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https://www.readbyqxmd.com/read/28076854/open-angle-glaucoma-drug-development-pipeline-during-the-last-20-years-1995-2015
#1
André Vicente, Sylvie Prud'homme, Joana Ferreira, Luís Abegão Pinto, Ingeborg Stalmans
OBJECTIVES: To analyse drug development for open-angle glaucoma during the last 20 years. METHODS: Research was performed by referring to clinical trials registered at the International Clinical Trials Registry Platform (ICTRP). A search for the condition "open-angle glaucoma" with the intervention "drug" was performed. We included trials registered from 01/01/1995 to 01/01/2015, only involving studies in phases 1, 2, and 3. Only studies resorting to novel treatment strategies (either novel drugs or yet-untested fixed associations of approved medication) were considered...
January 12, 2017: Ophthalmic Research
https://www.readbyqxmd.com/read/28069944/soluble-klotho-binds-monosialoganglioside-to-regulate-membrane-microdomains-and-growth-factor-signaling
#2
George Dalton, Sung-Wan An, Saif I Al-Juboori, Nicole Nischan, Joonho Yoon, Evgenia Dobrinskikh, Donald W Hilgemann, Jian Xie, Kate Luby-Phelps, Jennifer J Kohler, Lutz Birnbaumer, Chou-Long Huang
Soluble klotho, the shed ectodomain of the antiaging membrane protein α-klotho, is a pleiotropic endocrine/paracrine factor with no known receptors and poorly understood mechanism of action. Soluble klotho down-regulates growth factor-driven PI3K signaling, contributing to extension of lifespan, cardioprotection, and tumor inhibition. Here we show that soluble klotho binds membrane lipid rafts. Klotho binding to rafts alters lipid organization, decreases membrane's propensity to form large ordered domains for endocytosis, and down-regulates raft-dependent PI3K/Akt signaling...
January 9, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28069535/thyronamines-and-analogues-translational-research-on-thyronergic-amines-the-route-from-rediscovery-of-thyronamines-to-the-bedside
#3
Grazia Chiellini, Lorenza Bellusci, Martina Sabatini, Riccardo Zucchi
Thyronamines are a novel class of endogenous signaling compounds, structurally related to thyroid hormones (THs). Specific thyronamines, particularly 3-iodothyronamine (T1AM), stimulate with nanomolar affinity trace amine-associated receptor 1 (TAAR1), a G protein-coupled membrane receptor, and may also interact with other TAAR subtypes (particularly TAAR5), adrenergic receptors (particularly α2 receptors), amine transporters, and mitochondrial proteins. In addition to its structural similarities with THs, T1AM also contains the arylethylamine scaffold as in monoamine neurotransmitters, implicating an intriguing role for T1AM as both a neuromodulator and a hormone-like molecule constituting a part of thyroid hormone signaling...
January 6, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28065587/ffpm-a-pde4-inhibitor-reverses-learning-and-memory-deficits-in-app-ps1-transgenic-mice-via-camp-pka-creb-signaling-and-anti-inflammatory-effects
#4
Haibiao Guo, Yufang Cheng, Canmao Wang, Jingang Wu, Zhengqiang Zou, Bo Niu, Hui Yu, Haitao Wang, Jiangping Xu
Thus far, phosphodiesterase-4 (PDE4) inhibitors have not been approved for application in Alzheimer's disease (AD) in a clinical setting due to severe side effects, such as nausea and vomiting. In this study, we investigated the effect of FFPM, a novel PDE4 inhibitor, on learning and memory abilities, as well as the underlying mechanism in the APP/PS1 mouse model of AD. Pharmacokinetic studies have revealed that FFPM efficiently permeates into the brain, and reached peak values in plasma 2 h after orally dosing...
