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https://www.readbyqxmd.com/read/29053567/eco-friendly-formulated-zinc-oxide-nanoparticles-induction-of-cell-cycle-arrest-and-apoptosis-in-the-mcf-7-cancer-cell-line
#1
Amin Boroumand Moghaddam, Mona Moniri, Susan Azizi, Raha Abdul Rahim, Arbakariya Bin Ariff, Mohammad Navaderi, Rosfarizan Mohamad
Green products have strong potential in the discovery and development of unique drugs. Zinc oxide nanoparticles (ZnO NPs) have been observed to have powerful cytotoxicity against cells that cause breast cancer. The present study aims to examine the cell cycle profile, status of cell death, and pathways of apoptosis in breast cancer cells (MCF-7) treated with biosynthesized ZnO NPs. The anti-proliferative activity of ZnO NPs was determined using MTT assay. Cell cycle analysis and the mode of cell death were evaluated using a flow cytometry instrument...
October 20, 2017: Genes
https://www.readbyqxmd.com/read/29052423/streamlined-total-synthesis-of-trioxacarcins-and-its-application-to-the-design-synthesis-and-biological-evaluation-of-analogues-thereof-discovery-of-simpler-designed-and-potent-trioxacarcin-analogues
#2
K C Nicolaou, Pengxi Chen, Shugao Zhu, Quan Cai, Rohan D Erande, Ruofan Li, Hongbao Sun, Kiran Kumar Pulukuri, Stephan Rigol, Monette Aujay, Joseph Sandoval, Julia Gavrilyuk
A streamlined total synthesis of the naturally occurring antitumor agents trioxacarcins is described, along with its application to the construction of a series of designed analogues of these complex natural products. Biological evaluation of the synthesized compounds revealed a number of highly potent, and yet structurally simpler, compounds that are effective against certain cancer cell lines, including a drug-resistant line. A novel one-step synthesis of anthraquinones and chloro anthraquinones from simple ketone precursors and phenylselenyl chloride is also described...
October 20, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29052219/pharmacogenomic-discovery-to-function-and-mechanism-breast-cancer-as-a-case-study
#3
Liewei Wang, James Ingle, Richard Weinshilboum
Biomedical research is undergoing rapid change, with the development of a series of analytical omics techniques that are capable of generating Biomedical Big Data. These developments provide an unprecedented opportunity to gain novel insight into disease pathophysiology and mechanisms of drug action and response-but they also present significant challenges. Pharmacogenomics is a discipline within Clinical Pharmacology that has been at the forefront in defining, taking advantage of and dealing with the opportunities and challenges of this aspect of the Post-Genome Project world...
October 20, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29052131/merkel-cell-polyomavirus-a-new-dna-virus-associated-with-human-cancer
#4
Margo MacDonald, Jianxin You
Merkel cell polyomavirus (MCPyV or MCV) is a novel human polyomavirus that has been discovered in Merkel cell carcinoma (MCC), a highly aggressive skin cancer. MCPyV infection is widespread in the general population. MCPyV-associated MCC is one of the most aggressive skin cancers, killing more patients than other well-known cancers such as cutaneous T-cell lymphoma and chronic myelogenous leukemia (CML). Currently, however, there is no effective drug for curing this cancer. The incidence of MCC has tripled over the past two decades...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29050333/characterization-of-cadd522-a-small-molecule-that-inhibits-runx2-dna-binding-and-exhibits-antitumor-activity
#5
Myoung Sook Kim, Ramkishore Gernapudi, Eun Yong Choi, Rena G Lapidus, Antonino Passaniti
The RUNX2 transcription factor promotes breast cancer growth and metastasis through interactions with a variety of cofactors that activate or repress target genes. Using a direct drug discovery approach we identified CADD522 as a small molecule that inhibits the DNA binding of the runt box domain protein, RUNX2. The current study defines the effect of CADD522 on breast cancer growth and metastasis, and addresses the mechanisms by which it exerts its anti-tumor activity. CADD522 treatment resulted in significant growth inhibition, clonogenic survival, tumorsphere formation, and invasion of breast cancer cells...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29050278/identification-of-core-genes-and-outcome-in-gastric-cancer-using-bioinformatics-analysis
#6
Chenhua Sun, Qi Yuan, Dongdong Wu, Xiaohu Meng, Baolin Wang
