keyword
https://read.qxmd.com/read/34680166/reversal-of-abcg2-bcrp-mediated-multidrug-resistance-by-5-3-5-trihydroxy-3-6-7-4-tetramethoxyflavone-isolated-from-the-australian-desert-plant-eremophila-galeata-chinnock
#21
JOURNAL ARTICLE
Malene J Petersen, Xamuel L Lund, Susan J Semple, Bevan Buirchell, Henrik Franzyk, Michael Gajhede, Kenneth T Kongstad, Jan Stenvang, Dan Staerk
Multidrug resistance (MDR) is a major challenge in cancer treatment, and the breast cancer resistance protein (BCRP) is an important target in the search for new MDR-reversing drugs. With the aim of discovering new potential BCRP inhibitors, the crude extract of leaves of Eremophila galeata , a plant endemic to Australia, was investigated for inhibitory activity of parental (HT29par ) as well as BCRP-overexpressing HT29 colon cancer cells resistant to the chemotherapeutic SN-38 (i.e., HT29SN38 cells). This identified a fraction, eluted with 40% acetonitrile on a solid-phase extraction column, which showed weak growth-inhibitory activity on HT29SN38 cells when administered alone, but exhibited concentration-dependent growth inhibition when administered in combination with SN-38...
October 18, 2021: Biomolecules
https://read.qxmd.com/read/34643455/a-systems-level-analysis-of-bile-acids-effects-on-rat-colon-epithelial-cells
#22
JOURNAL ARTICLE
Jonathan Yde, Qi Wu, Johan Borg, Robert A Fenton, Hanne Bjerregaard Moeller
Bile acid diarrhoea is a chronic condition caused by increased delivery of bile acids to the colon. The underlying mechanisms remain to be elucidated. To investigate genes involved in bile acid diarrhoea, systems-level analyses were employed on a rat bile acid diarrhoea model. Twelve male Wistar Munich rats, housed in metabolic cages, were fed either control or bile acid-mixed (1% w/w) diets for ten days. Food intake, water intake, urine volume, bodyweight and faecal output were monitored daily. After euthanasia, colonic epithelial cells were isolated using calcium-chelation and processed for systems-level analyses, i...
October 13, 2021: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://read.qxmd.com/read/34572902/vkng-1-antagonizes-abcg2-mediated-multidrug-resistance-via-p-akt-and-bcl-2-pathway-in-colon-cancer-in-vitro-and-in-vivo-study
#23
JOURNAL ARTICLE
Silpa Narayanan, Ying-Fang Fan, Nehaben A Gujarati, Qiu-Xu Teng, Jing-Quan Wang, Chao-Yun Cai, Yuqi Yang, Anirudh J Chintalapati, Yixiong Lei, Vijaya L Korlipara, Zhe-Sheng Chen
The emergence of multidrug resistance (MDR) to chemotherapeutic drugs is a major problem in the therapy of cancer. Knowledge of the mechanisms of drug resistance in cancer is necessary for developing efficacious therapies. ATP-binding cassette (ABC) transporters are transmembrane proteins that efflux chemotherapeutic drugs from cancer cells, thereby producing MDR. Our research efforts have led to the discovery of VKNG-1, a compound that selectively inhibits the ABCG2 transporter and reverses resistanctabe to standard anticancer drugs both in vitro and in vivo...
September 17, 2021: Cancers
https://read.qxmd.com/read/34353271/explorations-of-atp-binding-cassette-transporters-and-apoptosis-signal-pathways-of-2-hydroxyanthraquinone-substituted-cyclotriphosphazenes-in-mcf-7-and-dld-1-cell-lines
#24
JOURNAL ARTICLE
Burak Yazgan, Seda Mesci, Nagihan Bayık, Maşuk Akşahin, Gönül Yenilmez Çiftçi, Tuba Yıldırım
BACKGROUND: As a class with biological properties, such as anti-cancer, anti-bacterial, anti-HIV, and various physical effects, phosphazene derivatives constitute the most striking part of inorganic compounds. Anthraquinones, on the other hand, are a broad family of compounds with a wide variety of biological properties; the biologically active anthraquinones have been used as valuable tool compounds for biochemical and pharmacological research. OBJECTIVE: In this study, we aimed to investigate the effect of the anthraquinone substituted cyclotriphosphazene compounds on apoptosis and drug resistance in MCF-7 and DLD-1 cells...
