, Université Claude Bernard - Lyon I, 2011. http://tel.archives-ouvertes.fr/tel-00846207.
Full textPeña, Solórzano Diana Catherine [Verfasser], Oliver [Akademischer Betreuer] Reiser, Burkhard [Akademischer Betreuer] Koenig, Rodrigo [Akademischer Betreuer] Abonia, and Claudia [Akademischer Betreuer] Rubiano. "New Analogs of Tariquidar: Synthesis, Characterization and Evaluation of their Inhibitory Activity against Breast Cancer Resistance Protein (ABCG2) / Diana Catherine Peña Solórzano ; Oliver Reiser, Burkhard Koenig, Rodrigo Abonia, Claudia Rubiano." Regensburg : Universitätsbibliothek Regensburg, 2018. http://d-nb.info/1160086311/34.
Full textCheng, Hsing Wen, and 鄭幸文. "A fluorescent cell-based functional screening of niclosamide derivatives as specific inhibitors of human ABCG2." Thesis, 2013. http://ndltd.ncl.edu.tw/handle/47162651364033822863.
Full text長庚大學
生物醫學研究所
101
A major problem in cancer is cancer metastasis. Many metastatic cancers are resistant to treatment with a variety of structurally unrelated anti-cancer drugs, a phenomenon that is known as multidrug resistance (MDR). MDR often is mediated by ATP-binding cassette (ABC) transporters that can generate energy from ATP hydrolysis to actively transport a variety of compounds across biological membranes. ABCB1 and ABCG2 are ABC transporters that have been shown to play an important role in the development of MDR in cancers. In an attempt to overcome ABCB1 or ABCG2-mediated MDR in cancer patients, many inventive strategies have been considered and evaluated. Currently, the most direct way to re-sensitize MDR cancer cells is to either inhibit the function directly, or to reduce the protein expression of these MDR-linked ABC transporters. Tremendous effort has been invested in the development of potent modulators of ABCB1 and ABCG2 for the past two decades. Unfortunately, due to a substantial overlapping substrate specificity between ABCB1 and ABCG2, finding a chemical scaffold that interacts strongly and specifically to one ABC drug transporter, has been challenging. Therefore, we are in search of novel chemical structures that can be developed and optimized into potent and selective modulator of ABC drug transporters. In this study, we showed for the first time that niclosamide, an antihelminthic agent, re-sensitizes the chemosensitivity in ABCG2-overexpressing MDR A549 Bec150 human lung cancer cells by directly inhibiting the function of ABCG2, as well as reducing protein expression level of ABCG2. Moreover, by performing high-throughput functional screening of large numbers of niclosamide derivatives, 5 derivatives with distinct chemical structures were identified as candidates to be developed into potent ABCG2 modulators for the future.
LI, HAI-CHEN, and 李海辰. "Synthesis of imidazole analogs as ABCB1/ABCG2 inhibitors and the study of their structure-activity relationship." Thesis, 2016. http://ndltd.ncl.edu.tw/handle/18307404638521153952.
Full text東海大學
化學系
104
During the treatment of cancer, multidrug resistance (MDR) is one of the most intractable problems. Multidrug resistance is often caused by the overexpression of ABC transporter (ATP-binding cassette transporter) ABCB1, ABCC1, ABCG2 which result in cancer drug to be exported out of the cell, rendering chemotherapy ineffective. As an effort to counteract this problem, we first took the substructure of tariquidar,2-benzamido-N-phenylbenzamide as the lead compound, and synthesize derivatives with different functional groups. While the synthesis of these derivatives were not as successful, we then synthesized compounds derived from three imidazole inhibitors screened at Professor Chung-Pu Wu’s laboratory, Chang Gung University. The ABC transporter protein inhibitory activity, showed that the nitrile substituting derivative demonstrated the best activity and when carboxyl group was esterified, the activity increased as well. The inhibitory activity of compounds showed that the hydrophobic group was preferred for ABCG2 inhibition. Neither electronic nor structure size of substituents appeared to affect the ABC transporter inhibition.
Luo, Shi Yu, and 羅仕瑜. "Human ABCB1 (P-glycoprotein/MDR1) and ABCG2 (BCRP/MXR) Mediate Resistance to Polo-like kinase 1 inhibitors." Thesis, 2014. http://ndltd.ncl.edu.tw/handle/48402034791397339617.
