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https://www.readbyqxmd.com/read/29673714/discovery-and-evaluation-of-nna-v-1-5-sodium-channel-blockers-with-potent-cell-invasion-inhibitory-activity-in-breast-cancer-cells
#1
Shilpa Dutta, Osbaldo Lopez Charcas, Samuel Tanner, Frédéric Gradek, Virginie Driffort, Sébastien Roger, Katri Selander, Sadanandan E Velu, Wayne Brouillette
Voltage-gated sodium channels (VGSC) are a well-established drug target for anti-epileptic, anti-arrhythmic and pain medications due to their presence and the important roles that they play in excitable cells. Recently, their presence has been recognized in non-excitable cells such as cancer cells and their overexpression has been shown to be associated with metastatic behavior in a variety of human cancers. The neonatal isoform of the VGSC subtype, Nav 1.5 (nNav 1.5) is overexpressed in the highly aggressive human breast cancer cell line, MDA-MB-231...
April 3, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29672977/phytotherapeutics-in-cancer-invasion-and-metastasis
#2
REVIEW
Bahare Salehi, Paolo Zucca, Mehdi Sharifi-Rad, Raffaele Pezzani, Sadegh Rajabi, William N Setzer, Elena Maria Varoni, Marcello Iriti, Farzad Kobarfard, Javad Sharifi-Rad
Cancer is a multifactorial disease, and therefore, a multitarget approach is needed to face the complex cancer biology, based on the combined use of different natural and synthetic anticancer agents able to target synergistically multiple signaling pathways involved in carcinogenesis, including angiogenesis and metastasis. In this view, the plant kingdom represents an unlimited source of phytotherapeutics with promising perspectives in the field of anticancer drug discovery. This narrative review aims to provide an updated overview on the bioactive phytochemicals exhibiting a promising potential as adjuvants in conventional anticancer therapies, with emphasis on antiangiogenic and antimetastatic activities...
April 19, 2018: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/29671783/telomerase-inhibition-by-a-new-synthetic-derivative-of-the-aporphine-alkaloid-boldine
#3
Sakineh Kazemi Noureini, Mitra Kheirabadi, Fatima Masoumi, Farve Khosrogerdi, Younes Zarei, Cristian Suárez-Rozas, Julio Salas-Norambuena, Bruce Kennedy Cassels
Telomerase, the enzyme responsible for cell immortality, is an important target in anti-cancer drug discovery. Boldine, an abundant aporphine alkaloid of Peumus boldus , is known to inhibit telomerase at non-toxic concentrations. Cytotoxicity of N -benzylsecoboldine hydrochloride (BSB), a synthetic derivative of boldine, was determined using the MTT method in MCF7 and MDA-MB231 cells. Aliquots of cell lysates were incubated with various concentrations of BSB in qTRAP (quantitative telomere repeat amplification protocol)-ligand experiments before substrate elongation by telomerase or amplification by hot-start Taq polymerase...