August 5, 2021: Anti-cancer Agents in Medicinal Chemistry
https://read.qxmd.com/read/34205602/the-potential-role-of-sildenafil-in-cancer-management-through-epr-augmentation
#25
REVIEW
Mohamed Haider, Amr Elsherbeny, Valeria Pittalà, Antonino N Fallica, Maha Ali Alghamdi, Khaled Greish
Enhanced permeation retention (EPR) was a significant milestone discovery by Maeda et al. paving the path for the emerging field of nanomedicine to become a powerful tool in the fight against cancer. Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE-5) used for the treatment of erectile dysfunction (ED) through the relaxation of smooth muscles and the modulation of vascular endothelial permeability. Overexpression of PDE-5 has been reported in lung, colon, metastatic breast cancers, and bladder squamous carcinoma...
June 21, 2021: Journal of Personalized Medicine
https://read.qxmd.com/read/33671108/the-novel-benzamide-derivative-vkng-2-restores-the-efficacy-of-chemotherapeutic-drugs-in-colon-cancer-cell-lines-by-inhibiting-the-abcg2-transporter
#26
JOURNAL ARTICLE
Silpa Narayanan, Nehaben A Gujarati, Jing-Quan Wang, Zhuo-Xun Wu, Jagadish Koya, Qingbin Cui, Vijaya L Korlipara, Charles R Ashby, Zhe-Sheng Chen
The overexpression of ATP-binding cassette transporter, ABCG2, plays an important role in mediating multidrug resistance (MDR) in certain types of cancer cells. ABCG2-mediated MDR can significantly attenuate or abrogate the efficacy of anticancer drugs by increasing their efflux from cancer cells. In this study, we determined the efficacy of the novel benzamide derivative, VKNG-2, to overcome MDR due to the overexpression of the ABCG2 transporter in the colon cancer cell line, S1-M1-80. In vitro , 5 μM of VKNG-2 reversed the resistance of S1-M1-80 cell line to mitoxantrone (70-fold increase in efficacy) or SN-38 (112-fold increase in efficacy)...
February 28, 2021: International Journal of Molecular Sciences
https://read.qxmd.com/read/33170084/cancer-stem-cell-markers-in-relation-to-patient-survival-outcomes-lessons-for-integrative-diagnostics-and-next-generation-anticancer-drug-development
#27
JOURNAL ARTICLE
Kevin Dzobo, Chelene Ganz, Nicholas Ekow Thomford, Dimakatso Alice Senthebane
Solid tumors display a complex biology that requires a multipronged treatment strategy. Most anticancer interventions, including chemotherapy, are currently unable to prevent treatment resistance and relapse. In general, therapeutics target cancer cells and overlook the tumor microenvironment (TME) and the presence of cancer stem cells (CSCs) with self-renewal and tumorigenic abilities. CSCs have been postulated to play key roles in tumor initiation, progression, therapy resistance, and metastasis. Hence, CSC markers have been suggested as diagnostics to forecast cancer prognosis as well as molecular targets for new-generation cancer treatments, especially in resistant disease...
November 10, 2020: Omics: a Journal of Integrative Biology
https://read.qxmd.com/read/33158067/poziotinib-inhibits-the-efflux-activity-of-the-abcb1-and-abcg2-transporters-and-the-expression-of-the-abcg2-transporter-protein-in-multidrug-resistant-colon-cancer-cells
#28
JOURNAL ARTICLE
Yongchao Zhang, Zhuo-Xun Wu, Yuqi Yang, Jing-Quan Wang, Jun Li, Zoey Sun, Qiu-Xu Teng, Charles R Ashby, Dong-Hua Yang
Colorectal cancer (CRC) is a leading cause of cancer deaths in the United States. Currently, chemotherapy is a first-line treatment for CRC. However, one major drawback of chemotherapy is the emergence of multidrug resistance (MDR). It has been well-established that the overexpression of the ABCB1 and/or ABCG2 transporters can produce MDR in cancer cells. In this study, we report that in vitro, poziotinib can antagonize both ABCB1- and ABCG2-mediated MDR at 0.1-0.6 μM in the human colon cancer cell lines, SW620/Ad300 and S1-M1-80...
