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Pharmaceuticals

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https://www.readbyqxmd.com/read/28106831/ablation-of-protein-kinase-ck2%C3%AE-in-skeletal-muscle-fibers-interferes-with-their-oxidative-capacity
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
https://www.readbyqxmd.com/read/28067769/identification-of-a-potent-allosteric-inhibitor-of-human-protein-kinase-ck2-by-bacterial-surface-display-library-screening
#7
Christian Nienberg, Claudia Garmann, Andreas Gratz, Andre Bollacke, Claudia Götz, Joachim Jose
Human protein kinase CK2 has emerged as promising target for the treatment of neoplastic diseases. The vast majority of kinase inhibitors known today target the ATP binding site, which is highly conserved among kinases and hence leads to limited selectivity. In order to identify non-ATP competitive inhibitors, a 12-mer peptide library of 6 × 10⁵ variants was displayed on the surface of E. coli by autodisplay. Screening of this peptide library on variants with affinity to CK2 was performed by fluorophore-conjugated CK2 and subsequent flow cytometry...
January 5, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28045438/d11-mediated-inhibition-of-protein-kinase-ck2-impairs-hif-1%C3%AE-mediated-signaling-in-human-glioblastoma-cells
#8
Susanne Schaefer, Tina H Svenstrup, Mette Fischer, Barbara Guerra
Compelling evidence indicates that protein kinase CK2 plays an important role in many steps of cancer initiation and progression, therefore, the development of effective and cell-permeable inhibitors targeting this kinase has become an important objective for the treatment of a variety of cancer types including glioblastoma. We have recently identified 1,3-dichloro-6-[(E)-((4-methoxyphenyl)imino)methyl]dibenzo(b,d)furan-2,7-diol (D11) as a potent and selective inhibitor of protein kinase CK2. In this study, we have further characterized this compound and demonstrated that it suppresses CK2 kinase activity by mixed type inhibition (KI 7...
January 1, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28036067/drosophila-protein-kinase-ck2-genetics-regulatory-complexity-and-emerging-roles-during-development
#9
REVIEW
Mohna Bandyopadhyay, Scott Arbet, Clifton P Bishop, Ashok P Bidwai
CK2 is a Ser/Thr protein kinase that is highly conserved amongst all eukaryotes. It is a well-known oncogenic kinase that regulates vital cell autonomous functions and animal development. Genetic studies in the fruit fly Drosophila are providing unique insights into the roles of CK2 in cell signaling, embryogenesis, organogenesis, neurogenesis, and the circadian clock, and are revealing hitherto unknown complexities in CK2 functions and regulation. Here, we review Drosophila CK2 with respect to its structure, subunit diversity, potential mechanisms of regulation, developmental abnormalities linked to mutations in the gene encoding CK2 subunits, and emerging roles in multiple aspects of eye development...
December 29, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/28036027/the-phosphorylation-of-pdx-1-by-protein-kinase-ck2-is-crucial-for-its-stability
#10
Sabrina Klein, Rui Meng, Mathias Montenarh, Claudia Götz
The homeodomain protein PDX-1 is a critical regulator of pancreatic development and insulin production in pancreatic β-cells. We have recently shown that PDX-1 is a substrate of protein kinase CK2; a multifunctional protein kinase which is implicated in the regulation of various cellular aspects, such as differentiation, proliferation, and survival. The CK2 phosphorylation site of PDX-1 is located within the binding region of the E3 ubiquitin ligase adaptor protein PCIF1. To study the interaction between PDX-1 and PCIF1 we used immunofluorescence analysis, co-immunoprecipitation, GST-pull-down studies, and proximity ligation assay (PLA)...
December 28, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/28036014/germinated-thai-black-rice-extract-protects-experimental-diabetic-rats-from-oxidative-stress-and-other-diabetes-related-consequences
#11
Chaiyavat Chaiyasut, Bhagavathi Sundaram Sivamaruthi, Noppawat Pengkumsri, Waranya Keapai, Periyanaina Kesika, Manee Saelee, Parichart Tojing, Sasithorn Sirilun, Khontaros Chaiyasut, Sartjin Peerajan, Narissara Lailerd
Background: Diabetes mellitus (DM), particularly type 2 DM (T2DM), is one of the most common metabolic disorder worldwide. The prevention measures and treatment strategies for DM are improving steadily. The current study explains the impact of germination on phytochemical content of Thai black rice (BR), and the influence of germinated BR extract (GBRE) supplementation on diabetic conditions in rats. Methods: BR was germinated and the phenolic, anthocyanin, and γ-aminobutyric acid (GABA) content of the extract were analyzed using HPLC and spectrophotometric methods...
December 28, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/28035950/progress-confirmed-for-pharmaceuticals-in-2016
#12
EDITORIAL
Jean Jacques Vanden Eynde
n/a.
December 26, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/28009816/the-new-role-for-an-old-kinase-protein-kinase-ck2-regulates-metal-ion-transport
#13
REVIEW
Adam J Johnson, Ming J Wu
The pleiotropic serine/threonine protein kinase CK2 was the first kinase discovered. It is renowned for its role in cell proliferation and anti-apoptosis. The complexity of this kinase is well reflected by the findings of past decades in terms of its heterotetrameric structure, subcellular location, constitutive activity and the extensive catalogue of substrates. With the advent of non-biased high-throughput functional genomics such as genome-wide deletion mutant screening, novel aspects of CK2 functionality have been revealed...
