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https://www.readbyqxmd.com/read/28538688/in-silico-study-and-bioprospection-of-the-antibacterial-and-antioxidant-effects-of-flavone-and-its-hydroxylated-derivatives
#1
Camila de Albuquerque Montenegro, Gregório Fernandes Gonçalves, Abrahão Alves de Oliveira Filho, Andressa Brito Lira, Thays Thyara Mendes Cassiano, Natanael Teles Ramos de Lima, José Maria Barbosa-Filho, Margareth de Fátima Formiga Melo Diniz, Hilzeth Luna Freire Pessôa
Flavonoid compounds are widely used as natural protective species, which can act as anti-inflammatory, antioxidant, anticoagulant, antihypertensive and antitumor agents. This study set out to investigate the probable pharmacological activities, along with the antibacterial and antioxidant effects, of flavone and its hydroxy derivatives: 3-hydroxyflavone, 5-hydroxyflavone and 6-hydroxyflavone. To do so, we investigated their pharmacological characteristics, using in silico tests that indicate likelihood of activity or inactivity, with the PASS online software, and the antimicrobial potential against Gram positive and Gram negative bacteria was also analyzed, including bacteria of clinical importance...
May 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28538564/discussion-combining-smoothened-agonist-and-nel-like-protein-1-enhances-bone-healing
#2
Ryan C Ransom, Michael T Longaker
No abstract text is available yet for this article.
June 2017: Plastic and Reconstructive Surgery
https://www.readbyqxmd.com/read/28538228/glycemic-control-in-the-treatment-of-psoriasis
#3
Wilfred Ip, Mark G Kirchhof
Psoriasis is a common chronic inflammatory skin disease that manifests as scaly erythematous plaques as a consequence of keratinocyte hyperproliferation and inflammation. It is commonly associated with diabetes, obesity, and the metabolic syndrome. While there are numerous approved treatment options available, they have limitations including availability, toxicities such as immunosuppression, and high cost. There is increasing evidence to suggest that several hypoglycemic agents used in the treatment of type 2 diabetes, including glucagon-like peptide-1 receptor agonists, dipeptidyl peptidase-4 inhibitors, thiazolidinediones and biguanides, exert beneficial effects in psoriasis...
May 25, 2017: Dermatology: International Journal for Clinical and Investigative Dermatology
https://www.readbyqxmd.com/read/28538185/regulation-of-active-dna-demethylation-through-rar-mediated-recruitment-of-a-tet-tdg-complex
#4
Haider M Hassan, Bart Kolendowski, Majdina Isovic, Kerstin Bose, Helen J Dranse, Arthur V Sampaio, T Michael Underhill, Joseph Torchia
Retinoic acid (RA) plays important roles in development, growth, and homeostasis through regulation of the nuclear receptors for RA (RARs). Herein, we identify Hypermethylated in Cancer 1 (Hic1) as an RA-inducible gene. HIC1 encodes a tumor suppressor, which is often silenced by promoter hypermethylation in cancer. Treatment of cells with an RAR agonist causes a rapid recruitment of an RAR/RXR complex consisting of TDG, the lysine acetyltransferase CBP, and TET 1/2 to the Hic1 promoter. Complex binding coincides with a transient accumulation of 5fC/5caC and concomitant upregulation of Hic1 expression, both of which are TDG dependent...
May 23, 2017: Cell Reports
https://www.readbyqxmd.com/read/28538150/lanthanides-report-calcium-sensor-in-the-vestibule-of-ryanodine-receptor
#5
Sándor Sárközi, István Komáromi, István Jóna, János Almássy
Ca(2+) regulates ryanodine receptor's (RyR) activity through an activating and an inhibiting Ca(2+)-binding site located on the cytoplasmic side of the RyR channel. Their altered sensitivity plays an important role in the pathology of malignant hyperthermia and heart failure. We used lanthanide ions (Ln(3+)) as probes to investigate the Ca(2+) sensors of RyR, because they specifically bind to Ca(2+)-binding proteins and they are impermeable to the channel. Eu(3+)'s and Sm(3+)'s action was tested on single RyR1 channels reconstituted into planar lipid bilayers...
May 23, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28538086/sphingosine-1-phosphate-receptor-1-agonist-sew2871-causes-severe-cardiac-side-effects-and-does-not-improve-microvascular-barrier-breakdown-in-sepsis
#6
Sven Flemming, Natalie Burkard, Michael Meir, Martin Alexander Schick, Christoph-Thomas Germer, Nicolas Schlegel
BACKGROUND: Endothelial barrier dysfunction is a hallmark in the pathogenesis of sepsis. Sphingosine-1-phosphate (S1P) has been proposed to be critically involved in the maintenance of endothelial barrier function predominately by activating S1P receptor-1 (S1P1). Previous studies have shown that the specific S1P1 agonist SEW2871 improves endothelial barrier function under inflammatory conditions. However, the effectiveness of SEW2871 and potential side effects remained largely unexplored in a clinically relevant model of sepsis...