January 5, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28040841/incidence-of-bradycardia-in-pediatric-patients-receiving-dexmedetomidine-anesthesia-a-meta-analysis
#5
Maowei Gong, Yuanyuan Man, Qiang Fu
Background Dexmedetomidine, an α2-receptor agonist, provides potent sedation, analgesia, and anxiolysis without respiratory depression and is used in a variety of surgical and procedural situations. Aim of the review The aim of this study was to estimate the incidence of bradycardia in pediatric patients who received dexmedetomidine as a sole agent for any procedural, intensive care or surgical sedation. Method Literature was searched in electronic databases and studies were selected by following pre-determined eligibility criteria...
December 31, 2016: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/28035776/direct-enzymatic-branch-end-extension-of-glycocluster-presented-glycans-an-effective-strategy-for-programming-glycan-bioactivity
#6
Carlos Bayón, Ning He, Mario Deir-Kaspar, Pilar Blasco, Sabine André, Hans-Joachim Gabius, Ángel Rumbero, Jesús Jiménez-Barbero, Wolf-Dieter Fessner, María J Hernáiz
The sequence of a glycan and its topology of presentation team up to determine the specificity and selectivity of recognition by saccharide receptors (lectins). Structure-activity analysis would be furthered if the glycan part of a glycocluster could be efficiently elaborated in situ while keeping all other parameters constant. By using a bacterial α2,6-sialyltransferase and a small library of bi- to tetravalent glycoclusters, we illustrate the complete conversion of scaffold-presented lactoside units into two different sialylated ligands based on N-acetyl/glycolyl-neuraminic acid incorporation...
November 2, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28029766/neuroprotective-effects-of-a-structurally-new-family-of-high-affinity-imidazoline-i2-receptor-ligands
#7
Sònia Abás, Amaia M Erdozain, Benjamin Keller, Sergio Rodríguez-Arévalo, Luis F Callado, Jesús A García-Sevilla, Carmen Escolano
The imidazoline I2 receptors (I2-IRs) are widely distributed in the brain, and I2-IR ligands may have therapeutic potential as neuroprotective agents. Since structural data for I2-IR remains unknown, the discovery of selective I2-IR ligands devoid of α2-adrenoceptor (α2-AR) affinity is likely to provide valuable tools in defining the pharmacological characterization of these receptors. We report the pharmacological characterization of a new family of (2-imidazolin-4-yl)phosphonates. Radioligand binding studies showed that they displayed a higher affinity for I2-IRs than idazoxan, and high I2/α2 selectivity...
January 4, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28028077/endogenous-%C3%AE-2a-adrenoceptor-operated-sympathoadrenergic-tones-attenuate-insulin-secretion-via-camp-trpm2-signaling
#8
Kiyonori Ito, Katsuya Dezaki, Masashi Yoshida, Hodaka Yamada, Rina Miura, Rauza Sukma Rita, Susumu Ookawara, Kaoru Tabei, Masanobu Kawakami, Kazuo Hara, Yoshiyuki Morishita, Toshihiko Yada, Masafumi Kakei
In pancreatic β-cells, pharmacological concentrations of catecholamines, including adrenaline, have been used to inhibit insulin release and explore the multiple mechanisms involved. However, the significance of these signaling pathways for physiological adrenergic functions in β-cells is largely unknown. In the process of glucose-induced insulin secretion, opening of background current through non-selective cation channels (NSCCs) might facilitate membrane depolarization by closure of the ATP-sensitive K(+) channels...
December 27, 2016: Diabetes
https://www.readbyqxmd.com/read/28018351/allorecognition-of-hla-c-mismatches-by-cd8-t-cells-in-hematopoietic-stem-cell-transplantation-is-a-complex-interplay-between-mismatched-peptide-binding-region-residues-hla-c-expression-and-hla-dpb1-disparities
#9
Florence Bettens, Stéphane Buhler, Jean-Marie Tiercy
HLA-C locus mismatches (MMs) are the most frequent class I disparities in unrelated hematopoietic stem cell transplantation (HSCT) and have a detrimental impact on clinical outcome. Recently, a few retrospective clinical studies have reported some variability in the immunogenicity of HLA-C incompatibilities. To get better insight into presumably permissive HLA-C MMs, we have developed a one-way in vitro mixed lymphocyte reaction (MLR) assay allowing to quantify activated CD56(-)CD137(+)CD8(+) lymphocytes in HLA-C incompatible combinations...