Gastric cancer (GC) is a common malignant neoplasm of gastrointestinal tract. We chose gene expression profile of GSE54129 from GEO database aiming to find key genes during the occurrence and development of GC. 132 samples, including 111 cancer and 21 normal gastric mucosa epitheliums, were included in this analysis. Differentially expressed genes (DEGs) between GC patients and health people were picked out using GEO2R tool, then we performed gene ontology (GO) analysis and Kyoto Encyclopedia of Gene and Genome (KEGG) pathway analysis using The Database for Annotation, Visualization and Integrated Discovery (DAVID)...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29048400/cd10-aldh-cells-are-the-sole-cisplatin-resistant-component-of-a-novel-ovarian-cancer-stem-cell-hierarchy
#7
Brendan Ffrench, Claudia Gasch, Karsten Hokamp, Cathy Spillane, Gordon Blackshields, Thamir Mahmoud Mahgoub, Mark Bates, Louise Kehoe, Aoibhinn Mooney, Ronan Doyle, Brendan Doyle, Dearbhaile O'Donnell, Noreen Gleeson, Bryan T Hennessy, Britta Stordal, Ciaran O'Riain, Helen Lambkin, Sharon O'Toole, John J O'Leary, Michael F Gallagher
It is long established that tumour-initiating cancer stem cells (CSCs) possess chemoresistant properties. However, little is known of the mechanisms involved, particularly with respect to the organisation of CSCs as stem-progenitor-differentiated cell hierarchies. Here we aimed to elucidate the relationship between CSC hierarchies and chemoresistance in an ovarian cancer model. Using a single cell-based approach to CSC discovery and validation, we report a novel, four-component CSC hierarchy based around the markers cluster of differentiation 10 (CD10) and aldehyde dehydrogenase (ALDH)...
October 19, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/29047025/targeting-the-ubiquitin-proteasome-system-for-cancer-treatment-discovering-novel-inhibitors-from-nature-and-drug-repurposing
#8
Claire L Soave, Tracey Guerin, Jinbao Liu, Q Ping Dou
In the past 15 years, the proteasome has been validated as an anti-cancer drug target and 20S proteasome inhibitors (such as bortezomib and carfilzomib) have been approved by the FDA for the treatment of multiple myeloma and some other liquid tumors. However, there are shortcomings of clinical proteasome inhibitors, including severe toxicity, drug resistance, and no effect in solid tumors. At the same time, extensive research has been conducted in the areas of natural compounds and old drug repositioning towards the goal of discovering effective, economical, low toxicity proteasome-inhibitory anti-cancer drugs...
October 18, 2017: Cancer Metastasis Reviews
https://www.readbyqxmd.com/read/29045731/the-chimpanzee-model-of-viral-hepatitis-advances-in-understanding-the-immune-response-and-treatment-of-viral-hepatitis
#9
Robert E Lanford, Christopher M Walker, Stanley M Lemon
Chimpanzees (Pan troglodytes) have contributed to diverse fields of biomedical research due to their close genetic relationship to humans and in many instances due to the lack of any other animal model. This review focuses on the contributions of the chimpanzee model to research on hepatitis viruses where chimpanzees represented the only animal model (hepatitis B and C) or the most appropriate animal model (hepatitis A). Research with chimpanzees led to the development of vaccines for HAV and HBV that are used worldwide to protect hundreds of millions from these diseases and, where fully implemented, have provided immunity for entire generations...
October 17, 2017: ILAR Journal
https://www.readbyqxmd.com/read/29045529/impact-of-genetic-variations-in-the-mapk-signaling-pathway-on-outcome-in-metastatic-colorectal-cancer-patients-treated-with-first-line-folfiri-and-bevacizumab-data-from-fire-3-and-tribe-trials
#10
M D Berger, S Stintzing, V Heinemann, D Yang, S Cao, Y Sunakawa, Y Ning, S Matsusaka, S Okazaki, Y Miyamoto, M Suenaga, M Schirripa, S Soni, W Zhang, A Falcone, F Loupakis, H-J Lenz
Background: The MAPK-interacting kinase 1 (MKNK1) is localized downstream of the RAS/RAF/ERK and the MAP3K1/MKK/p38 signaling pathway. Through phosphorylation MKNK1 regulates the function of eukaryotic translation initiation factor 4E, a key player in translational control, whose expression is often upregulated in metastatic colorectal cancer patients (mCRC). Preclinical data suggest that MKNK1 increases angiogenesis by upregulating angiogenic factors. We therefore hypothesize that variations in the MKNK1 gene predict outcome in mCRC patients treated with first-line FOLFIRI and bevacizumab (bev)...
