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anticancer drug research

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https://www.readbyqxmd.com/read/28335655/the-therapeutic-potential-of-targeting-abc-transporters-to-combat-multi-drug-resistance
#1
Piyush Bugde, Riya Biswas, Fabrice Merien, Jun Lu, Dong-Xu Liu, Mingwei Chen, Shufeng Zhou, Yan Li
Most disseminated cancers remain fatal despite the availability of a variety of conventional and novel treatments including surgery, chemotherapy, radiotherapy, immunotherapy, and biologically targeted therapy. A major factor responsible for the failure of chemotherapy in the treatment of cancer is the development of multidrug resistance (MDR). The overexpression of various ABC transporters in cancer cells can efficiently remove the anticancer drug from the cell, thus causing the drug to lose its effect. Areas covered: In this review, we summarised the ongoing research related to the mechanism, function, and regulation of ABC transporters...
March 24, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28335244/human-serum-albumin-nanoparticles-for-use-in-cancer-drug-delivery-process-optimization-and-in-vitro-characterization
#2
Nikita Lomis, Susan Westfall, Leila Farahdel, Meenakshi Malhotra, Dominique Shum-Tim, Satya Prakash
Human serum albumin nanoparticles (HSA-NPs) are widely-used drug delivery systems with applications in various diseases, like cancer. For intravenous administration of HSA-NPs, the particle size, surface charge, drug loading and in vitro release kinetics are important parameters for consideration. This study focuses on the development of stable HSA-NPs containing the anti-cancer drug paclitaxel (PTX) via the emulsion-solvent evaporation method using a high-pressure homogenizer. The key parameters for the preparation of PTX-HSA-NPs are: the starting concentrations of HSA, PTX and the organic solvent, including the homogenization pressure and its number cycles, were optimized...
June 15, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28330413/molecular-dynamic-simulation-and-dft-study-on-the-drug-dna-interaction-crocetin-as-an-anticancer-and-dna-nanostructure-model
#3
Ebrahim Azarhazin, Mohammad Izadyar, Mohammad Reza Housaindokht
In this research, the interaction of Crocetin as an anticancer drug and a Dickerson DNA has been investigated. 25 ns molecular dynamic simulations of Crocetin and DNA composed of twelve base pairs and a sequence of d(CGCGAATTCGCG)2 were done in water. Three definite parts of the B-DNA were considered in analyzing the best interactive site from the thermodynamic point of view. Binding energy analysis showed that van der Waals interaction is the most important part related to the reciprocal O and H atoms of the Crocetin and DNA...
March 22, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28324509/human-telomeric-g-quadruplex-structures-and-g-quadruplex-interactive-compounds
#4
Clement Lin, Danzhou Yang
G-quadruplexes are noncanonical secondary structures formed in DNA sequences containing consecutive runs of guanines. It has been shown that the 3' G-rich single-stranded overhangs of human telomeres can form G-quadruplex structures, and the human telomeric DNA G-quadruplexes are considered attractive targets for anticancer drugs. G-quadruplex-interactive compounds have been shown to inhibit telomerase access as well as telomere capping. Nuclear magnetic resonance (NMR) spectroscopy is a powerful method in determining the G-quadruplex structures under physiologically relevant conditions...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28323051/anticancer-and-anti-angiogenic-activities-of-extract-from-actinidia-eriantha-benth-root
#5
Jian-Guo Wu, Li Ma, Shui-Hua Lin, Yan-Bin Wu, Jun Yi, Bin-Jun Yang, Jin-Zhong Wu, Ka-Hing Wong
ETHNOPHARMACOLOGICAL RELEVANCE: The roots of Actinidia eriantha Benth (AER) are commonly used traditional folk medicine for the treatment of gastric carcinoma, nasopharyngeal carcinoma, and breast carcinoma. Besides, the anti-proliferative and immunomodulatory effects of AER polysaccharides on tumor-bearing mice have been reported previously. AIM OF THE STUDY: This work was carried out to investigate the anticancer and anti-angiogenic activities of AER. MATERIALS AND METHODS: The growth inhibitory effects of ethanol extracts from the leaves (EEL), stems (EES) and roots (EER) of A...