2016: Frontiers in Immunology
https://www.readbyqxmd.com/read/28012946/impaired-gabaergic-inhibition-in-the-hippocampus-of-fmr1-knockout-mice
#10
Victor Sabanov, Sien Braat, Laura D'Andrea, Rob Willemsen, Shimriet Zeidler, Liesbeth Rooms, Claudia Bagni, R Frank Kooy, Detlef Balschun
Many clinical and molecular features of the fragile X syndrome, a common form of intellectual disability and autism, can be modeled by deletion of the Fmr1 protein (Fmrp) in mice. Previous studies showed a decreased expression of several components of the GABAergic system in Fmr1 knockout mice. Here, we used this mouse model to investigate the functional consequences of Fmrp deletion on hippocampal GABAergic inhibition in the CA1-region of the hippocampus. Whole-cell patch-clamp recordings demonstrated a significantly reduced amplitude of evoked inhibitory postsynaptic currents (eIPSCs) and a decrease in the amplitude and frequency of spontaneous IPSCs...
December 21, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/28012205/activated-%C3%AE-2-macroglobulin-induces-mesenchymal-cellular-migration-of-raw264-7-cells-through-low-density-lipoprotein-receptor-related-protein-1
#11
Darío G Ferrer, Virginia Actis Dato, Javier R Jaldín Fincati, Valeria E Lorenc, María C Sánchez, Gustavo A Chiabrando
Distinct modes of cell migration contribute to diverse types of cell movements. The mesenchymal mode is characterized by a multistep cycle of membrane protrusion, the formation of focal adhesion, and the stabilization at the leading edge associated with the degradation of extracellular matrix (ECM) components and with regulated extracellular proteolysis. Both α2 -Macroglobulin (α2 M) and its receptor, low density lipoprotein receptor-related protein 1 (LRP1), play important roles in inflammatory processes, by controlling the extracellular activity of several proteases...
December 24, 2016: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28000867/dexmedetomidine-may-upregulate-the-expression-of-caveolin%C3%A2-1-in-lung-tissues-of-rats-with-sepsis-and-improve-the-short%C3%A2-term-outcome
#12
Yun Zhang, Ke Ran, Shu-Bin Zhang, Lili Jiang, Dan Wang, Zhi-Jian Li
Dexmedetomidine (DXM) is a selective α2-adrenoceptor (α2‑AR) and imidazoline receptor (IR) agonist that has been reported to regulate inflammatory responses mediated by diverse signaling pathways through α2‑AR. The majority of the reported receptors or downstream molecules have been demonstrated to locate with caveolin‑1, a protein suggested to participate in regulating Toll‑like receptor 4 (TLR4)‑mediated inflammatory responses and the pathogen endocytosis capability of macrophages. The present study hypothesized that DXM may influence these pathways by regulating the expression of caveolin‑1 and mediating the subsequent effects...
December 15, 2016: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28000081/rotavirus-nsp486-175-interacts-with-h9c2-2-1-cells-in-vitro-elevates-intracellular-ca-2-levels-and-can-become-cytotoxic-a-possible-mechanism-for-extra-intestinal-pathogenesis
#13
Xiaoshun Xiong, Yinyin Hu, Caixia Liu, Xiangyang Li
Rotavirus (RV) is the predominant cause of infantile gastroenteritis with multiple pathogenic factors, among which enterotoxin NSP4 is the most significant factor. NSP4 has been shown to induce elevation of the intracellular calcium concentration, alteration of the cytoskeleton organization, and cytopathic effect among other processes. However, increasing evidence suggests that RVs can escape from the gastrointestinal tract and invade other organs and tissues to cause extra-intestinal diseases. In this study, we investigated whether NSP4 has a pathogenic effect on extra-intestinal cells and examined possible molecular mechanisms in vitro...
