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https://www.readbyqxmd.com/read/27915186/role-of-the-purinergic-signaling-in-epilepsy
#1
REVIEW
Marek Cieślak, Andrzej Wojtczak, Michał Komoszyński
Adenine nucleotides and adenosine are signaling molecules that activate purinergic receptors P1 and P2. Activation of A1 adenosine receptors has an anticonvulsant action, whereas activation of A2A receptors might initiate seizures. Therefore, a significant limitation to the use of A1 receptor agonists as drugs in the CNS might be their peripheral side effects. The anti-epileptic activity of adenosine is related to its increased concentration outside the cell. This increase might result from the inhibition of the equilibrative nucleoside transporters (ENTs)...
September 22, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27915171/progress-in-the-development-of-%C3%AE-lactams-as-n-acylethanolamine-acid-amidase-naaa-inhibitors-synthesis-and-sar-study-of-new-potent-n-o-substituted-derivatives
#2
R Petracca, S Ponzano, S M Bertozzi, O Sasso, D Piomelli, T Bandiera, F Bertozzi
The anti-inflammatory effects resulting from raising the levels of palmitoylethanolamide (PEA), an endogenous bioactive lipid, led to envisage N-Acylethanolamine Acid Amidase (NAAA), the cysteine hydrolase mainly responsible for PEA degradation, as an attractive target for small molecule inhibitors. Previous work in our group identified serine-derived β-lactams as potent and systemically active inhibitors of NAAA activity. Aiming to expand the SAR study around this class of compounds, we investigated the effect of the substitution on the endocyclic nitrogen by designing and synthesizing a series of N-substituted β-lactams...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27915130/gamma-irradiation-enhanced-tollip-mediated-anti-inflammatory-action-through-structural-modification-of-quercetin-in-lipopolysaccharide-stimulated-macrophages
#3
Eui-Baek Byun, Beom-Su Jang, Hye-Min Kim, Mi-So Yang, Nak-Yun Sung, Eui-Hong Byun
The changes in molecular structure and anti-inflammatory action of a gamma-irradiated quercetin were examined. Quercetin was gamma-irradiated at doses of 0, 15, 30, 50, 100 and 150kGy, which induced new radiolytic peaks (the highest radiolytic peak at a dose of 30kGy). Treatment of intact- and gamma-irradiated quercetin did not induce a significant cellular toxicity of macrophages at concentrations ranging from 12.5 to 50μM. Treatment of LPS-stimulated macrophages with gamma-irradiated quercetin (30kGy) showed a higher inhibitory action than intact-quercetin groups in the excessive expression of inducible nitric oxide synthases-mediated nitric oxide, prostaglandin E2, pro-inflammatory cytokines level, such as tumor necrosis factor-α, interleukin-6 and interleukin-1β, reactive oxygen species, as well as cell surface molecules (CD80, CD86, and MHC class I/II)...
November 30, 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27915042/non-coding-rnas-and-berberine-a-new-mechanism-of-its-anti-diabetic-activities
#4
REVIEW
Wenguang Chang
Type 2 Diabetes (T2D) is a metabolic disease with high mortality and morbidity. Non-coding RNAs, including small and long non-coding RNAs, are a novel class of functional RNA molecules that regulate multiple biological functions through diverse mechanisms. Studies in the last decade have demonstrated that non-coding RNAs may represent compelling therapeutic targets and play important roles in regulating the course of insulin resistance and T2D. Berberine, a plant-based alkaloid, has shown promise as an anti-hyperglycaemic, anti-hyperlipidaemic agent against T2D...
November 30, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27915030/the-effect-of-anionic-dicephalic-surfactants-on-fabrication-of-varied-core-nanocarriers-for-sustained-release-of-porphyrin-photosensitizers
#5
Urszula Bazylińska, Renata Frąckowiak, Zbigniew Brzózka, Kazimiera A Wilk
Double-headed anionic surfactants could provide a profound group of efficient stabilizers of new template-mediated nanocarriers for effective encapsulation and sustained release of highly hydrophobic photosensitizers, and therefore their improved therapeutic activity in photodynamic therapy (PDT) protocols. We have thus encapsulated porphyrin-origin dyes, i.e., verteporfin (VP) and meso-tetraphenylporphyrin (TPP) in different types of sodium alkyliminobisacetates, Cn(COONa)2-stabilized nanosystems including biocompatible poly(l-glutamic acid)/poly(l-lysine) - PGA/PLL, multilayer nanocapsules (NCs)...
