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https://www.readbyqxmd.com/read/29303993/endolysosomal-cation-channels-and-cancer-a-link-with-great-potential
#1
REVIEW
Christian Grimm, Karin Bartel, Angelika M Vollmar, Martin Biel
The endolysosomal system (ES) consists of lysosomes; early, late, and recycling endosomes; and autophagosomes. It is a key regulator not only of macromolecule degradation and recycling, plasma membrane repair, homeostasis, and lipid storage, but also of antigen presentation, immune defense, cell motility, cell death signaling, tumor growth, and cancer progression. In addition, it plays a critical role in autophagy, and the autophagy-lysosome pathway is intimately associated with the hallmarks of cancer, such as escaping cell death pathways, evading immune surveillance, and deregulating metabolism...
January 5, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29301331/antimicrobial-and-antibiofilm-activity-of-up-5-an-ultrashort-antimicrobial-peptide-designed-using-only-arginine-and-biphenylalanine
#2
Ammar Almaaytah, Mohammed T Qaoud, Gubran Khalil Mohammed, Ahmad Abualhaijaa, Daniel Knappe, Ralf Hoffmann, Qosay Al-Balas
The recent upsurge of multidrug resistant bacteria (MDRB) among global communities has become one of the most serious challenges facing health professionals and the human population worldwide. Cationic ultrashort antimicrobial peptides (USAMPs) are a promising group of molecules that meet the required criteria of novel antimicrobial drug development. UP-5, a novel penta-peptide, displayed significant antimicrobial activities against various standard and clinical isolates of MDRB. UP-5 displayed MICs values within the range of (10-15 μM) and (55-65 μM) against Gram-positive and Gram-negative bacteria, respectively...
January 2, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29295496/roles-of-heat-shock-proteins-in-apoptosis-oxidative-stress-human-inflammatory-diseases-and-cancer
#3
REVIEW
Paul Chukwudi Ikwegbue, Priscilla Masamba, Babatunji Emmanuel Oyinloye, Abidemi Paul Kappo
Heat shock proteins (HSPs) play cytoprotective activities under pathological conditions through the initiation of protein folding, repair, refolding of misfolded peptides, and possible degradation of irreparable proteins. Excessive apoptosis, resulting from increased reactive oxygen species (ROS) cellular levels and subsequent amplified inflammatory reactions, is well known in the pathogenesis and progression of several human inflammatory diseases (HIDs) and cancer. Under normal physiological conditions, ROS levels and inflammatory reactions are kept in check for the cellular benefits of fighting off infectious agents through antioxidant mechanisms; however, this balance can be disrupted under pathological conditions, thus leading to oxidative stress and massive cellular destruction...
December 23, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29267190/2017-a-fruitful-year-for-pharmaceuticals
#4
EDITORIAL
Jean Jacques Vanden Eynde
First of all, let me wish you a healthy and wonderful year in 2018 [...].
December 21, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29258264/convenient-preparation-of-18f-labeled-peptide-probes-for-potential-claudin-4-pet-imaging
#5
Lucia Feni, M Aymen Omrane, Moritz Fischer, Boris D Zlatopolskiy, Bernd Neumaier, Ines Neundorf
Since pancreatic cancer is often diagnosed in a late state of cancer development, diagnostic opportunities allowing early disease detection are highly sought after. As such, cancer expression of claudin proteins is markedly dysregulated, making it an attractive target for molecular imaging like positron emission tomography (PET). Claudins are a family of transmembrane proteins that have a pivotal role as members of the tight junctions. In particular, claudin-3 and claudin-4 are frequently overexpressed in pancreatic cancer...
December 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29240701/25th-conference-of-gp2a
#6
Michael D Threadgill, Susan E Matthews, Francesca Giuntini
The 25th Conference of GP2A was held on 31 August and 1 September 2017 in Liverpool, UK, with the aim of exchange of ideas and experience, particularly amongst young medicinal chemists. Topics included bioactive compounds from plants and lichens, and design and development of drugs. Abstracts of invited lectures, proffered oral presentations, flash presentations and posters presented during the meeting are collected in this report.