April 19, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29671387/positioning-europe-for-the-epitranscriptomics-challenge
#4
Michael Jantsch, Alessandro Quattrone, Mary O'Connell, Mark Helm, Michaela Frye, Manuel Macias-Gonzales, Marie Ohman, Stefan Ameres, Luc Willems, Francois Fuks, Anastasis Oulas, Stepanka Vanacova, Henrik Nielsen, Cecile Bousquet-Antonelli, Yuri Motorin, Jean-Yves Roignant, Nikolaos Balatsos, Andras Dinnyes, Pavel Baranov, Vincent Kelly, Ayelet Lamm, Gideon Rechavi, Mattia Pelizzola, Janis Liepins, Irina Holodnuka Kholodnyuk, Vanessa Zammit, Duncan Ayers, Finn Drablos, John Arne Dahl, Janusz Bujnicki, Carmen Jeronimo, Raquel Almeida, Monica Neagu, Marieta Costache, Jasna Bankovic, Bojana Banovic, Jan Kyselovic, Luis Miguel Valor, Stefan Selbert, Pinar Pir, Turan Demircan, Victoria Cowling, Matthias Schäfer, Walter Rossmanith, Denis Lafontaine, Alexandre David, Clement Carre, Frank Lyko, Raffael Schaffrath, Schraga Schwartz, Andre Verdel, Arne Klungland, Elzbieta Purta, Gordana Timotijevic, Fernando Cardona, Alberto Davalos, Ester Ballana, Donal O Carroll, Jernej Ule, Rupert Fray
The genetic alphabet consists of the four letters: C, A, G, and T in DNA and C,A,G, and U in RNA. Triplets of these four letters jointly encode 20 different amino acids out of which proteins of all organisms are built. This system is universal and is found in all kingdoms of life. However, bases in DNA and RNA can be chemically modified. In DNA, around 10 different modifications are known, and those have been studied intensively over the past 20 years. Scientific studies on DNA modifications and proteins that recognize them gave rise to the large field of epigenetic and epigenomic research...
April 19, 2018: RNA Biology
https://www.readbyqxmd.com/read/29671350/total-synthesis-and-cyclization-strategy-of-samoamide-a-a-cytotoxic-cyclic-octapeptide-rich-in-proline-and-phenlalanine-isolated-from-marine-cyanobacterium
#5
Qi Chang, Yu-Lei Li, Xia Zhao
Samoamide A is a cyclic octapeptide rich in proline and phenylalanine residues isolated from an American Samoa marine cyanobacterium, which exhibits potent activity against H460 human non-small-cell lung cancer cells (IC50 of 1.1 μM). The first total synthesis of samoamide A was achieved by employing a strategy of a solid-phase peptide synthesis (SPPS) and a head-to-tail cyclization selecting free steric-hinrance connection sites. Then the final product was purified and identified. This strategy not only provides a basis in producing potent cytotoxic agents for drug discovery, but also provides a reference to the total synthesis of proline-rich peptides...
April 19, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29670855/current-therapies-for-human-epidermal-growth-factor-receptor-2-positive-metastatic-breast-cancer-patients
#6
REVIEW
Alexey A Larionov
The median survival of patients with human epidermal growth factor receptor 2 (HER2)-positive metastatic breast cancer (MBC) has more than doubled, since the discovery of HER2-targeted treatments: it rose from less than 2 years in 2001 (prior introduction of trastuzumab) to more than 4 years in 2017. The initial generation of HER2-targeted therapies included trastuzumab with taxanes in the first line, followed by the addition of lapatinib and by a switch to another cytotoxic agent after progression. Results of CLEOPATRA, EMILIA, and TH3RESA trials have changed this clinical practice...
2018: Frontiers in Oncology
https://www.readbyqxmd.com/read/29670361/identification-of-molecular-target-genes-and-key-pathways-in-hepatocellular-carcinoma-by-bioinformatics-analysis
#7
Lei Zhou, Yanyan Du, Lingqun Kong, Xingyuan Zhang, Qiangpu Chen
Background and aim: Hepatocellular carcinoma (HCC) is a major cause of cancer mortality and is increasing incidence worldwide. The aim of this study was to identify the key genes and microRNAs in HCC and explore their potential mechanisms. Methods: The gene expression profiles of GSE76427, GSE64041, GSE57957, and the microRNA dataset GSE67882 were downloaded from the Gene Expression Omnibus database. The online tool GEO2R was used to obtain differentially expressed genes (DEGs) and miRNAs (DEMs)...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29670288/structural-basis-of-ligand-binding-modes-at-the-neuropeptide-y-y-1-receptor
#8
Zhenlin Yang, Shuo Han, Max Keller, Anette Kaiser, Brian J Bender, Mathias Bosse, Kerstin Burkert, Lisa M Kögler, David Wifling, Guenther Bernhardt, Nicole Plank, Timo Littmann, Peter Schmidt, Cuiying Yi, Beibei Li, Sheng Ye, Rongguang Zhang, Bo Xu, Dan Larhammar, Raymond C Stevens, Daniel Huster, Jens Meiler, Qiang Zhao, Annette G Beck-Sickinger, Armin Buschauer, Beili Wu
Neuropeptide Y (NPY) receptors belong to the G-protein-coupled receptor superfamily and have important roles in food intake, anxiety and cancer biology 1,2 . The NPY-Y receptor system has emerged as one of the most complex networks with three peptide ligands (NPY, peptide YY and pancreatic polypeptide) binding to four receptors in most mammals, namely the Y1 , Y2 , Y4 and Y5 receptors, with different affinity and selectivity 3 . NPY is the most powerful stimulant of food intake and this effect is primarily mediated by the Y1 receptor (Y1 R) 4 ...
