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https://www.readbyqxmd.com/read/28822237/beyond-genomics-targeting-the-epigenome-in-diffuse-large-b-cell-lymphoma
#1
REVIEW
Andrea Kühnl, David Cunningham, Ian Chau
After decades of intense research on genetic alterations in cancer and successful implementation of genetically-based targeted therapies, the field of cancer epigenetics is only beginning to be fully recognized. The discovery of frequent mutations in genes modifying the epigenome in diffuse large B-cell lymphoma (DLBCL) has highlighted the outstanding role of epigenetic deregulation in this disease. Identification of epigenetically-driven DLBCL subgroups and development of novel epigenetic drugs have rapidly advanced...
August 9, 2017: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/28822145/-advances-in-studies-on-autoimmune-diseases-treated-by-halofuginone
#2
REVIEW
Shi-Qi Wang, Ze-Hua Duan, Ya-Rong Zhao, Huan Dou
Halofuginone (HF) is a derivative of dichroine which is the extract of traditional Chinese medicine. It is widely used as an efficient anticoccidial drug. Recent studies have found that HF has unique biological activities, showing great potential capacities in the treatment of autoimmune diseases. In the article, we summarized the therapeutic effects of HF in a variety of autoimmune diseases and its mechanism, providing references for further clinical studies of HF.
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28822103/current-progress-in-innovative-engineered-antibodies
#3
REVIEW
William R Strohl
As of May 1, 2017, 74 antibody-based molecules have been approved by a regulatory authority in a major market. Additionally, there are 70 and 575 antibody-based molecules in phase III and phase I/II clinical trials, respectively. These total 719 antibody-based clinical stage molecules include 493 naked IgGs, 87 antibody-drug conjugates, 61 bispecific antibodies, 37 total Fc fusion proteins, 17 radioimmunoglobulins, 13 antibody fragments, and 11 immunocytokines. New uses for these antibodies are being discovered each year...
August 18, 2017: Protein & Cell
https://www.readbyqxmd.com/read/28822076/studies-of-the-benzopyran-class-of-selective-cox-2-inhibitors-using-3d-qsar-and-molecular-docking
#4
Dharmendra K Yadav, Saloni, Praveen Sharma, Sanjeev Misra, Harpreet Singh, Ricardo L Mancera, Kang Kim, Cheongyun Jang, Mi-Hyun Kim, Horacio Pérez-Sánchez, Eun Ha Choi, Surendra Kumar
The Gaussian-based 3D-QSAR studies for 58 selective COX-2 (cyclooxygenase-2) inhibitors belonging to benzopyran chemical class were performed. Partial least squares analysis produced statistically significant model with (R training(2)  = 0.866) and predictability (Q training(2)  = 0.66, Q test(2)  = 0.846). The 3D-QSAR model includes steric, electrostatic, hydrophobic, and hydrogen bond acceptor field indicators, whereas the potential field contributions indicate that the steric and hydrophobic features of the molecules play an important role in governing their biological activity...
August 18, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28821941/rheumatologic-care-of-nursing-home-residents-with-rheumatoid-arthritis-a-comparison-of-the-year-before-and-after-nursing-home-admission
#5
Andres Luque Ramos, Katinka Albrecht, Angela Zink, Falk Hoffmann
The purpose of this study was to investigate health care for patients with rheumatoid arthritis (RA) before and after admission to nursing homes. Data of a German health insurance fund from persons with diagnostic codes of RA, aged ≥65 years, admitted to a nursing home between 2010 and 2014 and continuously insured 1 year before and after admission were used. The proportion of patients with ≥1 rheumatologist visit and ≥1 prescription of biologic or conventional synthetic disease-modifying antirheumatic drugs (bDMARDs or csDMARDs), glucocorticoids and non-steroidal anti-inflammatory drugs (NSAIDs) in the year before and after admission were calculated...