November 19, 2016: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/27915028/catalytic-synthesis-of-%C3%AE-amino-chromone-phosphonates-and-their-antimicrobial-toxicity-and-potential-hiv-1-rt-inhibitors-based-on-silico-screening
#6
Abosede Oluwabukola Jaiyeola, K Anand, K Kasumbwe, M Ramesh, R M Gengan
The α-amino phosphonates exhibit a wide range of biological properties which create demand for simple and efficient synthetic routes of new molecules. In this study synthesis of a new series of derivatives of α-amino chromone phosphonates (ACPs) was reported using RhBT catalyst. The RhBT was first prepared by simply mixing boron nitride in a solution of rhodium acetate, under inert atmosphere for a week followed by filtration (yield: 92%). The catalyst can be re-used for up to four times and showed minimal loss of activity...
November 23, 2016: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/27914999/dual-therapy-for-refractory-overactive-bladder-in-children-a-prospective-open-label-study
#7
Fannie Morin, Anne-Sophie Blais, Geneviève Nadeau, Katherine Moore, Lucie Genois, Stéphane Bolduc
PURPOSE: Mirabegron (β3-adrenoreceptor agonist) is a new molecule with a distinct mechanism of action from antimuscarinics. Combination therapy with solifenacin was recently studied in adult population. Our objective was to evaluate the efficacy and safety of mirabegron as add-on therapy, to treat urinary incontinence in children with idiopathic OAB, refractory/intolerant to antimuscarinics. MATERIALS AND METHODS: A prospective off-label study using add-on regimens of mirabegron was conducted with pediatric patients presenting no symptom improvement under intensive behavioural and medical therapies and/or significant side effects (S/E) on antimuscarinic dose escalation...
November 30, 2016: Journal of Urology
https://www.readbyqxmd.com/read/27914923/alloantigen-gene-transfer-to-hepatocytes-promotes-tolerance-to-pancreatic-islet-graft-by-inducing-cd8-regulatory-t-cells
#8
Valentin Le Guen, Jean-Paul Judor, Françoise Boeffard, Vanessa Gauttier, Nicolas Ferry, Jean-Paul Soulillou, Sophie Brouard, Sophie Conchon
BACKGROUND & AIM: Induction of donor-specific immune tolerance is a good alternative to chronic life-long immunosuppression for transplant patients. Donor major histocompatibility complex (MHC) molecules represent the main targets of the allogeneic immune response of transplant recipients. Liver-targeted gene transfer with viral vectors induces tolerance toward the encoded antigen. The aim of this work was to determine whether alloantigen gene transfer to hepatocytes induces tolerance and promotes graft acceptance...
November 30, 2016: Journal of Hepatology
https://www.readbyqxmd.com/read/27914888/the-first-report-on-transcriptome-analysis-of-the-venom-gland-of-iranian-scorpion-hemiscorpius-lepturus
#9
Fatemeh Kazemi-Lomedasht, Vahid Khalaj, Kamran Pooshang Bagheri, Mahdi Behdani, Delavar Shahbazzadeh
Hemiscorpius lepturus scorpion is one of the most venomous members of the Hemiscorpiidae family. H. lepturus is distributed in Iran, Iraq and Yemen. The prevalence and severity of scorpionism is high and health services are not able to control it. Scorpionism in Iran especially in the southern regions (Khuzestan, Sistan and Baluchestan, Hormozgan, Ilam) is one of the main health challenges. Due to the medical and health importance of scorpionism, the focus of various studies has been on the identification of H...