April 18, 2018: Nature
https://www.readbyqxmd.com/read/29669996/structural-diversity-and-biological-activities-of-diterpenoids-derived-from-euphorbia-fischeriana-steud
#9
REVIEW
Baiyu Jian, Hao Zhang, Jicheng Liu
Diterpenoids are the focus of natural product drug discovery because of their great structural diversity and pronounced biological activities. Euphorbia fischeriana Steud is a Chinese traditional medicinal herb for curing edema, ascites, and cancer. This plant contains rich diterpenoids. Based on the carbon skeleton and substituents, it can be classified into thirteen subtypes: ent -abietane, daphnane, tigliane, ingenane, ent -atisane, ent -rosane, ent -kaurene, ent -kaurane, secotigliane, lathyrane, ent-pimarene, isopimarene and dimeric...
April 18, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29669750/current-challenges-and-opportunities-in-treating-glioblastoma
#10
Andrea Shergalis, Armand Bankhead, Urarika Luesakul, Nongnuj Muangsin, Nouri Neamati
Glioblastoma multiforme (GBM), the most common and aggressive primary brain tumor, has a high mortality rate despite extensive efforts to develop new treatments. GBM exhibits both intra- and intertumor heterogeneity, lending to resistance and eventual tumor recurrence. Large-scale genomic and proteomic analysis of GBM tumors has uncovered potential drug targets. Effective and "druggable" targets must be validated to embark on a robust medicinal chemistry campaign culminating in the discovery of clinical candidates...
July 2018: Pharmacological Reviews
https://www.readbyqxmd.com/read/29667346/in-situ-vaccination-harvesting-low-hanging-fruit-on-the-cancer-immunotherapy-tree
#11
REVIEW
Mee Rie Sheen, Steven Fiering
After 100 years of debate, it is clear that cancer is recognized by the immune system and this has generated immense interest in cancer immunotherapy. The systemic nature of the immune system gives immunotherapy the ability to treat metastatic disease, which currently requires chemotherapy that frequently fails. Like chemotherapy, most immunotherapy is systemically applied in an effort to generate systemic antitumor immune response. However, local administration of immunostimulatory reagents into a recognized tumor by in situ vaccination (ISV) can also generate systemic antitumor immunity to fight metastatic disease...
April 18, 2018: Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology
https://www.readbyqxmd.com/read/29667271/syndrome-and-outcome-of-antibody-negative-limbic-encephalitis
#12
Francesc Graus, Domingo Escudero, Laura Oleaga, Jordi Bruna, Alberto Villarejo-Galende, Jordi Ballabriga, María Inés Barceló, Francisco Gilo, Stoyan Popkirov, Pavel Stourac, Josep Dalmau
OBJECTIVE: To report the clinical characteristics of 12 patients with limbic encephalitis (LE) who were antibody-negative after a comprehensive immunological study. METHODS: Review of clinical records of 163 patients with LE. Immunohistochemistry on rat brain, cultured neurons, and cell-based assays were used to identify neuronal autoantibodies. Patients were included if 1) there was adequate clinical, CSF, and MRI information to classify the syndrome as LE, 2) MRI images were accesible for central review, and 3) serum and CSF were available and confirmed negative for neuronal antibodies...