August 18, 2017: Rheumatology International
https://www.readbyqxmd.com/read/28821079/highly-monodisperse-colloidal-coacervates-based-on-a-bioactive-lactose-modified-chitosan-from-synthesis-to-characterization
#6
Franco Furlani, Pasquale Sacco, Eleonora Marsich, Ivan Donati, Sergio Paoletti
The present contribution aims at describing the fabrication of coacervates in the nano-size range starting from a 1-deoxylactit-1-yl chitosan (in this manuscript termed as CTL60) and the multivalent anion tripolyphosphate (TPP). Colloidal coacervates have been obtained for precise values of the molar ratio of TPP to CTL60 repeating unit. Coacervation is ensured only at pH 4.5 and not at 7.4, thus demonstrating the key role of electrostatic interactions in the stabilization of the coacervates. At a variance with chitosan, CTL60 favors the formation of highly homogeneous coacervates with very low values of the polydispersity index (PDI)...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28821011/the-photodynamic-action-of-pheophorbide-a-induces-cell-death-through-oxidative-stress-in-leishmania-amazonensis
#7
Nathielle Miranda, Hélito Volpato, Jean Henrique da Silva Rodrigues, Wilker Caetano, Tânia Ueda-Nakamura, Sueli de Oliveira Silva, Celso Vataru Nakamura
Leishmaniasis is a disease caused by hemoflagellate protozoa, affecting millions of people worldwide. The difficulties of treating patients with this parasitosis include the limited efficacy and many side effects of the currently available drugs. Therefore, the search for new compounds with leishmanicidal action is necessary. Photodynamic therapy has been studied in the medical field because of its selectivity, utilizing a combination of visible light, a photosensitizer compound, and singlet oxygen to reach the area of treatment...
August 11, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28820879/a-kinetic-view-of-gpcr-allostery-and-biased-agonism
#8
J Robert Lane, Lauren T May, Robert G Parton, Patrick M Sexton, Arthur Christopoulos
G-protein-coupled receptors (GPCRs) are one of the most tractable classes of drug targets. These dynamic proteins can adopt multiple active states that are linked to distinct functional outcomes. Such states can be differentially stabilized by ligands interacting with the endogenous agonist-binding orthosteric site and/or by ligands acting via spatially distinct allosteric sites, leading to the phenomena of 'biased agonism' or 'biased modulation'. These paradigms are having a major impact on modern drug discovery, but it is becoming increasingly apparent that 'kinetic context', at the level of both ligand-receptor and receptor-signal pathway kinetics, can have a profound impact on the observation and quantification of these phenomena...
August 18, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/28820585/chemo-enzymatic-assembly-of-isotopically-labeled-folates
#9
Antonio Angelastro, William Michael Dawson, Louis Y P Luk, E Joel Loveridge, Rudolf K Allemann
Pterin-containing natural products have diverse functions in life but an efficient and easy scheme for their in vitro synthesis is not available. Here, we report a chemo-enzymatic 14-step, one-pot synthesis that can be used to generate 13C- and 15N-labeled dihydrofolates (H2F) from glucose, guanine and p-aminobenzoyl-L-glutamic acid. This synthesis stands out from previous approaches to produce H2F in that the average yield of each step is >91% and it requires only one single purification step. The use of a one-pot reaction allowed us to overcome potential problems with individual steps during the synthesis...
August 18, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28820568/enhanced-drug-delivery-into-cell-cytosol-via-glycoprotein-h-derived-peptide-conjugated-nanoemulsions
#10
Teresa Fotticchia, Raffaele Vecchione, Pasqualina Liana Scognamiglio, Daniela Guarnieri, Vincenzo Calcagno, Concetta Di Natale, Chiara Attanasio, Maria De Gregorio, Chiara Di Cicco, Vincenzo Quagliariello, Nicola Maurea, Antonio Barbieri, Luca Raiola, Rosario Vincenzo Iaffaioli, Paolo Antonio Netti
The key role of nanocarriers in improving the pharmacological properties of commonly used drugs is recognized worldwide. It is also known that in the development of new effective nanocarriers the use of targeting moieties integrated on their surface is essential. Herein, we propose a nanocarrier based on an oil in water nanoemulsion coated with a membranotropic peptide derived from the glycoprotein H of Herpes simplex virus 1, known as gH625, in order to reduce endo-lysosomal accumulation and to enhance cytosolic localization...
