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Pharmaceuticals

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https://www.readbyqxmd.com/read/28230733/ck2-molecular-targeting-tumor-cell-specific-delivery-of-rnai-in-various-models-of-cancer
#1
REVIEW
Janeen H Trembley, Betsy T Kren, Md Joynal Abedin, Rachel I Vogel, Claire M Cannon, Gretchen M Unger, Khalil Ahmed
Protein kinase CK2 demonstrates increased protein expression relative to non-transformed cells in the majority of cancers that have been examined. The elevated levels of CK2 are involved in promoting not only continued proliferation of cancer cells but also their resistance to cell death; thus, CK2 has emerged as a plausible target for cancer therapy. Our focus has been to target CK2 catalytic subunits at the molecular level using RNA interference (RNAi) strategies to achieve their downregulation. The delivery of oligonucleotide therapeutic agents warrants that they are protected and are delivered specifically to cancer cells...
February 21, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28230762/the-development-of-ck2-inhibitors-from-traditional-pharmacology-to-in-silico-rational-drug-design
#2
REVIEW
Giorgio Cozza
Casein kinase II (CK2) is an ubiquitous and pleiotropic serine/threonine protein kinase able to phosphorylate hundreds of substrates. Being implicated in several human diseases, from neurodegeneration to cancer, the biological roles of CK2 have been intensively studied. Upregulation of CK2 has been shown to be critical to tumor progression, making this kinase an attractive target for cancer therapy. Several CK2 inhibitors have been developed so far, the first being discovered by "trial and error testing". In the last decade, the development of in silico rational drug design has prompted the discovery, de novo design and optimization of several CK2 inhibitors, active in the low nanomolar range...
February 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28208677/targeting-protein-kinase-ck2-evaluating-cx-4945-potential-for-gl261-glioblastoma-therapy-in-immunocompetent-mice
#3
Laura Ferrer-Font, Lucia Villamañan, Nuria Arias-Ramos, Jordi Vilardell, Maria Plana, Maria Ruzzene, Lorenzo A Pinna, Emilio Itarte, Carles Arús, Ana Paula Candiota
Glioblastoma (GBM) causes poor survival in patients even with aggressive treatment. Temozolomide (TMZ) is the standard chemotherapeutic choice for GBM treatment but resistance always ensues. Protein kinase CK2 (CK2) contributes to tumour development and proliferation in cancer, and it is overexpressed in human GBM. Accordingly, targeting CK2 in GBM may benefit patients. Our goal has been to evaluate whether CK2 inhibitors (iCK2s) could increase survival in an immunocompetent preclinical GBM model. Cultured GL261 cells were treated with different iCK2s including CX-4945, and target effects evaluated in vitro...
February 12, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28208634/rna-eluting-surfaces-for-the-modulation-of-gene-expression-as-a-novel-stent-concept
#4
Olivia Koenig, Diane Zengerle, Nadja Perle, Susanne Hossfeld, Bernd Neumann, Andreas Behring, Meltem Avci-Adali, Tobias Walker, Christian Schlensak, Hans Peter Wendel, Andrea Nolte
Presently, a new era of drug-eluting stents is continuing to improve late adverse effects such as thrombosis after coronary stent implantation in atherosclerotic vessels. The application of gene expression-modulating stents releasing specific small interfering RNAs (siRNAs) or messenger RNAs (mRNAs) to the vascular wall might have the potential to improve the regeneration of the vessel wall and to inhibit adverse effects as a new promising therapeutic strategy. Different poly (lactic-co-glycolic acid) (PLGA) resomers for their ability as an siRNA delivery carrier against intercellular adhesion molecule (ICAM)-1 with a depot effect were tested...