April 18, 2018: European Journal of Neurology: the Official Journal of the European Federation of Neurological Societies
https://www.readbyqxmd.com/read/29667003/chemical-genomics-reveals-inhibition-of-breast-cancer-lung-metastasis-by-ponatinib-via-c-jun
#13
Wei Shao, Shasha Li, Lu Li, Kequan Lin, Xinhong Liu, Haiyan Wang, Huili Wang, Dong Wang
Metastasis is the leading cause of human cancer deaths. Unfortunately, no approved drugs are available for anti-metastatic treatment. In our study, high-throughput sequencing-based high-throughput screening (HTS2 ) and a breast cancer lung metastasis (BCLM)-associated gene signature were combined to discover anti-metastatic drugs. After screening of thousands of compounds, we identified Ponatinib as a BCLM inhibitor. Ponatinib significantly inhibited the migration and mammosphere formation of breast cancer cells in vitro and blocked BCLM in multiple mouse models...
April 17, 2018: Protein & Cell
https://www.readbyqxmd.com/read/29665843/next-generation-sequencing-analysis-of-receptor-type-tyrosine-kinase-genes-in-surgically-resected-colon-cancer-identification-of-gain-of-function-mutations-in-the-ret-proto-oncogene
#14
Duarte Mendes Oliveira, Katia Grillone, Chiara Mignogna, Valentina De Falco, Carmelo Laudanna, Flavia Biamonte, Rosa Locane, Francesco Corcione, Massimiliano Fabozzi, Rosario Sacco, Giuseppe Viglietto, Donatella Malanga, Antonia Rizzuto
BACKGROUND: Improvement in genetic characterization of Colon Cancer (CC) patients is required to propose new potential targets, since surgical resection coupled to chemotherapy, presents several limits such as cancer recurrence and drug resistance. Targeted therapies have more efficacy and less toxicity than standard treatments. One of the most relevant cancer-specific actionable targets are receptor tyrosine kinases (RTKs) whose role in CC need to be better investigated. METHODS: We have analysed 37 CC patients using the Ion AmpliSeq™ Comprehensive Cancer Panel (CCP)...
April 17, 2018: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/29665527/discovery-of-1-8-acridinedione-derivatives-as-novel-gcn5-inhibitors-via-high-throughput-screening
#15
Huan Xiong, Jie Han, Jun Wang, Wenchao Lu, Chen Wang, Yu Chen, Fulin Lian, Naixia Zhang, Yu-Chih Liu, Chenhua Zhang, Hong Ding, Hualiang Jiang, Wencong Lu, Cheng Luo, Bing Zhou
The general control nonrepressed protein 5 (GCN5) plays a crucial role in many biological processes. Dysregulation of GCN5 has been closely related to various human diseases, especially cancers. Hence, the exploitation of small molecules targeting GCN5 is essential for drug design and academic research. Based on the amplified luminescent proximity homogeneous assay screen methodology, we performed high throughput screening and discovered a novel GCN5 inhibitor DC_G16 with 1,8-acridinedione scaffold. Structure optimization led to the identification of a highly potent inhibitor, namely DC_G16-11 with the half-maximal inhibitory concentration (IC50 ) value of 6...