November 4, 2020: Cancers
https://read.qxmd.com/read/32818544/golph3-inhibition-reverses-oxaliplatin-resistance-of-colon-cancer-cells-via-suppression-of-pi3k-akt-mtor-pathway
#29
JOURNAL ARTICLE
Tao Yu, Qi An, Xiang-Long Cao, Hua Yang, Jian Cui, Zi-Jian Li, Gang Xiao
OBJECTIVE: To explore whether GOLPH3 regulated oxaliplatin (L-OHP) resistance of colon cancer cells via PI3K/AKT/mTOR pathway. METHODS: HCT116/L-OHP cells were divided into Blank, Control/GOLPH3 shRNA, BEZ235 (a PI3K/AKT/mTOR inhibitor), and GOLPH3 + BEZ235 groups followed by the detection with MTT, soft agar colony formation, flow cytometry and TUNEL assays. Mice bearing HCT116/L-OHP xenografts were randomized into Control, L-OHP, NC/GOLPH3 shRNA, L-OHP + NC/GOLPH3 shRNA groups...
August 17, 2020: Life Sciences
https://read.qxmd.com/read/32697585/spatiotemporally-targeted-nanomedicine-overcomes-hypoxia-induced-drug-resistance-of-tumor-cells-after-disrupting-neovasculature
#30
JOURNAL ARTICLE
Jinjin Chen, Zhongyu Jiang, Weiguo Xu, Tianmeng Sun, Xiuli Zhuang, Jianxun Ding, Xuesi Chen
Vascular disrupting agents (VDAs) are emerging anticancer agents, which show rising demand for combination with cytostatic drugs (CSDs), owing to inadequate tumor inhibition when applied singly. Nevertheless, the combination remains a challenge due to the different working sites of VDAs and CSDs and hypoxia-induced drug resistance after disrupting neovasculature by VDAs. Herein, we developed a shell-stacked nanoparticle (SNP) for coencapsulation of a VDA combretastatin A-4 phosphate (CA4P) and a proteasome inhibitor bortezomib (BTZ)...
August 12, 2020: Nano Letters
https://read.qxmd.com/read/32560222/preclinical-evaluation-of-the-novel-small-molecule-msi-n1014-for-treating-drug-resistant-colon-cancer-via-the-lgr5-%C3%AE-catenin-mir-142-3p-network-and-reducing-cancer-associated-fibroblast-transformation
#31
JOURNAL ARTICLE
Vijesh Kumar Yadav, Yan-Jiun Huang, Thomashire Anita George, Po-Li Wei, Maryam Rachmawati Sumitra, Ching-Liang Ho, Tzu-Hao Chang, Alexander T H Wu, Hsu-Shan Huang
Colorectal cancer represents one of the most prevalent malignancies globally, with an estimated 140,000 new cases in the United States alone in 2019. Despite advancements in interventions, drug resistance occurs in virtually all patients diagnosed with late stages of colon cancer. Amplified epidermal growth factor receptor (EGFR) signaling is one of the most prevalent oncogenic drivers in patients and induces increased Janus kinase (JAK)/signal transduction and activator of transcription (STAT) and β-catenin functions, all of which facilitate disease progression...
June 16, 2020: Cancers
https://read.qxmd.com/read/32326511/an-explorative-analysis-of-abcg2-top-1-mrna-expression-as-a-biomarker-test-for-folfiri-treatment-in-stage-iii-colon-cancer-patients-results-from-retrospective-analyses-of-the-petacc-3-trial
#32
JOURNAL ARTICLE
Jan Stenvang, Eva Budinská, Eric van Cutsem, Fred Bosman, Vlad Popovici, Nils Brünner
Biomarker-guided treatment for patients with colon cancer is needed. We tested ABCG2 and topoisomerase 1 (TOP1) mRNA expression as predictive biomarkers for irinotecan benefit in the PETACC-3 patient cohort. The present study included 580 patients with mRNA expression data from Stage III colon cancer samples from the PETACC-3 study, which randomized the patients to Fluorouracil/leucovorin (5FUL) +/- irinotecan. The primary end-points were recurrence free survival (RFS) and overall survival (OS). Patients were divided into one group with high ABCG2 expression (above median) and low TOP-1 expression (below 75 percentile) ("resistant") ( n = 216) and another group including all other combinations of these two genes ("sensitive") ( n = 364)...
