Academic literature on the topic 'ABCG2 inhibitors'
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Journal articles on the topic "ABCG2 inhibitors"
Henrich, Curtis J., Heidi R. Bokesch, Michael Dean, Susan E. Bates, Robert W. Robey, Ekaterina I. Goncharova, Jennifer A. Wilson, and James B. McMahon. "A High-Throughput Cell-Based Assay for Inhibitors of ABCG2 Activity." Journal of Biomolecular Screening 11, no. 2 (December 16, 2005): 176–83. http://dx.doi.org/10.1177/1087057105284576.
Full textKokubo, Shoji, Shinobu Ohnuma, Megumi Murakami, Haruhisa Kikuchi, Shota Funayama, Hideyuki Suzuki, Taiki Kajiwara, et al. "A Phenylfurocoumarin Derivative Reverses ABCG2-Mediated Multidrug Resistance In Vitro and In Vivo." International Journal of Molecular Sciences 22, no. 22 (November 19, 2021): 12502. http://dx.doi.org/10.3390/ijms222212502.
Full textNatarajan, Karthika, Jasjeet Bhullar, Suneet Shukla, Mehmet Burcu, Suresh V. Ambudkar, and Maria R. Baer. "The Pim Kinase Inhibitor SGI-1776 Chemosensitizes Multidrug Resistant Cells by Both Inhibiting Drug Transport by ABCB1 and ABCG2 and Decreasing ABCB1 and ABCG2 Surface Expression On Cells That Overexpress Pim-1." Blood 120, no. 21 (November 16, 2012): 2462. http://dx.doi.org/10.1182/blood.v120.21.2462.2462.
Full textCurran, Sean, Toni-Marie Achilli, Elizabeth Leary, Benjamin T. Wilks, Marguerite M. Vantangoli, Kim Boekelheide, and Jeffrey R. Morgan. "A 3D spheroid system to evaluate inhibitors of the ABCG2 transporter in drug uptake and penetration." TECHNOLOGY 03, no. 01 (March 2015): 54–63. http://dx.doi.org/10.1142/s2339547815500028.
Full textBarrera, Borja, Jon A. Otero, Estefanía Egido, Julio G. Prieto, Anna Seelig, Ana I. Álvarez, and Gracia Merino. "The Anthelmintic Triclabendazole and Its Metabolites Inhibit the Membrane Transporter ABCG2/BCRP." Antimicrobial Agents and Chemotherapy 56, no. 7 (April 16, 2012): 3535–43. http://dx.doi.org/10.1128/aac.06345-11.
Full textWang, Jing-Quan, Jonathan Y. Li, Qiu-Xu Teng, Zi-Ning Lei, Ning Ji, Qingbin Cui, Leli Zeng, Yihang Pan, Dong-Hua Yang, and Zhe-Sheng Chen. "Venetoclax, a BCL-2 Inhibitor, Enhances the Efficacy of Chemotherapeutic Agents in Wild-Type ABCG2-Overexpression-Mediated MDR Cancer Cells." Cancers 12, no. 2 (February 18, 2020): 466. http://dx.doi.org/10.3390/cancers12020466.
Full textStockmann, Philipp, Lydia Kuhnert, Wencke Leinung, Cathleen Lakoma, Birte Scholz, Svetlana Paskas, Sanja Mijatović, Danijela Maksimović-Ivanić, Walther Honscha, and Evamarie Hey-Hawkins. "The More the Better—Investigation of Polymethoxylated N-Carboranyl Quinazolines as Novel Hybrid Breast Cancer Resistance Protein Inhibitors." Pharmaceutics 15, no. 1 (January 10, 2023): 241. http://dx.doi.org/10.3390/pharmaceutics15010241.
Full textInoue, Yutaka, Takashi Morita, Mari Onozuka, Ken-ichi Saito, Kazumi Sano, Kazuhiko Hanada, Masami Kondo, et al. "Impact of Q141K on the Transport of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors by ABCG2." Cells 8, no. 7 (July 23, 2019): 763. http://dx.doi.org/10.3390/cells8070763.
Full textDi Micco, Simone, Veronica Di Sarno, Martina Rossi, Vincenzo Vestuto, Takumi Konno, Sara Novi, Mario Felice Tecce, et al. "In Silico Identification and In Vitro Evaluation of New ABCG2 Transporter Inhibitors as Potential Anticancer Agents." International Journal of Molecular Sciences 24, no. 1 (December 31, 2022): 725. http://dx.doi.org/10.3390/ijms24010725.