Full text長庚大學
生物醫學研究所
102
The overexpression of the serine/threonine specific polo-like kinase 1 (Plk1) has been detected in various types of cancer, and thus has fast become an attractive therapeutic target for cancer therapy. Plk1 inhibitors BI 2536, volasertib and GSK461364, were designed to selectively inhibit cancer cell proliferation by promoting G2/M cell cycle arrest at nanomolar concentrations. Unfortunately, alike most chemotherapeutic agents, the development of acquired resistance to Plk1 inhibitors is prone to present a significant therapeutic challenge. One of the most common mechanisms for acquired resistance in cancer chemotherapy is associated with the overexpression of ATP-binding cassette (ABC) transporters ABCB1, ABCC1 and ABCG2. Here, we discovered that in human cancer cells, the overexpression of ABCB1 and/or ABCG2 can lead to acquired resistance to three selective Plk1 inhibitors, BI 2536, volasertib and GSK461364. Moreover, these Plk1 inhibitors stimulate the ATPase activity of ABCB1 and ABCG2, as well as competitively inhibit the drug substrate transport mediated by ABCB1 and ABCG2. More significantly, the reduced chemosensitivity and Plk1 inhibitors-mediated G2/M cell cycle arrest in cancer cells overexpressing either ABCB1 or ABCG2 can be significantly restored in the presence of selective inhibitor of ABCB1 and ABCG2. Taken together, our findings indicate that in order to circumvent ABCB1 or ABCG2-mediated acquired resistance to Plk1 inhibitors, a combined regimen of Plk1 inhibitors and modulators or clinically active drugs that potently inhibit the function of ABC drug transporters, should be considered as a potential treatment strategy in the clinic.
Repeľová, Beáta. "Studium vlivu antiretrovirálních léčiv na transmembránový transport tenofoviru disoproxil fumarátu přes monovrstvu MDCKII-ABCB1 buněk." Master's thesis, 2017. http://www.nusl.cz/ntk/nusl-371009.
Full textManzella, Adam. "Structure dependent characterization of polychlorinated biphenyls (PCBs) and polybrominated diphenyl ethers (PBDEs) as inhibitors of the breast cancer resistance protein (ABCG2) transporter." 2007. http://proquest.umi.com/pqdweb?did=1425299851&sid=16&Fmt=2&clientId=39334&RQT=309&VName=PQD.
Full textTitle from PDF title page (viewed on Mar. 06, 2008) Available through UMI ProQuest Digital Dissertations. Thesis adviser: Olson, James. Includes bibliographical references.
Tuo, Wei Cherng, and 脫惟程. "A fluorescent cell-based high-throughput functional screening platform for the identification of drug substrates and inhibitors of multidrug resistance-associated ATP-binding cassette proteins ABCB1 and ABCG2." Thesis, 2014. http://ndltd.ncl.edu.tw/handle/434gng.
Full textChiang, Ming-Keng, and 江銘耿. "Predicting ABCG2 Inhibitor Binding Affinity Using Pharmacophore Ensemble/Support Vector Machine." Thesis, 2011. http://ndltd.ncl.edu.tw/handle/23232490754898853810.
Full text國立東華大學
化學系
99
ABCG2 (BCRP) is an ATP-dependent membrane transporter that plays a pivotal role in eliminating xenobiotics by active extrusion of xenobiotics from the cell. Because of this phenomenon which results in ABCG2 repels a variety of drugs and hence the resulting in increased efflux of chemotherapeutical agents and reduction of intracellular drug accumulation. Finally, the effect of cure is hard to attain. Accordingly, using inhibitor revers function and expression of ABCG2 on a cancer cell is the method of solving ABCG2 extrusion drugs An in silico model was derived to predict the inhibition of ABCG2 the newly invented pharmacophore ensemble/support vector machine (PhE/SVM) scheme based on the data compiled from the literature. The predictions by the PhE/SVM model are in good agreement with the experimental observed values for those molecules in the training set (n = 28, r2 = 0.87, q2 = 0.83, RMSE = 0.52, s = 0.25), test set (n = 31, r2 = 0.87, RMSE = 0.34, s = 0.23) and outlier set (n = 9, r2 = 0.84, RMSE = 0.47, s = 0.27). The generated PhE/SVM model also showed high accuracy when subjected to those validation criteria generally adopted to gauge the predictivity of a theoretical model. Thus, it can be asserted that this PhE/SVM model is an accurate, fast and robust model and can be employed to predict ABCG2 inhibitor binding affinity to facilitate drug discovery and drug development.
Chang, Yen Fu, and 張晏輔. "Investigating the interactions of Citarinostat, a histone deacetylase (HDAC) inhibitor, and PDGFR inhibitor 1, a platelet-derived growth factor (PDGFR) inhibitor, with ATP-binding cassette proteins ABCB1 and ABCG2." Thesis, 2019. http://ndltd.ncl.edu.tw/cgi-bin/gs32/gsweb.cgi/login?o=dnclcdr&s=id=%22107CGU05114088%22.&searchmode=basic.
Full textTseng, Pin Jung, and 曾品榕. "Investigating the interactions of MY-5445, a PDE5 inhibitor, and LY3023414, a PI3K/mTOR dual inhibitor, with MDR-linked ATP-binding cassette proteins ABCB1 and ABCG2." Thesis, 2019. http://ndltd.ncl.edu.tw/cgi-bin/gs32/gsweb.cgi/login?o=dnclcdr&s=id=%22107CGU05114084%22.&searchmode=basic.
Full textWang, Jyun Cheng, and 王俊程. "Investigating the chemosensitizing effect of TMP195, a HDAC class IIa inhibitor and avapritinib, a dual inhibitor of PDGFRα and KIT, in human multidrug resistant cancer cells overexpressing ABCB1 or ABCG2." Thesis, 2019. http://ndltd.ncl.edu.tw/cgi-bin/gs32/gsweb.cgi/login?o=dnclcdr&s=id=%22107CGU05114080%22.&searchmode=basic.
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