August 18, 2017: ACS Nano
https://www.readbyqxmd.com/read/28820471/metal-based-nanoparticles-for-the-treatment-of-infectious-diseases
#11
REVIEW
Blessing Atim Aderibigbe
Infectious diseases can be transmitted and they cause a significant burden on public health globally. They are the greatest world killers and it is estimated that they are responsible for the demise of over 17 million people annually. The impact of these diseases is greater in the developing countries. People with compromised immune systems and children are the most affected. Infectious diseases may be caused by bacteria, viruses, and protozoa. The treatment of infectious diseases is hampered by simultaneous resistance to multiple drugs, indicating that there is a serious and pressing need to develop new therapeutics that can overcome drug resistance...
August 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28820058/editorial-neurodegenerative-disorders-synthesis-drug-delivery-strategies-and-biological-evaluation-of-new-therapeutic-agents
#12
EDITORIAL
Antonio Di Stefano, Marcella Reale
No abstract text is available yet for this article.
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28820054/qsar-modeling-of-histamine-h3r-antagonists-inverse-agonists-as-future-drugs-for-neurodegenerative-diseases
#13
Michelle Fidelis Corrêa, João Paulo Dos Santos Fernandes
Histamine H3 receptor (H3R) is associated with several neuropsychological diseases. It is predominantly expressed in the central nervous system as presynaptic receptor, especially in regions associated with cognition and behavior, and is responsible for modulate the synthesis and release of histamine and other neurotransmitters such as acetylcholine, dopamine and serotonin. Therefore, H3R is an important target involved in several CNS disorders, such as narcolepsy, attention deficit hyperactivity disorder and schizophrenia...
August 17, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28819706/generation-of-a-functional-humanized-delta-like-ligand-4-transgenic-mouse-model
#14
John Wiseman, Pernilla Gregersson, Johan Johansson, Kerstin Magnell, Fernanda Pilataxi, Chris Morehouse, Philip Brohawn, Nicholas Holoweckyj, Patrick Strout, Song Cho
Humanized mouse models are important tools in many areas of biological drug development including, within oncology research, the development of antagonistic antibodies that have the potential to block tumor growth by controlling vascularization and are key to the generation of in vivo proof-of-concept efficacy data. However, due to cross reactivity between human antibodies and mouse target such studies regularly require mouse models expressing only the human version of the target molecule. Such humanized knock-in/knock-out, KIKO, models are dependent upon the generation of homozygous mice expressing only the human molecule, compensating for loss of the mouse form...
August 17, 2017: Transgenic Research
https://www.readbyqxmd.com/read/28819560/a-novel-peptide-blocking-cancer-cell-invasion-by-structure-based-drug-design
#15
Yuki Yamada, Seiji Kanayama, Fuminori Ito, Noriyuki Kurita, Hiroshi Kobayashi
The receptor for the urokinase-type plasminogen activator (uPA), uPAR, facilitates tumor cell invasion and metastasis by focusing on several ligands, including uPA, integrins and vitronectin. With computational prediction algorithms and structure-based drug design, we identified peptides containing the Gly-Lys-Gly-Glu-Gly-Glu-Gly-Lys-Gly sequence (peptide H1), which strongly interacts with uPAR. The aim of the present study was to investigate the effect of allosteric inhibition at the uPAR interface using a novel synthetic peptide and its function on ovarian cancer cell invasion...