Full textWu, Zhuo-Xun, Yuqi Yang, Qiu-Xu Teng, Jing-Quan Wang, Zi-Ning Lei, Jing-Qiu Wang, Sabrina Lusvarghi, Suresh V. Ambudkar, Dong-Hua Yang, and Zhe-Sheng Chen. "Tivantinib, A c-Met Inhibitor in Clinical Trials, Is Susceptible to ABCG2-Mediated Drug Resistance." Cancers 12, no. 1 (January 12, 2020): 186. http://dx.doi.org/10.3390/cancers12010186.
Full textDissertations / Theses on the topic "ABCG2 inhibitors"
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 textBooks on the topic "ABCG2 inhibitors"
Merriman, Tony R. The genetic basis of gout. Oxford University Press, 2016. http://dx.doi.org/10.1093/med/9780199668847.003.0040.
Full textConference papers on the topic "ABCG2 inhibitors"
Kokubo, Shoji, Shinobu Ohnuma, Hideaki Karasawa, Akihiro Yamamura, Hideyuki Suzuki, Megumi Murakami, Norihiko Sugisawa, et al. "Abstract 25: Identifying new inhibitors of ABCG2 by high-throughput screening." In Proceedings: AACR Annual Meeting 2019; March 29-April 3, 2019; Atlanta, GA. American Association for Cancer Research, 2019. http://dx.doi.org/10.1158/1538-7445.sabcs18-25.
Full textKokubo, Shoji, Shinobu Ohnuma, Hideaki Karasawa, Akihiro Yamamura, Hideyuki Suzuki, Megumi Murakami, Norihiko Sugisawa, et al. "Abstract 25: Identifying new inhibitors of ABCG2 by high-throughput screening." In Proceedings: AACR Annual Meeting 2019; March 29-April 3, 2019; Atlanta, GA. American Association for Cancer Research, 2019. http://dx.doi.org/10.1158/1538-7445.am2019-25.
Full textMohamad Pauzi, Abrar. "Abstract 4229: ATP-binding cassette transporter ABCG2/BCRP inhibition sensitizes CD133+ cells to MEK/BRAF inhibitors." In Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1538-7445.am2015-4229.
Full textBouraiou, Abdelmalek, Glaucio Valdameri, Isadora Zanzarini, Esma Lamera, Sofiane Bouacida, Ingrid Zattoni, Diogo Kita, Zouhair Bouaziz, Vivian Moure, and Marc Le Borgne. "Design, synthesis, X-ray structure and evaluation of functionalized hexacyclic carbazoles as new inhibitors of ABCG2 transporter." In 5th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/ecmc2019-06343.
Full textFan, Lin, Mark C. de Gooijer, Levi Buil, Nienke A. de Vries, Jos H. Beijnen, and Olaf van Tellingen. "Abstract LB-301: The impact of Abcb1 and Abcg2 on the brain penetration of PI3K-mTOR inhibitors." In Proceedings: AACR 101st Annual Meeting 2010‐‐ Apr 17‐21, 2010; Washington, DC. American Association for Cancer Research, 2010. http://dx.doi.org/10.1158/1538-7445.am10-lb-301.
Full textSodani, Kamlesh S., Amit K. Tiwari, Satyakam Singh, Atish Patel, Zhijie Xiao, Junjiang Chen, Yueli Sun, Tanaji T. Talele, and Zhe-Sheng Chen. "Abstract 777: GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance." In Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-777.
Full textSkoglund, Karin, Samuel Boiso Moreno, Kourosh Lotfi, Jan-Ingvar Jönsson, and Henrik Gréen. "Abstract 5596: Altered efficacy of tyrosine kinase inhibitors in chronic myeloid leukemia cells expressing wild type or polymorphic ABCG2." In Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-5596.
Full textWu, Chung-Pu, Hong-May Sim, and Suresh V. Ambudkar. "Abstract 766: Human ABCB1 and ABCG2 confer acquired resistance to Polo-like kinase 1 inhibitors, BI 2536, volasertib and GSK641364." In Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. American Association for Cancer Research, 2014. http://dx.doi.org/10.1158/1538-7445.am2014-766.
Full textBasseville, Agnes, Akina Tamaki, Caterina Ierano, Yvona Ward, Robert W. Robey, Ramanujan Hegde, and Susan E. Bates. "Abstract 2610: Histone deacetylase inhibitors mediate pharmacological rescue of the ABCG2 Q141K variant: Potential for therapeutics in cancer and gout." In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-2610.
Full textPatel, Atish S. "Abstract 760: Suppression of ABCG2 mediated MDRin vitroandin vivoby a novel inhibitor of ABCG2 transport." In Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. American Association for Cancer Research, 2014. http://dx.doi.org/10.1158/1538-7445.am2014-760.
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