February 10, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28208768/inhibition-of-protein-kinase-ck2-prevents-adipogenic-differentiation-of-mesenchymal-stem-cells-like-c3h-10t1-2-cells
#5
Lisa Schwind, Sarah Schetting, Mathias Montenarh
Protein kinase CK2 as a holoenzyme is composed of two catalytic α- or α'-subunits and two non-catalytic β-subunits. Knock-out experiments revealed that CK2α and CK2β are required for embryonic development. Little is known about the role of CK2 during differentiation of stem cells. Mesenchymal stem cells (MSCs) are multipotent cells which can be differentiated into adipocytes in vitro. Thus, MSCs and in particular C3H/10T1/2 cells are excellent tools to study a possible role of CK2 in adipogenesis. We found downregulation of the CK2 catalytic subunits as well as a decrease in CK2 kinase activity with progression of differentiation...
February 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28178206/the-link-between-protein-kinase-ck2-and-atypical-kinase-rio1
#6
REVIEW
Konrad Kubiński, Maciej Masłyk
The atypical kinase Rio1 is widespread in many organisms, ranging from Archaebacteria to humans, and is an essential factor in ribosome biogenesis. Little is known about the protein substrates of the enzyme and small-molecule inhibitors of the kinase. Protein kinase CK2 was the first interaction partner of Rio1, identified in yeast cells. The enzyme from various sources undergoes CK2-mediated phosphorylation at several sites and this modification regulates the activity of Rio1. The aim of this review is to present studies of the relationship between the two different kinases, with respect to CK2-mediated phosphorylation of Rio1, regulation of Rio1 activity, and similar susceptibility of the kinases to benzimidazole inhibitors...
February 7, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28165359/in-search-of-small-molecule-inhibitors-targeting-the-flexible-ck2-subunit-interface
#7
Benoît Bestgen, Zakia Belaid-Choucair, Thierry Lomberget, Marc Le Borgne, Odile Filhol, Claude Cochet
Protein kinase CK2 is a tetrameric holoenzyme composed of two catalytic (α and/or α') subunits and two regulatory (β) subunits. Crystallographic data paired with fluorescence imaging techniques have suggested that the formation of the CK2 holoenzyme complex within cells is a dynamic process. Although the monomeric CK2α subunit is endowed with a constitutive catalytic activity, many of the plethora of CK2 substrates are exclusively phosphorylated by the CK2 holoenzyme. This means that the spatial and high affinity interaction between CK2α and CK2β subunits is critically important and that its disruption may provide a powerful and selective way to block the phosphorylation of substrates requiring the presence of CK2β...
February 3, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28146112/second-international-electronic-conference-on-medicinal-chemistry-ecmc-2
#8
Annie Mayence, Jean Jacques Vanden Eynde
The second International Electronic Conference on Medicinal Chemistry, organized and sponsored by the publisher MDPI AG and the Journal Pharmaceuticals, took place in November 2016 on the SciForum website (www.sciforum.net/conference/ecmc-12). More than 150 authors from 22 countries participated in the event. Selected works presented during the scientific meeting are disclosed in this report.
January 31, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28134851/barriers-to-the-access-of-bevacizumab-in-patients-with-solid-tumors-and-the-potential-impact-of-biosimilars-a-physician-survey
#9
Bradley J Monk, Philip E Lammers, Thomas Cartwright, Ira Jacobs
Access to bevacizumab, an important component of oncology treatment regimens, may be limited. This survey of oncologists in the US (n = 150), Europe (n = 230), and emerging markets (EM: Brazil, Mexico, and Turkey; n = 130) examined use of and barriers to accessing bevacizumab as treatment of advanced solid tumors. We also assessed the likelihood that physicians would prescribe a bevacizumab biosimilar, if available. Bevacizumab was frequently used as early-line therapy in metastatic colorectal cancer, metastatic non-squamous non-small-cell lung cancer, and metastatic ovarian cancer (all markets), and as a second-line therapy in glioblastoma multiforme (US, EM)...