March 17, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28322141/lessons-learned-from-gemcitabine-impact-of-therapeutic-carrier-systems-and-gemcitabine-s-drug-conjugates-on-cancer-therapy
#6
REVIEW
Sathish Dyawanapelly, Animesh Kumar, Manish K Chourasia
Currently, drug delivery systems have a high impact in cancer therapy and are receiving more attention than conventional cancer treatment modalities. Compared with current cancer therapies, gemcitabine (2', 2'-difluoro-2'-deoxycytidine) has been proven to be an effective chemotherapeutic agent against pancreatic, colon, bladder, breast, ovarian, non-small-cell lung, and head and neck cancers in combination with other anticancer agents. To improve the safety and efficacy of cytotoxic drugs, several drug delivery systems have been explored...
2017: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/28315438/rectorite-intercalated-nanoparticles-for-improving-controlled-release-of-doxorubicin-hydrochloride
#7
Jian Jin, Hu Tu, Jiajia Chen, Gu Cheng, Xiaowen Shi, Hongbing Deng, Zubing Li, Yumin Du
Controlled release of drugs has been widely researched in biomedical area. Nanoparticles (NPs) as ideal drug carriers are often used to facilitate improvements in the therapeutic index of drugs. In this study, natural polymers carboxymethyl chitosan (CMC) and lysozyme (LY) were mixed to prepare CMC-LY NPs by electrostatic self-assembly interactions. In addition, layered silicate rectorite (REC) was introduced into NPs to explore the effect on the encapsulation efficacy and controlled release of doxorubicin hydrochloride (DOX)...
March 14, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28314784/integrative-cancer-pharmacogenomics-to-infer-large-scale-drug-taxonomy
#8
Nehme El-Hachem, Deena M A Gendoo, Laleh Soltan Ghoraie, Zhaleh Safikhani, Petr Smirnov, Christina Chung, Kenan Deng, Alisa Fang, Erin Birkwood, Chantal Ho, Ruth Isserlin, Gary Bader, Anna Goldenberg, Benjamin Haibe-Kains
Identification of drug targets and mechanism of action (MoA) for new and uncharacterized anticancer drugs is important for optimization of treatment efficacy. Current MoA prediction largely relies on prior information including side effects, therapeutic indication, and chemo-informatics. Such information is not transferable or applicable for newly identified, previously uncharacterized small molecules. Therefore, a shift in the paradigm of MoA predictions is necessary towards development of unbiased approaches that can elucidate drug relationships and efficiently classify new compounds with basic input data...
March 17, 2017: Cancer Research
https://www.readbyqxmd.com/read/28314511/novel-platinum-iv-complexes-conjugated-with-a-wogonin-derivative-as-multi-targeted-anticancer-agents
#9
Xiaodong Qin, Gang Xu, Feihong Chen, Lei Fang, Shaohua Gou
Platinum-based complexes like cisplatin and oxaliplatin are well known the mainstay of chemotherapy regimens on clinic. Wogonin, a natural product that possesses wide biological activities, is now in phase I clinical test as an anticancer agent in China. Herein reported are a series of novel Pt(IV) complexes that conjugated a wogonin derivative (compound 3) to the axial position via a linker group. After being tethered to the platinum(IV) complexes, the wogonin derivative provided multiple anticancer effects, especially in compound 10, a fusion containing wogonin and cisplatin units...
March 7, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28302224/-advances-in-the-research-of-the-regulation-of-chinese-traditional-medicine-monomer-and-its-derivatives-on-autophagy-in-non-small-cell-lung-cancer
#10
Meiyi Xiang, Ruilei Li, Zhiwei Zhang, Xin Song
The high morbidity and mortality of non-small cell lung cancer (NSCLC) did influence the quality of life of tumor patients world-wide. There is an urgent need to develop new therapies that have high anti-tumor activity and low toxicity side effects. It is widely accepted that autophagy can play diverse roles in carcinogenesis, such as induces pro-death of lung cancer cells or helps the escape from cell death, making it become a proper anticancer target. It's believed that various monomers of Chinese traditional medicine closely correlates to anti-NSCLC activities, and that even could affect the acquired multiple drug resistance (MDR)...