April 15, 2020: Cancers
https://read.qxmd.com/read/32143347/the-pyrazolo-3-4-d-pyrimidine-derivative-sco-201-reverses-multidrug-resistance-mediated-by-abcg2-bcrp
#33
JOURNAL ARTICLE
Sophie E B Ambjørner, Michael Wiese, Sebastian Christoph Köhler, Joen Svindt, Xamuel Loft Lund, Michael Gajhede, Lasse Saaby, Birger Brodin, Steffen Rump, Henning Weigt, Nils Brünner, Jan Stenvang
ATP-binding cassette (ABC) transporters, such as breast cancer resistance protein (BCRP), are key players in resistance to multiple anti-cancer drugs, leading to cancer treatment failure and cancer-related death. Currently, there are no clinically approved drugs for reversal of cancer drug resistance caused by ABC transporters. This study investigated if a novel drug candidate, SCO-201, could inhibit BCRP and reverse BCRP-mediated drug resistance. We applied in vitro cell viability assays in SN-38 (7-Ethyl-10-hydroxycamptothecin)-resistant colon cancer cells and in non-cancer cells with ectopic expression of BCRP...
March 4, 2020: Cells
https://read.qxmd.com/read/32061752/ire1%C3%AE-targeting-downregulates-abc-transporters-and-overcomes-drug-resistance-of-colon-cancer-cells
#34
JOURNAL ARTICLE
Qiang Gao, Xiu-Xiu Li, Yi-Ming Xu, Jin-Zhao Zhang, Shi-di Rong, Yan-Qing Qin, Jing Fang
Drug resistance is a big problem in cancer treatment and one of the most prominent mechanisms underlain is overexpression of ATP-binding cassette (ABC) transporters, particularly ABCB1, ABCC1 and ABCG2. Inhibition of ABC transporters is an important approach to overcome drug resistance. The inositol-requiring enzyme 1α (IRE1α), an arm of unfolded protein response (UPR), splices XBP1 mRNA to generate an active transcription factor XBP1s. UPR is implicated in drug resistance. However, the underlying mechanism is unclear...
April 28, 2020: Cancer Letters
https://read.qxmd.com/read/32044957/overexpressing-microrna-34a-overcomes-abcg2-mediated-drug-resistance-to-5-fu-in-side-population-cells-from-colon-cancer-via-suppressing-dll1
#35
JOURNAL ARTICLE
Zheng-Yuan Xie, Fen-Fen Wang, Zhi-Hua Xiao, Si-Fu Liu, Sheng-Lan Tang, Yue-Liang Lai
Colon cancer side population (SP) cells are a small subset of cancer cells that have cancer stemness capacity and enhanced drug resistance. ABCG2 is a multidrug resistance-related protein in SP cells, and has been demonstrated to be regulated by Notch signaling pathway. Recently, microRNAs are reported to play a critical role in SP cell fate. However, their role in ABCG2-mediated drug resistance in colon cancer SP cells remains unclear. In the current study, the different expressions of miR-552, miR-611, miR-34a, and miR-5000-3p were compared within SP and non-SP cells, which were separated from human colon cancer cell lines (SW480 and LoVo)...
February 11, 2020: Journal of Biochemistry
https://read.qxmd.com/read/31641961/integrin-egfr-interaction-regulates-anoikis-resistance-in-colon-cancer-cells
#36
JOURNAL ARTICLE
Deblina Guha, Taniya Saha, Sayantan Bose, Sreeparna Chakraborty, Subhanki Dhar, Poulami Khan, Arghya Adhikary, Tanya Das, Gaurisankar Sa
Anoikis resistance is an essential property of cancer cells that allow the extra-cellular matrix-detached cells to survive in a suspended state in body fluid in order to metastasize and invade to distant organs. It is known that integrins play an important role in anoikis resistance, but detailed mechanisms are not well understood. Here we report that highly metastatic colon cancer cells showed a higher degree of anoikis resistance than the normal intestinal epithelial cells. These anoikis-resistant cancer cells express high-levels of integrin-α2, β1, and activated EGFR in the anchorage-independent state than the anchorage-dependent state...