December 14, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29236079/unexpected-binding-mode-of-a-potent-indeno-1-2-b-indole-type-inhibitor-of-protein-kinase-ck2-revealed-by-complex-structures-with-the-catalytic-subunit-ck2%C3%AE-and-its-paralog-ck2%C3%AE
#7
Jennifer Hochscherf, Dirk Lindenblatt, Benedict Witulski, Robin Birus, Dagmar Aichele, Christelle Marminon, Zouhair Bouaziz, Marc Le Borgne, Joachim Jose, Karsten Niefind
Protein kinase CK2, a member of the eukaryotic protein kinase superfamily, is associated with cancer and other human pathologies and thus an attractive drug target. The indeno[1,2-b]indole scaffold is a novel lead structure to develop ATP-competitive CK2 inhibitors. Some indeno[1,2-b]indole-based CK2 inhibitors additionally obstruct ABCG2, an ABC half transporter overexpressed in breast cancer and co-responsible for drug efflux and resistance. Comprehensive derivatization studies revealed substitutions of the indeno[1,2-b]indole framework that boost either the CK2 or the ABCG2 selectivity or even support the dual inhibition potential...
December 13, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29231857/biodegradable-scaffolds-for-bone-regeneration-combined-with-drug-delivery-systems-in-osteomyelitis-therapy
#8
REVIEW
Rossella Dorati, Antonella DeTrizio, Tiziana Modena, Bice Conti, Francesco Benazzo, Giulia Gastaldi, Ida Genta
A great deal of research is ongoing in the area of tissue engineering (TE) for bone regeneration. A possible improvement in restoring damaged tissues involves the loading of drugs such as proteins, genes, growth factors, antibiotics, and anti-inflammatory drugs into scaffolds for tissue regeneration. This mini-review is focused on the combination of the local delivery of antibiotic agents with bone regenerative therapy for the treatment of a severe bone infection such as osteomyelitis. The review includes a brief explanation of scaffolds for bone regeneration including scaffolds characteristics and types, a focus on severe bone infections (especially osteomyelitis and its treatment), and a literature review of local antibiotic delivery by the combination of scaffolds and drug-delivery systems...
December 12, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29232822/microglia-m2a-polarization-as-potential-link-between-food-allergy-and-autism-spectrum-disorders
#9
REVIEW
Hans O Kalkman, Dominik Feuerbach
Atopic diseases are frequently co-morbid with autism spectrum disorders (ASD). Allergic responses are associated with an activation of mast cells, innate lymphoid cells, and Th2 cells. These cells produce type-2 cytokines (IL4 and IL13), which stimulate microglia and macrophages to adopt a phenotype referred to as 'alternative activation' or 'M2A'. M2A-polarized macrophages and microglia play a physiological role in tissue repair by secreting growth factors such as brain-derived neurotrophic factor (BDNF) and insulin-like growth factor-1...
December 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29207523/31i%C3%A3-mes-journ%C3%A3-es-franco-belges-de-pharmacochimie-meeting-report
#10
Raphaël Frédérick, Lionel Pochet, Pascal De Tullio, François Dufrasne
The "Journées Franco-Belges de Pharmacochimie" is a recognized two-day annual meeting on Medicinal Chemistry that is renowned for the advanced science presented, conviviality, and outstanding opportunities for senior and young scientists to exchange knowledge. Abstracts of plenary lectures, oral communications, and posters presented during the meeting are collected in this report.
December 4, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29182533/early-gabapentin-treatment-during-the-latency-period-increases-convulsive-threshold-reduces-microglial-activation-and-macrophage-infiltration-in-the-lithium-pilocarpine-model-of-epilepsy
#11
Alicia Rossi, Veronica Murta, Jerónimo Auzmendi, Alberto Javier Ramos
The lithium-pilocarpine model of epilepsy reproduces several features of temporal lobe epilepsy in humans, including the chronological timeline of an initial latency period followed by the development of spontaneous seizures. Epilepsy therapies in humans are implemented, as a rule, after the onset of the spontaneous seizures. We here studied the potential effect on epileptogenesis of starting an early treatment during the latency period, in order to prevent the development of spontaneous seizures. Adult male Wistar rats were treated with 3 mEq/kg LiCl, and 20 h later 30 mg/kg pilocarpine...