January 28, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28134850/ck2-in-cancer-cellular-and-biochemical-mechanisms-and-potential-therapeutic-target
#10
REVIEW
Melissa M J Chua, Charina E Ortega, Ayesha Sheikh, Migi Lee, Hussein Abdul-Rassoul, Kevan L Hartshorn, Isabel Dominguez
CK2 genes are overexpressed in many human cancers, and most often overexpression is associated with worse prognosis. Site-specific expression in mice leads to cancer development (e.g., breast, lymphoma) indicating the oncogenic nature of CK2. CK2 is involved in many key aspects of cancer including inhibition of apoptosis, modulation of signaling pathways, DNA damage response, and cell cycle regulation. A number of CK2 inhibitors are now available and have been shown to have activity against various cancers in vitro and in pre-clinical models...
January 28, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28134835/-the-24th-conference-of-the-groupement-des-pharmacochimistes-de-l-arc-atlantique-gp2a
#11
Jean-Jacques Hélesbeux, Olivier Duval
The GP2A European Conference is a two-day meeting focused on medicinal chemistry and the use of tools to explore all fields of drug discovery and drug design such as molecular modelling, bioorganic chemistry, MS studies, in vitro in vivo assays, and structure activity relationships. Abstracts of keynote lectures, plenary lectures, junior lectures, flash presentations, and posters presented during the meeting are collated in this report.
January 28, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28125020/relationship-between-surface-properties-and-in-vitro-drug-release-from-compressed-matrix-containing-polymeric-materials-with-different-hydrophobicity-degrees
#12
Cristhian J Yarce, Juan D Echeverri, Mario A Palacio, Carlos A Rivera, Constain H Salamanca
This work is the continuation of a study focused on establishing relations between surface thermodynamic properties and in vitro release mechanisms using a model drug (ampicillin trihydrate), besides analyzing the granulometric properties of new polymeric materials and thus establishing the potential to be used in the pharmaceutical field as modified delivery excipients. To do this, we used copolymeric materials derived from maleic anhydride with decreasing polarity corresponding to poly(isobutylene-alt-maleic acid) (hydrophilic), sodium salt of poly(maleic acid-alt-octadecene) (amphiphilic), poly(maleic anhydride-alt-octadecene) (hydrophobic) and the reference polymer hydroxyl-propyl-methyl-cellulose (HPMC)...
January 24, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28117671/aptamers-in-bordeaux-24-25-june-2016
#13
Jean-Jacques Toulmé, Paloma H Giangrande, Günter Mayer, Beatrix Suess, Frédéric Ducongé, Bruce Sullenger, Vittorio de Franciscis, Fabien Darfeuille, Eric Peyrin
The symposium covered the many different aspects of the selection and the characterization of aptamers as well as their application in analytical, diagnostic and therapeutic areas. Natural and artificial riboswitches were discussed. Recent advances for the design of mutated polymerases and of chemically modified nucleic acid bases that provide aptamers with new properties were presented. The power of aptamer platforms for multiplex analysis of biomarkers of major human diseases was described. The potential of aptamers for the treatment of cancer or cardiovascular diseases was also presented...
January 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28117670/exploring-the-ck2-paradox-restless-dangerous-dispensable
#14
REVIEW
Cinzia Franchin, Christian Borgo, Silvia Zaramella, Luca Cesaro, Giorgio Arrigoni, Mauro Salvi, Lorenzo A Pinna
The history of protein kinase CK2 is crowded with paradoxes and unanticipated findings. Named after a protein (casein) that is not among its physiological substrates, CK2 remained in search of its targets for more than two decades after its discovery in 1954, but it later came to be one of the most pleiotropic protein kinases. Being active in the absence of phosphorylation and/or specific stimuli, it looks unsuitable to participate in signaling cascades, but its "lateral" implication in a variety of signaling pathways is now soundly documented...
