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https://www.readbyqxmd.com/read/28637014/a-combination-of-valproic-acid-sodium-salt-chir99021-e-616452-tranylcypromine-and-3-deazaneplanocin-a-causes-stem-cell-like-characteristics-in-cancer-cells
#1
Shuang Sha, Yuanfen Zhai, Chengzhao Lin, Heyong Wang, Qing Chang, Shuang Song, Mingqiang Ren, Gentao Liu
Many studies are based on the hypothesis that recurrence and drug resistance in lung carcinoma are due to a subpopulation of cancer stem-like cells (CSLCs) in solid tumors. Therefore it is crucial to screen for and recognize lung CSLCs. In this study, we stimulated non-small cell lung cancer (NSCLC) A549 cells to display stem cell-like characteristics using a combination of five small molecule compounds. The putative A549 stem cells activated an important CSLC marker, CD133 protein, as well multiple CSLC-related genes including ATP-binding cassette transporter G2 (ABCG2), C-X-C chemokine receptor type 4 (CXCR4), NESTIN, and BMI1...
June 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28637009/jagged-2-jag2-enhances-tumorigenicity-and-chemoresistance-of-colorectal-cancer-cells
#2
Vivek Vaish, Joohwee Kim, Minsub Shim
Colorectal cancer (CRC) is one of the leading causes of cancer-related mortality. Recent studies have stated that NOTCH signaling plays an important role in the development and progression of CRC. However, the role of Jagged-2 (JAG2), one of the NOTCH ligands, has not been delineated in colorectal tumorigenesis and drug resistance. In the present study, we have examined the impact of targeting JAG2 on CRC cells. Among all the members of NOTCH ligands, only the expression of JAG2 was found up-regulated in the intestinal tumors of ApcMin/+ mice as compared to the nearby normal mucosa...
June 5, 2017: Oncotarget
https://www.readbyqxmd.com/read/28637008/cytotoxic-profiling-of-artesunic-and-betulinic-acids-and-their-synthetic-hybrid-compound-on-neurons-and-gliomas
#3
Annemarie Ackermann, Aysun Çapcı Karagöz, Ali Ghoochani, Michael Buchfelder, Ilker Eyüpoglu, Svetlana B Tsogoeva, Nicolai Savaskan
Gliomas are brain-born tumors with devastating impact on their brain microenvironment. Novel approaches employ multiple combinations of chemical compounds in synthetic hybrid molecules to target malignant tumors. Here, we report on the chemical hybridization approach exemplified by artesunic acid (ARTA) and naturally occurring triterpene betulinic acid (BETA). Artemisinin derived semisynthetic compound artesunic acid (ARTA) and naturally occurring triterpene BETA were used to synthetically couple to the hybrid compound termed 212A...
June 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28637003/structural-recognition-of-tubulysin-b-derivatives-by-multidrug-resistance-efflux-transporters-in-human-cancer-cells
#4
Michal Stark, Yehuda G Assaraf
Multidrug resistance (MDR) is a major hindrance to curative chemotherapy of various human malignancies. Hence, novel chemotherapeutics must be evaluated for their recognition by MDR efflux transporters. Herein we explored the cytotoxic activity of synthetic tubulysin B (Tub-B, EC1009) derivatives (Tub-B-hydrazide/EC0347 and Tub-B bis-ether/EC1820), and their recognition by the MDR efflux transporters P-glycoprotein 1 (P-gp), multidrug resistance-associated protein 1 (MRP1) and breast cancer resistance protein (BCRP)...
June 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28636554/proton-pump-inhibitors-increase-the-chemosensitivity-of-patients-with-advanced-colorectal-cancer
#5
Xiaoyu Wang, Chun Liu, Jiaqi Wang, Yue Fan, Zhenghua Wang, Yuanyuan Wang
Changes in pH can alter the uptake of chemotherapy drugs. Proton pump inhibitors (PPIs) may therefore increase the chemosensitivity of cancer cells and cytotoxicity of chemotherapeutic drugs by increasing their uptake. We investigated the chemosensitizing potential of PPIs in colorectal cancer (CRC). Our in vitro data show that the PPI pantoprazole increases the chemosensitivity of CRC HT29 and RKO cells to fluorouracil (5-FU). Our in vivo data demonstrate that pantoprazole also increases the ability of 5-FU to inhibit CRC tumor growth in mice...