March 20, 2017: Zhongguo Fei Ai za Zhi, Chinese Journal of Lung Cancer
https://www.readbyqxmd.com/read/28302184/cytokine-free-directed-differentiation-of-human-pluripotent-stem-cells-efficiently-produces-hemogenic-endothelium-with-lymphoid-potential
#11
Yekaterina Galat, Svetlana Dambaeva, Irina Elcheva, Aaruni Khanolkar, Kenneth Beaman, Philip M Iannaccone, Vasiliy Galat
BACKGROUND: The robust generation of human hematopoietic progenitor cells from induced or embryonic pluripotent stem cells would be beneficial for multiple areas of research, including mechanistic studies of hematopoiesis, the development of cellular therapies for autoimmune diseases, induced transplant tolerance, anticancer immunotherapies, disease modeling, and drug/toxicity screening. Over the past years, significant progress has been made in identifying effective protocols for hematopoietic differentiation from pluripotent stem cells and understanding stages of mesodermal, endothelial, and hematopoietic specification...
March 17, 2017: Stem Cell Research & Therapy
https://www.readbyqxmd.com/read/28299394/caenorhabditis-elegans-as-a-powerful-alternative-model-organism-to-promote-research-in-genetic-toxicology-and-biomedicine
#12
REVIEW
Sebastian Honnen
In view of increased life expectancy the risk for disturbed integrity of genetic information increases. This inevitably holds the implication for higher incidence of age-related diseases leading to considerable cost increase in health care systems. To develop preventive strategies it is crucial to evaluate external and internal noxae as possible threats to our DNA. Especially the interplay of DNA damage response (DDR) and DNA repair (DR) mechanisms needs further deciphering. Moreover, there is a distinct need for alternative in vivo test systems for basic research and also risk assessment in toxicology...
March 15, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28290771/institutional-profile-pharmacogenomic-research-in-r-stephanie-huang-laboratory
#13
Paul Geeleher, Aritro Nath, Rong Stephanie Huang
The Huang Lab was established in 2009 at the University of Chicago and has since been active in conducting pharmacogenomic research. Our laboratory's main research focus is translational pharmacogenomics with a particular interest in the pharmacogenomics of anticancer agents. By systematically evaluating the human genome and its relationships to drug response and toxicity, our goal is to develop clinically useful models that predict risk for adverse drug reactions and nonresponse prior to administration of chemotherapy...
March 14, 2017: Pharmacogenomics
https://www.readbyqxmd.com/read/28290490/the-high-price-of-anticancer-drugs-origins-implications-barriers-solutions
#14
REVIEW
Vinay Prasad, Kevin De Jesús, Sham Mailankody
Globally, annual spending on anticancer drugs is around US$100 billion, and is predicted to rise to $150 billion by 2020. In the USA, a novel anticancer drug routinely costs more than $100,000 per year of treatment. When adjusted for per capita spending power, however, drugs are most unaffordable in economically developing nations, such as India and China. Not only are launch prices high and rising, but individual drug prices are often escalated during exclusivity periods. High drug prices harm patients - often directly through increased out-of-pocket expenses, which reduce levels of patient compliance and lead to unfavourable outcomes - and harms society - by imposing cumulative price burdens that are unsustainable...
March 14, 2017: Nature Reviews. Clinical Oncology
https://www.readbyqxmd.com/read/28290183/synthesis-of-ultrasound-contrast-agents-characteristics-and-size-distribution-analysis-secondary-publication
#15
Hak Jong Lee, Tae-Jong Yoon, Young Il Yoon
Purpose: The purpose of this study was to establish a method for ultrasound (US) contrast agent synthesis and to evaluate the characteristics of the synthesized US contrast agent. Methods: A US contrast agent, composed of liposome and sulfur hexafluoride (SF6), was synthesized by dissolving 21 μmol 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine (DPPC, C40H80NO8P), 9 μmol cholesterol, and 1.9 μmol of dihexadecylphosphate (DCP, [CH3(CH2)15O]2P(O)OH) in chloroform...