November 28, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29160846/a-triphenylphosphonium-functionalized-mitochondriotropic-nanocarrier-for-efficient-co-delivery-of-doxorubicin-and-chloroquine-and-enhanced-antineoplastic-activity
#12
Katerina N Panagiotaki, Zili Sideratou, Spiros A Vlahopoulos, Maria Paravatou-Petsotas, Michael Zachariadis, Nikolas Khoury, Vassilis Zoumpourlis, Dimitris Tsiourvas
Drug delivery systems that target subcellular organelles and, in particular, mitochondria are considered to have great potential in treating disorders that are associated with mitochondrial dysfunction, including cancer or neurodegenerative diseases. To this end, a novel hyperbranched mitochondriotropic nanocarrier was developed for the efficient co-delivery of two different (both in chemical and pharmacological terms) bioactive compounds. The carrier is based on hyperbranched poly(ethyleneimine) functionalized with triphenylphosphonium groups that forms ~100 nm diameter nanoparticles in aqueous media and can encapsulate doxorubicin (DOX), a well-known anti-cancer drug, and chloroquine (CQ), a known chemosensitizer with arising potential in anticancer medication...
November 21, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29156606/synthesis-and-in-vitro-cytotoxicity-of-the-4-halogenoanilino-6-bromoquinazolines-and-their-6-4-fluorophenyl-substituted-derivatives-as-potential-inhibitors-of-epidermal-growth-factor-receptor-tyrosine-kinase
#13
Malose Jack Mphahlele, Hugues K Paumo, Yee Siew Choong
Series of the 2-unsubstituted and 2-(4-chlorophenyl)-substituted 4-anilino-6-bromoquinazolines and their 6-(4-fluorophenyl)-substituted derivatives were evaluated for in vitro cytotoxicity against MCF-7 and HeLa cells. The 2-unsubstituted 4-anilino-6-bromoquinazolines lacked activity, whereas most of their 2-(4-chlorophenyl) substituted derivatives were found to exhibit significant cytotoxicity and selectivity against HeLa cells. Replacement of bromine with 4-fluorophenyl group for the 2-unsubstituted 4-anilinoquinazolines resulted in superior activity against HeLa cells compared to Gefitinib...
November 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29144442/propagation-of-fibrillar-structural-forms-in-proteins-stopped-by-naturally-occurring-short-polypeptide-chain-fragments
#14
Irena Roterman, Mateusz Banach, Leszek Konieczny
Amyloids characterized by unbounded growth of fibrillar structures cause many pathological processes. Such unbounded propagation is due to the presence of a propagating hydrophobicity field around the fibril's main axis, preventing its closure (unlike in globular proteins). Interestingly, similar fragments, commonly referred to as solenoids, are present in many naturally occurring proteins, where their propagation is arrested by suitably located "stopper" fragments. In this work, we analyze the distribution of hydrophobicity in solenoids and in their corresponding "stoppers" from the point of view of the fuzzy oil drop model (called FOD in this paper)...
November 16, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29120370/amorphous-solid-dispersion-of-epigallocatechin-gallate-for-enhanced-physical-stability-and-controlled-release
#15
Yizheng Cao, Jing Teng, Jon Selbo
Epigallocatechin gallate (EGCG) has been recognized as the most prominent green tea extract due to its healthy influences. The high instability and low bioavailability, however, strongly limit its utilization in food and drug industries. This work, for the first time, develops amorphous solid dispersion of EGCG to enhance its bioavailability and physical stability. Four commonly used polymeric excipients are found to be compatible with EGCG in water-dioxane mixtures via a stepwise mixing method aided by vigorous mechanical interference...
November 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29099084/essential-oils-and-antifungal-activity
#16
REVIEW
Filomena Nazzaro, Florinda Fratianni, Raffaele Coppola, Vincenzo De Feo
Since ancient times, folk medicine and agro-food science have benefitted from the use of plant derivatives, such as essential oils, to combat different diseases, as well as to preserve food. In Nature, essential oils play a fundamental role in protecting the plant from biotic and abiotic attacks to which it may be subjected. Many researchers have analyzed in detail the modes of action of essential oils and most of their components. The purpose of this brief review is to describe the properties of essential oils, principally as antifungal agents, and their role in blocking cell communication mechanisms, fungal biofilm formation, and mycotoxin production...