August 2, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/29045126/characterization-of-three-druggable-hotspots-in-the-aurora-a-tpx2-interaction-using-biochemical-biophysical-and-fragment-based-approaches
#11
Patrick J McIntyre, Patrick M Collins, Lukáš Vrzal, Kristian Birchall, Laurence H Arnold, Chido Mpamhanga, Peter J Coombs, Selena G Burgess, Mark W Richards, Anja Winter, Václav Veverka, Frank von Delft, Andy Merritt, Richard Bayliss
The mitotic kinase Aurora-A and its partner protein TPX2 (Targeting Protein for Xenopus kinesin-like protein 2), are overexpressed in cancers and it has been proposed that they work together as an oncogenic holoenzyme. TPX2 is responsible for activating Aurora-A during mitosis, ensuring proper cell division. Disruption of the interface with TPX2 is therefore a potential target for novel anti-cancer drugs that exploit the increased sensitivity of cancer cells to mitotic stress. Here, we investigate the interface using co-precipitation assays and isothermal titration calorimetry to quantify the energetic contribution of individual residues of TPX2...
October 18, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/29039651/intracellular-drug-uptake-a-comparison-of-single-cell-measurements-using-tof-sims-imaging-and-quantification-from-cell-populations-with-lc-ms-ms
#12
Carla F Newman, Rasmus Havelund, Melissa K Passarelli, Peter S Marshall, Ian Francis, Andrew West, Morgan Russell Alexander, Ian S Gilmore, Colin T Dollery
ToF-SIMS is a label free imaging method that has been shown to enable imaging of amiodarone in single rat macrophage (NR8383) cells. In this study, we show the method extends to three other cell lines relevant to drug discovery: Human embryonic kidney (HEK293), cervical cancer (HeLa) and liver cancer (HepG2). There is significant interest in the variation of drug uptake at the single cell level and we use ToF-SIMS to show that there is great diversity between individual cells and when comparing each of the cell types...
October 17, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/29035165/development-of-highly-sensitive-cell-based-akt-kinase-elisa-for-monitoring-pi3k-beta-activity-and-compound-efficacy
#13
Mahesh Yanamandra, Labanyamoy Kole, Archana Giri, Sayan Mitra
Phosphatidylinositol-3 kinase pathway regulates multiple cellular function involving cell survival, growth, motility proliferation, apoptosis, and adhesion. These are deregulated in various diseases like cancer, atherosclerosis, and inflammation. PI3Ks phosphorylate phosphatidylinositol 4,5 biphosphate (PIP2) yielding phosphatidylinositol 3, 4, 5 triphosphate (PIP3) that in turn activates AKT kinase (serine/threonine kinase) which is the central enzyme in regulation of metabolic functions. Due to their implications in disease pathophysiology, PI3K/AKT inhibitors became attractive targets for pharmaceutical industries...
October 16, 2017: Journal of Immunoassay & Immunochemistry
https://www.readbyqxmd.com/read/29034591/organ-on-a-chip-platforms-a-convergence-of-advanced-materials-cells-and-microscale-technologies
#14
REVIEW
Samad Ahadian, Robert Civitarese, Dawn Bannerman, Mohammad Hossein Mohammadi, Rick Lu, Erika Wang, Locke Davenport-Huyer, Ben Lai, Boyang Zhang, Yimu Zhao, Serena Mandla, Anastasia Korolj, Milica Radisic
Significant advances in biomaterials, stem cell biology, and microscale technologies have enabled the fabrication of biologically relevant tissues and organs. Such tissues and organs, referred to as organ-on-a-chip (OOC) platforms, have emerged as a powerful tool in tissue analysis and disease modeling for biological and pharmacological applications. A variety of biomaterials are used in tissue fabrication providing multiple biological, structural, and mechanical cues in the regulation of cell behavior and tissue morphogenesis...
October 16, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/29031564/eif3a-a-new-anticancer-drug-target-in-the-eif-family
#15
Ji-Ye Yin, Jian-Ting Zhang, Wei Zhang, Hong-Hao Zhou, Zhao-Qian Liu
eIF3a is the largest subunit of eIF3, which is a key player in all steps of translation initiation. During the past years, eIF3a is recognized as a proto-oncogene, which is an important discovery in this field. It is widely reported to be correlated with cancer occurrence, metastasis, prognosis, and therapeutic response. Recently, the mechanisms of eIF3a action in the carcinogenesis are unveiled gradually. A number of cellular, physiological, and pathological processes involving eIF3a are identified. Most importantly, it is emerging as a new potential drug target in the eIF family, and some small molecule inhibitors are being developed...