June 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28636454/anticancer-potential-of-sanguinarine-for-various-human-malignancies
#6
Iman W Achkar, Fatima Mraiche, Ramzi M Mohammad, Shahab Uddin
Sanguinarine (Sang) - a benzophenanthridine alkaloid extracted from Sanguinaria canadensis - exhibits antioxidant, anti-inflammatory, proapoptotic and growth inhibitory activities on tumor cells of various cancer types as established by in vivo and in vitro studies. Although the underlying mechanism of Sang antitumor activity is yet to be fully elucidated, Sang has displayed multiple biological effects, which remain to suggest its possible use in plant-derived treatments of human malignancies. This review covers the anticancer abilities of Sang including inhibition of aberrantly activated signal transduction pathways, induction of cell death and inhibition of cancer cell proliferation...
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28636308/redox-sensitive-nanoscale-coordination-polymers-for-drug-delivery-and-cancer-theranostics
#7
Jiayue Zhao, Yu Yang, Xiao Han, Chao Liang, Jingjing Liu, Xuejiao Song, Zili Ge, Zhuang Liu
Nanoscale coordination polymers (NCPs) with inherent biodegradability, chemical diversities, and porous structures, are a promising class of nanomaterials in the nanomedicine field. Herein, a unique type of redox sensitive NCPs is constructed with manganese ions (Mn2+) and dithiodiglycolic acid as the disulfide (SS) containing organic bridging ligand. The obtained Mn-SS NCPs with mesoporous structure could be efficiently loaded with doxorubicin (DOX), a chemotherapeutics. The yielded Mn-SS/DOX nanoparticles are coated with a layer of polydopamine (PDA) and then modified by polyethylene glycol (PEG)...
June 21, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28635648/deoxyelephantopin-and-isodeoxyelephantopin-as-potential-anticancer-agents-with-effects-on-multiple-signaling-pathways
#8
REVIEW
Tahir Mehmood, Amara Maryam, Hamed A Ghramh, Muhammad Khan, Tonghui Ma
Cancer is the 2nd leading cause of death worldwide. The development of drugs to target only one specific signaling pathway has limited therapeutic success. Developing chemotherapeutics to target multiple signaling pathways has emerged as a new prototype for cancer treatment. Deoxyelephantopin (DET) and isodeoxyelephantopin (IDET) are sesquiterpene lactone components of "Elephantopus scaber and Elephantopus carolinianus", traditional Chinese medicinal herbs that have long been used as folk medicines to treat liver diseases, diabetes, diuresis, bronchitis, fever, diarrhea, dysentery, cancer, and inflammation...
June 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28635172/doxorubicin-kinetics-and-effects-on-lung-cancer-cell-lines-using-in-vitro-raman-micro-spectroscopy-binding-signatures-drug-resistance-and-dna-repair
#9
Zeineb Farhane, Franck Bonnier, Orla Howe, Alan Casey, Hugh J Byrne
Raman micro-spectroscopy is a non-invasive analytical tool, whose potential in cellular analysis and monitoring drug mechanisms of action has already been demonstrated, and which can potentially be used in pre-clinical and clinical applications for the prediction of chemotherapeutic efficacy. To further investigate such potential clinical application, it is important to demonstrate its capability to differentiate drug mechanisms of action and cellular resistances. Using the example of Doxorubicin (DOX), in this study, it was used to probe the cellular uptake, signatures of chemical binding and subsequent cellular responses, of the chemotherapeutic drug in two lung cancer cell lines, A549 and Calu-1...
June 21, 2017: Journal of Biophotonics
https://www.readbyqxmd.com/read/28634291/rhodium-metalloinsertor-binding-generates-a-lesion-with-selective-cytotoxicity-for-mismatch-repair-deficient-cells
#10
Julie M Bailis, Alyson G Weidmann, Natalie F Mariano, Jacqueline K Barton
The DNA mismatch repair (MMR) pathway recognizes and repairs errors in base pairing and acts to maintain genome stability. Cancers that have lost MMR function are common and comprise an important clinical subtype that is resistant to many standard of care chemotherapeutics such as cisplatin. We have identified a family of rhodium metalloinsertors that bind DNA mismatches with high specificity and are preferentially cytotoxic to MMR-deficient cells. Here, we characterize the cellular mechanism of action of the most potent and selective complex in this family, [Rh(chrysi)(phen)(PPO)](2+) (Rh-PPO)...