November 2, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29104261/neurochemical-changes-and-c-fos-mapping-in-the-brain-after-carisbamate-treatment-of-rats-subjected-to-lithium-pilocarpine-induced-status-epilepticus
#17
José Eduardo Marques-Carneiro, Astrid Nehlig, Jean-Christophe Cassel, Eduardo Ferreira Castro-Neto, Julia Julie Litzahn, Anne Pereira de Vasconcelos, Maria da Graça Naffah-Mazacoratti, Maria José da Silva Fernandes
The administration of lithium-pilocarpine (LiPilo) in adult rats is a validated model reproducing the main clinical and neuropathological features of temporal lobe epilepsy (TLE). Previous studies have shown that carisbamate (CRS) has the property of modifying epileptogenesis in this model. When treated with CRS, about 50% of rats undergoing LiPilo status epilepticus (SE) develop non-convulsive seizures (NCS) instead of convulsive ones (commonly observed in TLE). The goal of this work was to determine some of the early changes that occur after CRS administration, as they could be involved in the insult- and epileptogenesis-modifying effects of CRS...
November 1, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29088082/acorenone-b-ache-and-bche-inhibitor-as-a-major-compound-of-the-essential-oil-distilled-from-the-ecuadorian-species-niphogeton-dissecta-benth-j-f-macbr
#18
James Calva, Nicole Bec, Gianluca Gilardoni, Christian Larroque, Luis Cartuche, Carlo Bicchi, José Vinicio Montesinos
This study investigated the chemical composition, physical proprieties, biological activity, and enantiomeric analysis of the essential oil from the aerial parts of Niphogeton dissecta (culantrillo del cerro) from Ecuador, obtained by steam distillation. The qualitative and quantitative analysis of the essential oil was realized by gas chromatographic and spectroscopic techniques (GC-MS and GC-FID). Acorenone B was identified by GC-MS and NMR experiments. The enantiomeric distribution of some constituents has been assessed by enantio-GC through the use of a chiral cyclodextrin-based capillary column...
October 31, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29064422/systemic-interleukin-4-administration-after-spinal-cord-injury-modulates-inflammation-and-promotes-neuroprotection
#19
Rui Lima, Susana Monteiro, José P Lopes, Pedro Barradas, Natália L Vasconcelos, Eduardo D Gomes, Rita C Assunção-Silva, Fábio G Teixeira, Mónica Morais, Nuno Sousa, António J Salgado, Nuno A Silva
Traumatic spinal cord injury (SCI) causes dramatic disability and dysfunction in the motor, sensory and autonomic systems. The severe inflammatory reaction that occurs after SCI is strongly associated with further tissue damage. As such, immunomodulatory strategies have been developed, aimed at reducing inflammation, but also at shaping the immune response in order to protect, repair and promote regeneration of spared neural tissue. One of those promising strategies is the intraspinal administration of the cytokine interleukin-4 (IL-4) that was shown to promote a phenotype on specific immune cells associated with neuroprotection and repair...
October 24, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29053577/electrographic-changes-accompanying-recurrent-seizures-under-ketogenic-diet-treatment
#20
Chiara Lucchi, Maddalena Marchiò, Elisa Caramaschi, Carmela Giordano, Rocco Giordano, Azzurra Guerra, Giuseppe Biagini
The ketogenic diet (KD) is increasingly used to treat epilepsy refractory to antiepileptic drugs and other neurological disorders. In animal models, the KD was found to increase the threshold to seizures induced by different convulsive stimulations. However, in models in which suprathreshold stimuli were used, a paradoxical seizure worsening was consistently observed in KD-fed animals. To better define this phenomenon, we characterized the electrographic response to seizures induced in mice which were treated with the KD, and then corneally stimulated at 6-Hz in four different sessions...
October 20, 2017: Pharmaceuticals
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