January 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28106831/ablation-of-protein-kinase-ck2%C3%AE-in-skeletal-muscle-fibers-interferes-with-their-oxidative-capacity
#15
Nane Eiber, Luca Simeone, Said Hashemolhosseini
The tetrameric protein kinase CK2 was identified playing a role at neuromuscular junctions by studying CK2β-deficient muscle fibers in mice, and in cultured immortalized C2C12 muscle cells after individual knockdown of CK2α and CK2β subunits. In muscle cells, CK2 activity appeared to be at least required for regular aggregation of nicotinic acetylcholine receptors, which serves as a hallmark for the presence of a postsynaptic apparatus. Here, we set out to determine whether any other feature accompanies CK2β-deficient muscle fibers...
January 19, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28106830/-188-re-v-nitrido-radiopharmaceuticals-for-radionuclide-therapy
#16
REVIEW
Alessandra Boschi, Petra Martini, Licia Uccelli
The favorable nuclear properties of rhenium-188 for therapeutic application are described, together with new methods for the preparation of high yield and stable (188)Re radiopharmaceuticals characterized by the presence of the nitride rhenium core in their final chemical structure. (188)Re is readily available from an (188)W/(188)Re generator system and a parallelism between the general synthetic procedures applied for the preparation of nitride technetium-99m and rhenium-188 theranostics radiopharmaceuticals is reported...
January 19, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28085026/structural-hypervariability-of-the-two-human-protein-kinase-ck2-catalytic-subunit-paralogs-revealed-by-complex-structures-with-a-flavonol-and-a-thieno-2-3-d-pyrimidine-based-inhibitor
#17
Karsten Niefind, Nils Bischoff, Andriy G Golub, Volodymyr G Bdzhola, Anatoliy O Balanda, Andriy O Prykhod'ko, Sergiy M Yarmoluk
Protein kinase CK2 is associated with a number of human diseases, among them cancer, and is therefore a target for inhibitor development in industry and academia. Six crystal structures of either CK2α, the catalytic subunit of human protein kinase CK2, or its paralog CK2α' in complex with two ATP-competitive inhibitors-based on either a flavonol or a thieno[2,3-d]pyrimidine framework-are presented. The structures show examples for extreme structural deformations of the ATP-binding loop and its neighbourhood and of the hinge/helix αD region, i...
January 11, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28075385/acknowledgement-to-reviewers-of-pharmaceuticals-in-2016
#18
EDITORIAL
Pharmaceuticals Editorial Office
The editors of Pharmaceuticals would like to express their sincere gratitude to the following reviewers for assessing manuscripts in 2016.
January 10, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28075359/development-of-pharmacophore-model-for-indeno-1-2-b-indoles-as-human-protein-kinase-ck2-inhibitors-and-database-mining
#19
Samer Haidar, Zouhair Bouaziz, Christelle Marminon, Tuomo Laitinen, Antti Poso, Marc Le Borgne, Joachim Jose
Protein kinase CK2, initially designated as casein kinase 2, is an ubiquitously expressed serine/threonine kinase. This enzyme, implicated in many cellular processes, is highly expressed and active in many tumor cells. A large number of compounds has been developed as inhibitors comprising different backbones. Beside others, structures with an indeno[1,2-b]indole scaffold turned out to be potent new leads. With the aim of developing new inhibitors of human protein kinase CK2, we report here on the generation of common feature pharmacophore model to further explain the binding requirements for human CK2 inhibitors...
January 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28067771/ck2-an-emerging-target-for-neurological-and-psychiatric-disorders
#20
REVIEW
Julia Castello, Andre Ragnauth, Eitan Friedman, Heike Rebholz
Protein kinase CK2 has received a surge of attention in recent years due to the evidence of its overexpression in a variety of solid tumors and multiple myelomas as well as its participation in cell survival pathways. CK2 is also upregulated in the most prevalent and aggressive cancer of brain tissue, glioblastoma multiforme, and in preclinical models, pharmacological inhibition of the kinase has proven successful in reducing tumor size and animal mortality. CK2 is highly expressed in the mammalian brain and has many bona fide substrates that are crucial in neuronal or glial homeostasis and signaling processes across synapses...
January 5, 2017: Pharmaceuticals
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