February 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29663896/molecular-interaction-and-computational-analytical-studies-of-pinocembrin-for-its-antiangiogenic-potential-targeting-vegfr-2-a-persuader-of-metastasis
#16
Neha Sharma, Mala Sharma, Eram Shakeel, Qazi M Sajid Jamal, Mohammad A Kamal, Usman Sayeed, Mohammad K A Khan, Mohammad H Siddiqui, Jamal M Arif, Salman Akhtar
BACKGROUND: Designing a novel antagonist against VEGFR-2 is being applied currently to inhibit cancer growth and metastasis. Because of the unexpected side effects incurred by the contemporary anticancer medications, the focus has been laid towards identifying natural compounds that might carry the potential to inhibit tumor progression. VEGR-2 remains an important target for anticancer drug development as it is the master regulator of vascular growth. OBJECTIVE: The study focuses on virtual screening of compounds from plants of Asteraceae family that bears antiangiogenic potential and thus, inhibiting VEGFR-2 using a computational approach...
April 16, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29662021/roles-of-polyploid-multinucleated-giant-cancer-cells-in-metastasis-and-disease-relapse-following-anticancer-treatment
#17
Razmik Mirzayans, Bonnie Andrais, David Murray
Tumors and tumor-derived cell lines contain polyploid giant cells with significantly elevated genomic content, often with multiple nuclei. The frequency of giant cells can increase markedly following anticancer treatment. Although giant cells enter a dormant phase and therefore do not form macroscopic colonies (aggregates of ≥50 cells) in the conventional in vitro colony formation assay, they remain viable and metabolically active. The purpose of this commentary is to underscore the potential importance of polyploid/multinucleated giant cells in metastasis and cancer recurrence following exposure to anticancer agents...
April 15, 2018: Cancers
https://www.readbyqxmd.com/read/29659166/strategies-to-improve-tumor-penetration-of-nanomedicines-through-nanoparticle-design
#18
REVIEW
Ya-Ru Zhang, Run Lin, Hong-Jun Li, Wei-Ling He, Jin-Zhi Du, Jun Wang
Nanoparticles (NPs) have emerged as an effective means to deliver therapeutic drugs for cancer treatment, as they can preferentially accumulate at tumor site through the enhanced permeability and retention effect. Various forms of NPs including liposomes, polymeric micelles, and inorganic particles have been used for therapeutic applications. However, the therapeutic benefits of nanomedicines are suboptimal. Although many possible reasons may account for the compromised therapeutic efficacy, the inefficient tumor penetration can be a vital obstacle...
April 16, 2018: Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology
https://www.readbyqxmd.com/read/29657856/collaborative-academic-medical-product-development-an-8-year-review-of-commercialization-outcomes-at-the-institute-of-translational-health-sciences
#19
Lynn M Rose, Fiona Wills, Connie Bourassa-Shaw, Terri L Butler, Jeanette Griscavage Ennis, Kim Emmons, Patrick Shelby, Meher Antia, Kim Folger Bruce
Introduction: The Institute of Translational Health Sciences (ITHS), a Clinical and Translational Science Award (CTSA)-funded program at the University of Washington (UW), established the Drug and Device Advisory Committee (DDAC) to provide product-specific scientific and regulatory mentoring to investigators seeking to translate their discoveries into medical products. An 8-year retrospective analysis was undertaken to evaluate the impact of the DDAC programs on commercialization metrics...
August 2017: Journal of Clinical and Translational Science
https://www.readbyqxmd.com/read/29656203/an-overview-of-quinazolines-pharmacological-significance-and-recent-developments
#20
REVIEW
V Alagarsamy, K Chitra, G Saravanan, V Raja Solomon, M T Sulthana, B Narendhar
Most of the drugs and pharmacologically relevant molecules possess heterocyclic ring structures and presence of hetero atoms or groupings divulges privileged specificities in their pharmacological targets. Especially the heterocyclic systems, quinazoline is a biologically imperative scaffold known to be linked with several pharmacological activities. Some of the protuberant pharmacological responses attributed to this system are analgesic, anti-inflammatory, anti-convulsant, sedative-hypnotic, anti-histaminic, anti-hypertensive, anti-cancer, anti-microbial, anti-tubercular and anti-viral activities...
March 30, 2018: European Journal of Medicinal Chemistry
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