November 30, 2016: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/27914796/design-and-synthesis-of-new-piperidone-grafted-acetylcholinesterase-inhibitors
#10
Alireza Basiri, Michelle Xiao, Alec McCarthy, Debashis Dutta, Siddappa N Byrareddy, Martin Conda-Sheridan
Alzheimer's disease (AD) is a neurodegenerative disorder affecting 35million people worldwide. A common strategy to improve the well-being of AD patients consists on the inhibition of acetylcholinesterase with the concomitant increase of the neurotransmitter acetylcholine at cholinergic synapses. Two series of unreported N-benzylpiperidines 5(a-h) and thiazolopyrimidines 9(a-q) molecules were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) inhibitory activities. Among the newly synthesized compounds, 5h, 9h, 9j, and 9p displayed higher AChE enzyme inhibitory activities than the standard drug, galantamine, with IC50 values of 0...
November 24, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27914793/challenges-in-translational-development-of-pharmaceutical-cocrystals
#11
Dnyaneshwar P Kale, Sandeep S Zode, Arvind K Bansal
The last 2 decades have witnessed increased research in the area of cocrystals resulting in deeper scientific understanding, increase in intellectual property landscape, and evolution in the regulatory environment. Pharmaceutical cocrystals have received significant attention as a new solid form on account of their ability to modulate poor physicochemical properties of drug molecules. However, pharmaceutical development of cocrystals could be challenging, thus limiting their translation into viable drug products...
November 30, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27914362/an-overview-of-the-binding-models-of-fgfr-tyrosine-kinases-in-complex-with-small-molecule-inhibitors
#12
REVIEW
Weiyan Cheng, Mixiang Wang, Xin Tian, Xiaojian Zhang
The fibroblast growth factor receptor (FGFR) family receptor tyrosine kinase (RTK) includes four structurally related members, termed as FGFR1, FGFR2, FGFR3, and FGFR4. Given its intimate role in the progression of several solid tumors, excessive FGFR signaling provides an opportunity for anticancer therapy. Along with extensive pharmacological studies validating the therapeutic potential of targeting the FGFRs for cancer treatment, co-crystal structures of FGFRs/inhibitors are continuously coming up to study the mechanism of actions and explore new inhibitors...
November 25, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914048/geometric-potentials-for-computational-protein-sequence-design
#13
Jie Li, Patrice Koehl
Computational protein sequence design is the rational design based on computer simulation of new protein molecules to fold to target three-dimensional structures, with the ultimate goal of designing novel functions. It requires a good understanding of the thermodynamic equilibrium properties of the protein of interest. Here, we consider the contribution of the solvent to the stability of the protein. We describe implicit solvent models, focusing on approximations of their nonpolar components using geometric potentials...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27914004/hybrid-receptor-bound-mm-gbsa-per-residue-energy-based-pharmacophore-modelling-enhanced-approach-for-identification-of-selective-lta4h-inhibitors-as-potential-anti-inflammatory-drugs
#14
Patrick Appiah-Kubi, Mahmoud Soliman
Leukotriene A4 hydrolase has been identified as an enzyme with dual anti- and pro-inflammatory role, thus, the conversion of leukotriene to leukotriene B4 in the initiation stage of inflammation and the removal of the chemotactic Pro-Gly-Pro tripeptide. These findings make leukotriene A4 hydrolase an attractive drug target: suggesting an innovative approach towards the identification and design of novel class of compounds that can selectively inhibit leukotriene B4 synthesis while sparing the aminopeptidase activity...
December 2, 2016: Cell Biochemistry and Biophysics
https://www.readbyqxmd.com/read/27913739/structure-activity-relation-of-amor-sugar-molecule-that-activates-pollen-tubes-for-ovular-guidance
#15
Jiao Jiao, Akane G Mizukami, Subramanian Sankaranarayanan, Junichiro Yamguchi, Kenichiro Itami, Tetsuya Higashiyama
Successful fertilization in flowering plants depends on the precise directional growth control of pollen tube through the female pistil tissue, towards the female gametophyte contained in the ovule for delivery of non-motile sperm cells. Cysteine-rich peptides LUREs secreted from the synergid cells on either side of the egg cell act as ovular attractants of pollen tubes. Competency control by the pistil is crucial for the response of pollen tubes to these ovular attractants. We recently reported that ovular 4-O-methyl-glucuronosyl arabinogalactan AMOR induces competency of the pollen tube to respond to ovular attractant LURE peptides in Torenia fournieri...