December 20, 2016: Virus Genes
https://www.readbyqxmd.com/read/27998004/dexmedetomidine-preconditioning-for-myocardial-protection-in-ischemia-reperfusion-injury-in-rats-by-downregulation-of-the-hmgb1-tlr4-nf-%C3%AE%C2%BAb-signaling-pathway
#14
Yu-Fan Yang, Ke Peng, Hong Liu, Xiao-Wen Meng, Jing-Jing Zhang, Fu-Hai Ji
Pharmacological preconditioning reduces myocardial infarct size in ischemia-reperfusion (I-R) injury. Dexmedetomidine, a selective α2 -adrenoceptor agonist, has proven cardioprotective effect when administered prior to I-R, although underlying mechanisms for this effect are not fully understood. We evaluated whether dexmedetomidine preconditioning could induce a myocardio-protective effect against I-R injury by inhibiting associated inflammatory processes through downregulation of the high mobility group box 1 (HMGB1)-toll-like receptor 4 (TLR4)-nuclear factor κB (NF-κB) signaling pathway...
December 20, 2016: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/27993973/anaplasma-marginale-outer-membrane-protein-a-is-an-adhesin-that-recognizes-sialylated-and-fucosylated-glycans-and-functionally-depends-on-an-essential-binding-domain
#15
Kathryn S Hebert, David Seidman, Aminat T Oki, Jerilyn Izac, Sarvani Emani, Lee D Oliver, Daniel P Miller, Brittney K Tegels, Reiji Kannagi, Richard T Marconi, Jason A Carlyon
Anaplasma marginale causes bovine anaplasmosis, a debilitating and potentially fatal tick-borne infection of cattle. Because A. marginale is an obligate intracellular organism, its adhesins that mediate entry into host cells are essential for survival. Here, we demonstrate that A. marginale outer membrane protein A (AmOmpA; AM854) contributes to the invasion of mammalian and tick host cells. AmOmpA exhibits predicted structural homology to OmpA of A. phagocytophilum (ApOmpA), an adhesin that uses key lysine and glycine residues to interact with α2,3-sialylated and α1,3-fucosylated glycan receptors, including 6-sulfo-sialyl Lewis x...
December 19, 2016: Infection and Immunity
https://www.readbyqxmd.com/read/27992510/noradrenaline-improves-behavioral-contrast-sensitivity-via-the-%C3%AE-adrenergic-receptor
#16
Ryo Mizuyama, Shogo Soma, Naofumi Suemastu, Satoshi Shimegi
Noradrenaline (NA) is released from the locus coeruleus in the brainstem to almost the whole brain depending on the physiological state or behavioral context. NA modulates various brain functions including vision, but many questions about the functional role of its effects and mechanisms remain unclear. To explore these matters, we focused on three questions, 1) whether NA improves detectability of a behavior-relevant visual stimulus, 2) which receptor subtypes contribute to the NA effects, and 3) whether the NA effects are specific for visual features such as spatial frequency (SF)...
2016: PloS One
https://www.readbyqxmd.com/read/27986643/cigarette-smoke-extracts-induce-overexpression-of-the-proto-oncogenic-gene-interleukin-13-receptor-%C3%AE-2-through-activation-of-the-pka-creb-signaling-pathway-to-trigger-malignant-transformation-of-lung-vascular-endothelial-cells-and-angiogenesis
#17
Mei Meng, Huaidong Liao, Bin Zhang, Yanyan Pan, Ying Kong, Wenming Liu, Ping Yang, Zihe Huo, Zhifei Cao, Quansheng Zhou
Cigarette smoking is a major cause of lung cancer. Tumor-associated endothelial cells (TAECs) play important roles in tumor angiogenesis and metastasis. However, whether cigarette smoking can trigger genesis of lung TAECs has not been reported yet. In the current study, we used lung endothelial cell (EC) lines as a model to study the pathological effect of cigarette smoke extracts (CSEs) on human lung ECs, and found that a lower dose of 4% CSEs obviously caused abnormal morphological changes in ECs, increased the permeability of endothelial monolayer, while a higher concentration of 8% CSEs caused EC apoptosis...