December 21, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/27999271/use-of-aptamers-as-diagnostics-tools-and-antiviral-agents-for-human-viruses
#14
REVIEW
Víctor M González, M Elena Martín, Gerónimo Fernández, Ana García-Sacristán
Appropriate diagnosis is the key factor for treatment of viral diseases. Time is the most important factor in rapidly developing and epidemiologically dangerous diseases, such as influenza, Ebola and SARS. Chronic viral diseases such as HIV-1 or HCV are asymptomatic or oligosymptomatic and the therapeutic success mainly depends on early detection of the infective agent. Over the last years, aptamer technology has been used in a wide range of diagnostic and therapeutic applications and, concretely, several strategies are currently being explored using aptamers against virus proteins...
December 16, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/27983625/trp-channels-in-skin-biology-and-pathophysiology
#15
REVIEW
Michael J Caterina, Zixuan Pang
Ion channels of the Transient Receptor Potential (TRP) family mediate the influx of monovalent and/or divalent cations into cells in response to a host of chemical or physical stimuli. In the skin, TRP channels are expressed in many cell types, including keratinocytes, sensory neurons, melanocytes, and immune/inflammatory cells. Within these diverse cell types, TRP channels participate in physiological processes ranging from sensation to skin homeostasis. In addition, there is a growing body of evidence implicating abnormal TRP channel function, as a product of excessive or deficient channel activity, in pathological skin conditions such as chronic pain and itch, dermatitis, vitiligo, alopecia, wound healing, skin carcinogenesis, and skin barrier compromise...
December 14, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/27973417/applications-of-high-throughput-sequencing-for-in-vitro-selection-and-characterization-of-aptamers
#16
REVIEW
Nam Nguyen Quang, Gérald Perret, Frédéric Ducongé
Aptamers are identified through an iterative process of evolutionary selection starting from a random pool containing billions of sequences. Simultaneously to the amplification of high-affinity candidates, the diversity in the pool is exponentially reduced after several rounds of in vitro selection. Until now, cloning and Sanger sequencing of about 100 sequences was usually used to identify the enriched candidates. However, High-Throughput Sequencing (HTS) is now extensively used to replace such low throughput sequencing approaches...
December 10, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/27916867/methods-of-synthesis-properties-and-biomedical-applications-of-cuo-nanoparticles
#17
REVIEW
Madalina Elena Grigore, Elena Ramona Biscu, Alina Maria Holban, Monica Cartelle Gestal, Alexandru Mihai Grumezescu
This study aims to provide an updated survey of the main synthesis methods of copper oxide (CuO) nanoparticles in order to obtain tailored nanosystems for various biomedical applications. The synthesis approach significantly impacts the properties of such nanoparticles and these properties in turn have a significant impact on their biomedical applications. Although not widely investigated as an efficient drug delivery system, CuO nanoparticles have great biological properties including effective antimicrobial action against a wide range of pathogens and also drug resistant bacteria...
November 30, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/27898030/assessment-of-the-activity-of-tigecycline-against-gram-positive-and-gram-negative-organisms-collected-from-italy-between-2012-and-2014-as-part-of-the-tigecycline-evaluation-and-surveillance-trial-t-e-s-t
#18
Stefania Stefani, Michael J Dowzicky
As part of the Tigecycline Evaluation and Surveillance Trial (T.E.S.T) we report the in vitro activity of tigecycline and its comparators against Gram-negative and Gram-positive organisms collected from Italian centers between 2012 and 2014. Minimum inhibitory concentrations were determined according to the broth microdilution methodology of the Clinical and Laboratory Standards Institute, and antimicrobial resistance was determined using the European Committee on Antimicrobial Susceptibility Testing interpretive criteria...
November 26, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/27869720/30i%C3%A3-mes-journ%C3%A3-es-franco-belges-de-pharmacochimie
#19
Samia Aci-Sèche, Frédéric Buron, Karen Plé, Laurent Robin, Franck Suzenet, Sylvain Routier
The "Journées Franco-Belges de Pharmacochimie" is a recognized annual meeting in organic and medicinal chemistry known for the quality of scientific exchange and conviviality. Young researchers were encouraged to present their work and share ideas with senior scientists. Abstracts of plenary lectures, oral communications, and posters presented during the meeting are collected in this report.
November 18, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/27854251/nociceptive-trp-channels-sensory-detectors-and-transducers-in-multiple-pain-pathologies
#20
REVIEW
Aaron D Mickle, Andrew J Shepherd, Durga P Mohapatra
Specialized receptors belonging to the transient receptor potential (TRP) family of ligand-gated ion channels constitute the critical detectors and transducers of pain-causing stimuli. Nociceptive TRP channels are predominantly expressed by distinct subsets of sensory neurons of the peripheral nervous system. Several of these TRP channels are also expressed in neurons of the central nervous system, and in non-neuronal cells that communicate with sensory nerves. Nociceptive TRPs are activated by specific physico-chemical stimuli to provide the excitatory trigger in neurons...
November 14, 2016: Pharmaceuticals
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