June 20, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28634229/akt-activation-by-ca2-calmodulin-dependent-protein-kinase-kinase-2-camkk2-in-ovarian-cancer-cells
#11
Angela M Gocher, Gissou Azabdaftari, Lindsey M Euscher, Shuhang Dai, Loukia G Karacosta, Thomas F Franke, Arthur M Edelman
Hyperactivation of Akt is associated with oncogenic changes in the growth, survival and chemoresistance of cancer cells. The PI3K/Phosphoinositide-dependent kinase (PDK) 1 pathway represents the canonical mechanism for phosphorylation of Akt at its primary activation site, Thr308. We observed that Ca2+/calmodulin (CaM)-dependent protein kinase kinase 2 (beta) (CaMKK2) is highly expressed in high-grade serous ovarian cancer and investigated its role in Akt activation in ovarian cancer (OVCa) cell lines (OVCAR-3, SKOV-3, Caov-3)...
June 20, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28633130/synthesis-screening-and-pro-apoptotic-activity-of-novel-acyl-spermidine-derivatives-on-human-cancer-cell-lines
#12
Syed Shoeb Razvi, Hany Choudhry, Said Salama Moselhy, Taha Abduallah Kumosani, Mohammed Nihal Hasan, Mazin A Zamzami, Khalid Omer Abualnaja, Abdulrahman Labeed Al-Malki, Mahmoud Alhosin, Tadao Asami
The polyamines putrescine, spermidine, and spermine are polycationic, alkyl polyamines which play a significant role in eukaryotic cell proliferation. The polyamine metabolism and function are dysregulated in tumor cells making them an attractive therapeutic target by employing polyamine analogs. These analogs have a high degree of similarity with the structure of polyamines but not with their function. Multidrug resistance is a major factor in the failure of many chemotherapeutic drugs which necessitates further research and exploration of better novel alternatives...
June 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28632865/effect-of-first-line-chemotherapy-combined-with-cetuximab-or-bevacizumab-on-overall-survival-in-patients-with-kras-wild-type-advanced-or-metastatic-colorectal-cancer-a-randomized-clinical-trial
#13
Alan P Venook, Donna Niedzwiecki, Heinz-Josef Lenz, Federico Innocenti, Briant Fruth, Jeffrey A Meyerhardt, Deborah Schrag, Claire Greene, Bert H O'Neil, James Norman Atkins, Scott Berry, Blase N Polite, Eileen M O'Reilly, Richard M Goldberg, Howard S Hochster, Richard L Schilsky, Monica M Bertagnolli, Anthony B El-Khoueiry, Peter Watson, Al B Benson, Daniel L Mulkerin, Robert J Mayer, Charles Blanke
Importance: Combining biologic monoclonal antibodies with chemotherapeutic cytotoxic drugs provides clinical benefit to patients with advanced or metastatic colorectal cancer, but the optimal choice of the initial biologic therapy in previously untreated patients is unknown. Objective: To determine if the addition of cetuximab vs bevacizumab to the combination of leucovorin, fluorouracil, and oxaliplatin (mFOLFOX6) regimen or the combination of leucovorin, fluorouracil, and irinotecan (FOLFIRI) regimen is superior as first-line therapy in advanced or metastatic KRAS wild-type (wt) colorectal cancer...
June 20, 2017: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/28631600/inhibition-of-carbonic-anhydrase-ix-by-ureidosulfonamide-inhibitor-u104-reduces-prostate-cancer-cell-growth-but-does-not-modulate-daunorubicin-or-cisplatin-cytotoxicity
#14
Anne Riemann, Antje Güttler, Verena Haupt, Henri Wichmann, Sarah Reime, Matthias Bache, Dirk Vordermark, Oliver Thews
Carbonic anhydrase IX has emerged as a promising target for cancer therapy. It is highly up-regulated in hypoxic regions and mediates pH regulation critical for tumor cell survival as well as extracellular acidification of the tumor microenvironment which promotes tumor aggressiveness via various mechanisms, such as augmenting metastatic potential. Therefore, the aim of this study was to analyze the complex interdependency between CA IX and the tumor microenvironment in prostate tumor cells in concern of potential therapeutic implications...
June 19, 2017: Oncology Research
https://www.readbyqxmd.com/read/28631569/insulin-induced-enhancement-of-mcf-7-breast-cancer-cell-response-to-5-fluorouracil-and-cyclophosphamide
#15
Siddarth Agrawal, Mateusz Łuc, Piotr Ziółkowski, Anil Kumar Agrawal, Ewa Pielka, Kinga Walaszek, Krzysztof Zduniak, Marta Woźniak
The study was designed to evaluate the potential use of insulin for cancer-specific treatment. Insulin-induced sensitivity of MCF-7 breast cancer cells to chemotherapeutic agents 5-fluorouracil and cyclophosphamide was evaluated. To investigate and establish the possible mechanisms of this phenomenon, we assessed cell proliferation, induction of apoptosis, activation of apoptotic and autophagic pathways, expression of glucose transporters 1 and 3, formation of reactive oxygen species, and wound-healing assay...