December 13, 2016: Cellular Signalling
https://www.readbyqxmd.com/read/27976583/enhanced-antiglioma-efficacy-of-ultrahigh-loading-capacity-paclitaxel-prodrug-conjugate-self-assembled-targeted-nanoparticles
#18
Yan Jiang, Xiuzhen Wang, Xin Liu, Wei Lv, Hongjuan Zhang, Mingwan Zhang, Xinrui Li, Hongliang Xin, Qunwei Xu
Glioblastoma multiforme (GBM) presents one of the most lethal brain tumor with a dismal prognosis. And nanodrug delivery system (nano-DDS) have raised a lot of concern, while the conventional nanoformulations addressed many limitations, especially the low drug loading capacity and poor stability in vivo. Herein, we proposed PTX prodrug (PTX-SS-C18) conjugate self-assembled nanoparticles (PSNPs) functionalized with Pep-1, glioma homing peptide, to overcome the blood brain tumor barrier (BBTB) via interleukin 13 receptor α2 (IL-13Rα2)-mediated endocytosis for targeting GMB...
December 23, 2016: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/27975177/involvement-of-histaminergic-and-noradrenergic-receptors-in-the-oxytocin-induced-food-intake-in-neonatal-meat-type-chicks
#19
Seyed Vahid Mirnaghizadeh, Morteza Zendehdel, Vahab Babapour
Oxytocin neurons have a physiological role in food intake and energy balance. Several studies have shown that central histaminergic and adrenergic systems synapse on oxytocin neurons but there is no information for their interaction on food intake regulation in birds. The purpose of this study was to examine the effects of intracerebroventricular (ICV) injection of α-fluoromethylhistidine (α-FMH, histidine decarboxylase inhibitor), chlorpheniramine (histamine H1 receptors antagonist), famotidine (histamine H2 receptors antagonist), thioperamide (histamine H3 receptors antagonist), prazosin (α1 receptor antagonist), yohimbine (α2 receptor antagonist), metoprolol (β1 adrenergic receptor antagonist), ICI 118,551 (β2 adrenergic receptor antagonist) and SR59230R (β3 adrenergic receptor antagonist) on oxytocin-induced hypophagia in 3-h food-deprived (FD3) neonatal broiler chicken...
December 14, 2016: Veterinary Research Communications
https://www.readbyqxmd.com/read/27974569/human-adenovirus-type-37-uses-%C3%AE-v%C3%AE-1-and-%C3%AE-3%C3%AE-1-integrins-for-infection-of-human-corneal-cells
#20
Rickard J Storm, B David Persson, Lars Nygård Skalman, Lars Frängsmyr, Mona Lindström, Greg Rankin, Richard Lundmark, Fatima Pedrosa Domellöf, Niklas Arnberg
: Epidemic keratoconjunctivitis (EKC) is a severe, contagious ocular disease that affects 20-40 million individuals worldwide every year. EKC is mainly caused by six types of human adenovirus (HAdV): HAdV-8, -19, -37, -53, -54, and -56. Of these, HAdV-8, -19, and -37 use sialic acid-containing glycans as cellular receptors. αVβ3, αVβ5, and a few additional integrins facilitate entry and endosomal release of other HAdVs. With the exception of a few biochemical analyses indicating that HAdV-37 can interact physically with αVβ5, little is known about the integrins used by EKC-causing HAdVs...
December 14, 2016: Journal of Virology
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