December 2, 2016: Plant Physiology
https://www.readbyqxmd.com/read/27913674/immunoglobulins-and-their-receptors-and-subversion-of-their-protective-roles-by-bacterial-pathogens
#16
REVIEW
Jenny M Woof
Immunoglobulins (Igs) play critical roles in immune defence against infectious disease. They elicit potent elimination processes such as triggering complement activation and engaging specific Fc receptors present on immune cells, resulting in phagocytosis and other killing mechanisms. Many important pathogens have evolved mechanisms to subvert or evade Ig-mediated defence. One such mechanism used by several pathogenic bacteria features proteins that bind the Ig Fc region and compromise engagement of host effector molecules...
December 15, 2016: Biochemical Society Transactions
https://www.readbyqxmd.com/read/27913623/chac2-an-enzyme-for-slow-turnover-of-cytosolic-glutathione
#17
Amandeep Kaur, Ruchi Gautam, Ritika Srivastava, Avinash Chandel, Akhilesh Kumar, Subramanian Karthikeyan, Anand Kumar Bachhawat
Glutathione degradation plays an important role in glutathione and redox homeostasis and thus it is imperative to understand the enzymes and the mechanisms involved in glutathione degradation in detail. We describe here ChaC2, a member of the ChaC family of γ-glutamylcyclotransferases, as an enzyme that degrades glutathione in the cytosol of mammalian cells. ChaC2 is distinct from the previously described ChaC1, to which ChaC2 shows about 50% sequence identity. Human and mouse ChaC2 proteins, purified in vitro, show 10-20 fold lower catalytic efficiency than ChaC1, although they showed comparable Km values (Km of 3...
December 2, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27913523/advances-and-practical-use-of-monoclonal-antibodies-in-multiple-myeloma-therapy
#18
Hans C Lee, Donna M Weber
The use of proteasome inhibitors and immunomodulatory agents in the treatment of myeloma have resulted in significant improvements in patient outcomes over the last decade. Although these agents now form the backbone of current myeloma treatment regimens both in the frontline and in a relapsed setting, drug resistance remains an inevitable challenge that most patients will encounter during their disease course. Hence, new treatment strategies continue to be explored, and the recent regulatory approvals of the monoclonal antibodies (mAbs) daratumumab (DARA) and elotuzumab (ELO), which target the plasma cell surface proteins CD38 and signaling lymphocytic activation molecule F7 (SLAMF7), respectively, have heralded the long-awaited era of antibody-based approaches in the treatment of myeloma...
December 2, 2016: Hematology—the Education Program of the American Society of Hematology
https://www.readbyqxmd.com/read/27913472/novel-agents-in-chronic-lymphocytic-leukemia
#19
Nicole Lamanna, Susan O'Brien
The advent of novel small-molecule inhibitors has transformed the treatment approaches for patients with chronic lymphocytic leukemia (CLL). These therapies are becoming increasingly used in patients with relapsed disease, patients with 17p deletion, and, as of recently, also in the frontline setting for previously untreated patients with CLL. Moreover, many of these are oral therapies that are significantly less myelosuppressive than chemoimmunotherapy. However, these agents have their own set of unique toxicities with which providers must gain familiarity...
December 2, 2016: Hematology—the Education Program of the American Society of Hematology
https://www.readbyqxmd.com/read/27913255/using-the-bitola-system-to-identify-candidate-molecules-in-the-interaction-between-oral-lichen-planus-and-depression
#20
Yuanbo Zhan, Shuang Zhou, Ying Li, Sen Mu, Xuejing Song, Feng Lin, Ruimin Zhang, Bin Zhang
Exacerbations of oral lichen planus (OLP) have been linked to the periods of psychological stress, anxiety and depression. The specific mechanism of the interaction is unclear. The aim of this study was to explore the candidate genes or molecules that play important roles in the interaction between OLP and depression. The BITOLA system was used to search all intermediate concepts relevant to the "Gene or Gene Product" for OLP and depression, and the gene expression data and tissue-specific gene data along with manual checking were then employed to filter the intermediate concepts...
November 29, 2016: Behavioural Brain Research
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