June 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/28631098/urolithins-impair-cell-proliferation-arrest-the-cell-cycle-and-induce-apoptosis-in-umuc3-bladder-cancer-cells
#16
Joana Liberal, Anália Carmo, Célia Gomes, Maria Teresa Cruz, Maria Teresa Batista
Ellagitannins have been gaining attention as potential anticancer molecules. However, the low bioavailability of ellagitannins and their extensive metabolization in the gastrointestinal tract into ellagic acid and urolithins suggest that the health benefits of consuming ellagitannins rely on the direct effects of their metabolites. Recently, chemopreventive and chemotherapeutic activities were ascribed to urolithins. Nonetheless, there is still a need to screen and evaluate the selectivity of these molecules and to elucidate their cellular mechanisms of action...
June 20, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28631011/isoprenyl-carboxyl-methyltransferase-inhibitors-a-brief-review-including-recent-patents
#17
REVIEW
Woo Seok Yang, Seung-Gu Yeo, Sungjae Yang, Kyung-Hee Kim, Byong Chul Yoo, Jae Youl Cho
Among the enzymes involved in the post-translational modification of Ras, isoprenyl carboxyl methyltransferase (ICMT) has been explored by a number of researchers as a significant enzyme controlling the activation of Ras. Indeed, inhibition of ICMT exhibited promising anti-cancer activity against various cancer cell lines. This paper reviews patents and research articles published between 2009 and 2016 that reported inhibitors of ICMT as potential chemotherapeutic agents targeting Ras-induced growth factor signaling...
June 19, 2017: Amino Acids
https://www.readbyqxmd.com/read/28630436/a-novel-gd-dtpa-conjugated-poly-l-%C3%AE-glutamyl-glutamine-paclitaxel-polymeric-delivery-system-for-tumor-theranostics
#18
Lipeng Gao, Jinge Zhou, Jing Yu, Qilong Li, Xueying Liu, Lei Sun, Ting Peng, Jing Wang, Jianzhong Zhu, Jihong Sun, Weiyue Lu, Lei Yu, Zhiqiang Yan, Yiting Wang
The conventional chemotherapeutics could not be traced in vivo and provide timely feedback on the clinical effectiveness of drugs. In this study, poly(L-γ-glutamyl-glutamine)-paclitaxel (PGG-PTX), as a model polymer, was chemically conjugated with Gd-DTPA (Gd-diethylenetriaminepentaacetic acid), a T1-contrast agent of MRI, to prepare a Gd-DTPA-conjugated PGG-PTX (PGG-PTX-DTPA-Gd) delivery system used for tumor theranostics. PGG-PTX-DTPA-Gd can be self-assembled to NPs in water with a z-average hydrodynamic diameter about 35...
June 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28629893/a-new-nir-triggered-dox-and-icg-co-delivery-system-for-enhanced-multidrug-resistant-cancer-treatment-through-simultaneous-chemo-photothermal-photodynamic-therapy
#19
Yanna Yu, Zhipeng Zhang, Yun Wang, Hao Zhu, Fangzhou Li, Yuanyuan Shen, Shengrong Guo
It is a great challenge to combat multidrug resistant (MDR) cancer effectively. To address this issue, we developed a new near-infrared (NIR) triggered chemotherapeutic agent doxorubicin (DOX) and photosensitizer indocyanine green (ICG) co-release system by aid of NIR induced photothermal effect of gold nanocages (AuNCs) and temperature sensitive phase-change property of 1-tetradecanol at its melting point of 39°C, which could simultaneously exerted chemo/photothermal/photodynamic treatment on MDR human breast cancer MCF-7/ADR cells...
June 16, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28628925/apoptosis-and-caspase-3-pathway-role-on-anti-proliferative-effects-of-scrophulariaoxy-sepala-methanolic-extract-on-caco-2-cells
#20
Ali Namvaran, Mehdi Fazeli, Safar Farajnia, Gholamreza Hamidian, Hassan Rezazadeh
Colorectal cancer is one the most important malignancies worldwide and finding new treatment option for this cancer is of high priority. Natural compounds are common source of drugs for treatment of various diseases including cancers. The aim of this study was to investigate the effects of Scrophularia oxysepala extract on Caco-2 cells and explore the possible role of caspase 3 pathway in inducing cell death in this cancer cells in compare with chemotherapy agents of cisplatin and capecitabine. The methanolic extract of Scrophularia oxysepala (SO) was prepared by drench method...
June 19, 2017: Drug Research
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