September 2017: Biomedical Reports
https://www.readbyqxmd.com/read/28819546/oxidative-stress-harms-and-benefits-for-human-health
#16
REVIEW
Gabriele Pizzino, Natasha Irrera, Mariapaola Cucinotta, Giovanni Pallio, Federica Mannino, Vincenzo Arcoraci, Francesco Squadrito, Domenica Altavilla, Alessandra Bitto
Oxidative stress is a phenomenon caused by an imbalance between production and accumulation of oxygen reactive species (ROS) in cells and tissues and the ability of a biological system to detoxify these reactive products. ROS can play, and in fact they do it, several physiological roles (i.e., cell signaling), and they are normally generated as by-products of oxygen metabolism; despite this, environmental stressors (i.e., UV, ionizing radiations, pollutants, and heavy metals) and xenobiotics (i.e., antiblastic drugs) contribute to greatly increase ROS production, therefore causing the imbalance that leads to cell and tissue damage (oxidative stress)...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28819441/vsv-based-virotherapy-in-ovarian-cancer-the-past-the-present-and-%C3%A2-future
#17
REVIEW
Beata Urszula Orzechowska, Marcin Jędryka, Katarzyna Zwolińska, Rafał Matkowski
The standard approach to treating patients with advanced epithelial ovarian cancer (EOC) after primary debulking surgery remains taxane and platinum-based chemotherapy. Despite treatment with this strategy, the vast majority of patients relapse and develop drug-resistant metastatic disease that may be driven by cancer stem cells (CSCs) or cancer initiating cells (CICs). Oncolytic viruses circumvent typical drug-resistance mechanisms, therefore they may provide a safe and effective alternative treatment for chemotherapy-resistant CSCs/CICs...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28819252/soft-electroporation-for-delivering-molecules-into-tightly-adherent-mammalian-cells-through-3d-hollow-nanoelectrodes
#18
Valeria Caprettini, Andrea Cerea, Giovanni Melle, Laura Lovato, Rosario Capozza, Jian-An Huang, Francesco Tantussi, Michele Dipalo, Francesco De Angelis
Electroporation of in-vitro cultured cells is widely used in biological and medical areas to deliver molecules of interest inside cells. Since very high electric fields are required to electroporate the plasma membrane, depending on the geometry of the electrodes the required voltages can be very high and often critical to cell viability. Furthermore, in traditional electroporation configuration based on planar electrodes there is no a priori certain feedback about which cell has been targeted and delivered and the addition of fluorophores may be needed to gain this information...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28819043/increased-acetylation-of-microtubules-rescues-human-tau-induced-microtubule-defects-and-neuromuscular-junction-abnormalities-in-drosophila
#19
Chuan-Xi Mao, Xue Wen, Shan Jin, Yong Q Zhang
Tau normally associates with and stabilizes microtubules (MTs), but is hyperphosphorylated and aggregated into neurofibrillary tangles in Alzheimer's disease and related neurodegenerative diseases, which are collectively known as tauopathies. MTs are regulated by different forms of post-translational modification including acetylation; acetylated MTs represent a more stable microtubule population. In our previous study, we show that inhibition of histone deacetylase 6 (HDAC6), which deacetylates tubulin at lysine 40, rescues defects in MTs and in neuromuscular junction growth caused by tau overexpression...
August 17, 2017: Disease Models & Mechanisms
https://www.readbyqxmd.com/read/28818953/new-horizons-for-precision-medicine-in-biliary-tract-cancers
#20
REVIEW
Juan W Valle, Angela Lamarca, Lipika Goyal, Jorge Barriuso, Andrew X Zhu
Biliary tract cancers (BTC), including cholangiocarcinoma and gallbladder cancer, are poor-prognosis and low-incidence cancers, although the incidence of intrahepatic cholangiocarcinoma is rising. A minority of patients present with resectable disease but relapse rates are high; benefit from adjuvant capecitabine chemotherapy has been demonstrated. Cisplatin/gemcitabine combination chemotherapy has emerged as the reference first-line treatment regimen; there is no standard second-line therapy. Selected patients may be suitable for liver-directed therapy (e...
August 17, 2017: Cancer Discovery
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