December 2019: Apoptosis: An International Journal on Programmed Cell Death
https://read.qxmd.com/read/31621972/microrna-29b-inhibits-cell-growth-and-promotes-sensitivity-to-oxaliplatin-in-colon-cancer-by-targeting-folr1
#37
JOURNAL ARTICLE
Qiang Fu, Jindai Zhang, Gaofeng Huang, Yonglei Zhang, Minghai Zhao, Yongchao Zhang, Jianguo Xie
The present study was aimed to explore the functional role of microRNA (miR)-29b in colon cancer, as well as underlying mechanisms. Expressions of miR-29b and folate receptor 1 (FOLR1) were measured in both human colon tumor samples and cell lines. Colon cancer cell lines SW480 and SW620 were transfected with miR-29b mimic, antisense oligonucleotides (ASO)-miR-29b, small interfering (siRNA) against FOLR1 (si-FOLR1), or corresponding negative controls (NCs), and then were incubated with or without oxaliplatin (L-OHP)...
October 17, 2019: BioFactors
https://read.qxmd.com/read/31211831/intestinal-inflammation-modulates-the-epithelial-response-to-butyrate-in-patients-with-inflammatory-bowel-disease
#38
JOURNAL ARTICLE
Elena Ferrer-Picón, Isabella Dotti, Ana M Corraliza, Aida Mayorgas, Miriam Esteller, José Carlos Perales, Elena Ricart, Maria C Masamunt, Anna Carrasco, Eva Tristán, Maria Esteve, Azucena Salas
BACKGROUND: Butyrate-producing gut bacteria are reduced in patients with active inflammatory bowel disease (IBD), supporting the hypothesis that butyrate supplementation may be beneficial in this setting. Nonetheless, earlier studies suggest that the oxidation of butyrate in IBD patients is altered. We propose that inflammation may decrease epithelial butyrate consumption. METHODS: Non-IBD controls and IBD patients were recruited for the study. Stool samples were used for short-chain fatty acid and bacterial butyryl CoA:acetate CoA-transferase quantification...
January 1, 2020: Inflammatory Bowel Diseases
https://read.qxmd.com/read/31207436/the-reference-liver-abc-and-slc-drug-transporters-in-healthy-donor-and-metastatic-livers
#39
JOURNAL ARTICLE
Mateusz Kurzawski, Sylwia Szeląg-Pieniek, Joanna Łapczuk-Romańska, Maciej Wrzesiński, Jerzy Sieńko, Stefan Oswald, Marek Droździk
BACKGROUND: Analysis of results and conclusions in studies dedicated to pathology of the liver are usually based on comparison of pathological liver specimens and control/reference (considered as healthy) tissues. There are two main sources of the control liver samples used as the reference livers, i.e. deceased organ donor livers and non-tumorous tissue from metastatic livers, which are also applied for drug transporter investigations. However, no information has yet been published on drug transporters in these two major types of reference livers...
April 9, 2019: Pharmacological Reports: PR
https://read.qxmd.com/read/31186779/prognostic-implication-of-abc-transporters-and-cancer-stem-cell-markers-in-patients-with-stage-iii-colon-cancer-receiving-adjuvant-folfox-4-chemotherapy
#40
JOURNAL ARTICLE
Song-Hee Han, Jin Won Kim, Milim Kim, Jee Hyun Kim, Keun-Wook Lee, Bo-Hyung Kim, Heung-Kwon Oh, Duck-Woo Kim, Sung-Bum Kang, Hyunchul Kim, Eun Shin
Cancer stem cell (CSC) and ATP-binding cassette (ABC) transporters are associated with treatment resistance and outcomes of patients with cancer. The present study investigated the prognostic implications of pre-therapeutic expression of ABC transporters and CSC markers in patients with colon cancer (CC) who received adjuvant 5-fluorouracil, leucovorin and oxaliplatin combination therapy (FOLFOX-4). The immunohistochemical expression of 3 ABC transporters, including ABC subfamily C member 2 (ABCC2), ABCC3 and ABC subfamily G member 2 (ABCG2), and 3 CSC markers, including sex determining region Y-box 2 (SOX2), leucine-rich repeat-containing G protein-coupled receptor 5 and aldehyde dehydrogenase 1, were determined in 164 CC tissues from patients with stage III CC, who underwent postoperative FOLFOX-4 chemotherapy...
June 2019: Oncology Letters
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