October 12, 2017: Cancer Letters
https://www.readbyqxmd.com/read/29031066/serendipitous-discovery-of-potent-human-head-and-neck-squamous-cell-carcinoma-anti-cancer-molecules-a-fortunate-failure-of-a-rational-molecular-design
#16
Chiara Zagni, Venerando Pistarà, Luciana A Oliveira, Rogerio M Castilho, Giovanni Romeo, Ugo Chiacchio, Antonio Rescifina
Histone deacetylase inhibitors (HDACis) play an important role as valuable drugs targeted to cancer therapy: several HDACis are currently being tested in clinical trials. Two new potential HDACis 1a and 1d, characterized by the presence of a biphenyl-4-sulfonamide group as a connection unit between the N-{4-[(E)-(2-formylhydrazinylidene)methyl]-3-hydroxyphenyl} and the 2-hydroxy-N-(trifluoroacetyl)benzamide moiety, respectively, as two zinc-binding group (ZBG), have been designed, synthesized and tested for their biological activity...
October 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29029409/metabolic-characterization-and-pathway-analysis-of-berberine-protects-against-prostate-cancer
#17
Xianna Li, Aihua Zhang, Hui Sun, Zhidong Liu, Tianlei Zhang, Shi Qiu, Liang Liu, Xijun Wang
Recent explosion of biological data brings a great challenge for the traditional methods. With increasing scale of large data sets, much advanced tools are required for the depth interpretation problems. As a rapid-developing technology, metabolomics can provide a useful method to discover the pathogenesis of diseases. This study was explored the dynamic changes of metabolic profiling in cells model and Balb/C nude-mouse model of prostate cancer, to clarify the therapeutic mechanism of berberine, as a case study...
September 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29028926/structure-based-prediction-of-protein-peptide-binding-regions-using-random-forest
#18
Ghazaleh Taherzadeh, Yaoqi Zhou, Alan Wee-Chung Liew, Yuedong Yang
Motivation: Protein-peptide interactions are one of the most important biological interactions and play crucial role in many diseases including cancer. Therefore, knowledge of these interactions provides invaluable insights into all cellular processes, functional mechanisms, and drug discovery. Protein-peptide interactions can be analyzed by studying the structures of protein-peptide complexes. However, only a small portion has known complex structures and experimental determination of protein-peptide interaction is costly and inefficient...
September 26, 2017: Bioinformatics
https://www.readbyqxmd.com/read/29027931/discovering-the-biological-target-of-5-epi-sinuleptolide-using-a-combination-of-proteomic-approaches
#19
Elva Morretta, Roberta Esposito, Carmen Festa, Raffaele Riccio, Agostino Casapullo, Maria Chiara Monti
Sinuleptolide and its congeners are diterpenes with a norcembranoid skeleton isolated from the soft coral genus Sinularia. These marine metabolites are endowed with relevant biological activities, mainly associated with cancer development. 5-epi-sinuleptolide has been selected as a candidate for target discovery studies through the application of complementary proteomic approaches. Specifically, a combination of conventional chemical proteomics based on affinity chromatography, coupled with high-resolution mass spectrometry and bioinformatics, as well as drug affinity responsive target stability (DARTS), led to a clear identification of actins as main targets for 5-epi-sinuleptolide...
October 13, 2017: Marine Drugs
https://www.readbyqxmd.com/read/29027562/monomeric-and-dimeric-coordinatively-saturated-and-substitutionally-inert-ru-ii-polypyridyl-complexes-as-anticancer-drug-candidates
#20
REVIEW
Anna Notaro, Gilles Gasser
Due to the increasing impact of cancer on worldwide mortality, more and more attention is being devoted to the investigation of novel anticancer strategies. Among these, chemotherapy plays a key role in fighting cancer. This explains the increasing engagement of both the pharmaceutical industry and academia towards the discovery of new chemotherapeutic agents. In recent years, metal-based drugs have attracted much attention due to their atypical physico-chemical properties compared to organic molecules. After the approval of cisplatin as a chemotherapeutic agent in 1978, several types of metal-based drugs have been explored...
October 13, 2017: Chemical Society Reviews
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