February 14, 2017: Ultrasonography
https://www.readbyqxmd.com/read/28287321/curcumin-nanotechnologies-and-its-anticancer-activity
#16
Parasuraman Aiya Subramani, Kalpana Panati, Venkata Ramireddy Narala
Cancer is one of the leading causes of death worldwide. Curcumin is a well-established anticancer agent in vitro but its efficacy is yet to be proven in clinical trials. Poor bioavailability of curcumin is the principal reason behind the lack of efficiency of curcumin in clinical trials. Many studies prove that the bioavailability of curcumin can be improved by administering it through nanoparticle drug carriers. This review focuses on the efforts made in the field of nanotechnology to improve the bioavailability of curcumin...
April 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28286420/hlbt-100-a-highly-potent-anti-cancer-flavanone-from-tillandsia-recurvata-l-l
#17
Henry I C Lowe, Ngeh J Toyang, Charah T Watson, Kenneth N Ayeah, Joseph Bryant
BACKGROUND: The incidence and mortalities from cancers remain on the rise worldwide. Despite significant efforts to discover and develop novel anticancer agents, many cancers remain in the unmet need category. As such, efforts to discover and develop new and more effective and less toxic agents against cancer remain a top global priority. Our drug discovery approach is natural products based with a focus on plants. Tillandsia recurvata (L.) L. is one of the plants selected by our research team for further studies based on previous bioactivity findings on the anticancer activity of this plant...
2017: Cancer Cell International
https://www.readbyqxmd.com/read/28284095/development-of-2-4-diaminoquinazoline-derivatives-as-potent-pak4-inhibitors-by-the-core-refinement-strategy
#18
Chenzhou Hao, Wanxu Huang, Xiaodong Li, Jing Guo, Meng Chen, Zizheng Yan, Kai Wang, Xiaolin Jiang, Shuai Song, Jian Wang, Dongmei Zhao, Feng Li, Maosheng Cheng
Upon analysis of the reported crystal structure of PAK4 inhibitor KY04031 (PAK4 IC50 = 0.790 μM) in the active site of PAK4, we investigated the possibility of changing the triazine core of KY04031 to a quinazoline. Using KY04031 as a starting compound, a library of 2, 4-diaminoquinazoline derivatives were designed and synthesized. These compounds were evaluated for PAK4 inhibition, leading to the identification of compound 9d (PAK4 IC50 = 0.033 μM). Compound 9d significantly induced the cell cycle in the G1/S phase and inhibited migration and invasion of A549 cells that over-express PAK4 via regulation of the PAK4-LIMK1 signalling pathway...
March 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28283781/gold-compounds-as-cysteine-protease-inhibitors-perspectives-for-pharmaceutical-application-as-antiparasitic-agents
#19
Lara Massai, Luigi Messori, Nicola Micale, Tanja Schirmeister, Louis Maes, Dolores Fregona, Maria Agostina Cinellu, Chiara Gabbiani
Gold compounds form a new class of promising metal-based drugs with a number of potential therapeutic applications, particularly in the fields of anticancer and antimicrobial treatments. Previous research revealed that a group of structurally diverse gold compounds cause conspicuous inhibition of the protease activities of the human proteasome. Given the pharmacological importance of protease inhibition, the present study further explored whether these gold compounds might inhibit a few other proteases that are accepted druggable targets for disease treatment...
March 10, 2017: Biometals: An International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine
https://www.readbyqxmd.com/read/28283484/comparative-effectiveness-and-safety-of-erythropoiesis-stimulating-agents-biosimilars-vs-originators-in-clinical-practice-a-population-based-cohort-study-in-italy
#20
Francesco Trotta, Valeria Belleudi, Danilo Fusco, Laura Amato, Alessandra Mecozzi, Flavia Mayer, Massimo Sansone, Marina Davoli, Antonio Addis
OBJECTIVES: To evaluate the benefit/risk profile of epoetin α biosimilar with the erythropoiesis-stimulating agents (ESAs) originators when administered to naïve patients from clinical practice. DESIGN: Population-based observational cohort study. SETTING: All residents in the Lazio Region, Italy, with chronic kidney disease (CKD) or cancer retrieved from the Electronic Therapeutic Plan (ETP) Register for ESA between 2012 and 2014. PARTICIPANTS: Overall, 13 470 incident ESA users were available for the analysis, 8161 in the CKD and 5309 in the oncology setting, respectively...
March 10, 2017: BMJ Open
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