May 23, 2017: Shock
https://www.readbyqxmd.com/read/28537785/a-practical-guide-to-the-use-of-eltrombopag-in-children-with-chronic-immune-thrombocytopenia
#7
John D Grainger, Sharon Thind
INTRODUCTION: Pediatric immune thrombocytopenia (ITP) may be associated with significant burden on children and their parents/caregivers. Thrombopoietin (TPO) receptor agonists (RAs) have been used to treat adult patients with chronic ITP (cITP) for nearly a decade and following pediatric studies Eltrombopag has been recently approved for pediatric cITP in the United States and Europe. TPO-RA s may help reduce the risk of bleeding and the need for conventional ITP therapies. REVIEW: In this review, the clinical data demonstrating the efficacy and safety of TPO-RAs in pediatric ITP are evaluated, key recommendations regarding safe administration of eltrombopag are provided, and potential future directions in management of pediatric ITP are discussed...
May 24, 2017: Pediatric Hematology and Oncology
https://www.readbyqxmd.com/read/28537730/discovery-of-small-molecules-as-multi-toll-like-receptor-agonists-with-proinflammatory-and-anticancer-activities
#8
Lei Zhang, Varun Dewan, Hang Hubert Yin
Therapies based on activation of multiple Toll-like receptors (TLRs) may offer superior therapeutic profiles than that of single TLR activation. To discover new small molecules that could activate multiple TLRs, we performed a cell-based high-throughput screening of a small-molecule library based on TLR3-mediated NF-κB activation. Subsequent structural optimization and counter screening of other TLRs produced the first small molecule (CU-CPT24e) capable of simultaneously activating TLRs 3, 8, and 9. Biochemical studies demonstrated that CU-CPT24e could induce a strong immune response via the production of various cytokines in human monocytic THP-1 cells...
May 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28535631/-a-multi-center-study-for-the-association-between-the-perception-and-control-of-disease-among-asthmatic-patients-in-chinese-urban-areas
#9
Y Nong, J T Lin, W Q Wang, X Zhou, C Z Wang, M Huang, S X Cai, P Chen, Q C Lin, J Y Zhou, Y H Gu, Y D Yuan, D J Sun, X H Yang, L Yang, J M Huo, Z C Chen, P Jiang, J Zhang, X W Ye, H G Liu, H P Tang, R Y Liu, C T Liu, W Zhang, C P Hu, Y Q Chen, X J Liu, L M Dai, W Zhou, Y J Huang, J Y Xu
Objective: To investigate the current perception of disease among asthmatic patients in Chinese urban areas, and to address its association with asthma control. Methods: This was a nationwide, multi-center, cross-sectional study covering 30 third-level, grade A hospitals in 30 provinces, municipalities and autonomous regions (not including Tibet) across Chinese mainland. The survey was carried out from October 2015 to May 2016. Asthmatic outpatients were selected to receive face-to-face questionnaire survey on asthma control including Asthma Control Test (ACT) score, classification of asthma control level[according to the Global Initiative for Asthma (GINA) 2015 classification system, as assessed by the physician completing the survey], perception of asthma (including question 1: nature of asthma as a disease; question 2: selection of first-line therapeutic agents to be regularly used daily for asthma; question 3: appropriate timing of the use of short-acting aerosols of β(2) receptor agonists; and question 4: therapeutic goals for asthma)...
May 16, 2017: Zhonghua Yi Xue za Zhi [Chinese medical journal]
https://www.readbyqxmd.com/read/28535499/the-role-of-5-htr6-in-mossy-fiber-sprouting-activating-fyn-and-p-erk1-2-in-pilocarpine-induced-chronic-epileptic-rats
#10
Wanhui Lin, Wenli Huang, Shenggen Chen, Mingxing Lin, Qingyu Huang, Huapin Huang
OBJECTIVE: Our primary objective is to verify whether 5-HTR6 is involved in the development of mossy fiber sprouting (MFS), and to determine how the progression of MFS is affected by 5-HTR6. METHODS: A total of 90 male adult Sprague-Dawley rats were allocated into either the control group (n=36) or the epileptic group (n=54). Status epilepticus (SE) of rats was induced by the intraperitoneal (i.p.) injection of LiCl-pilocarpine. We conducted our experiments in two stages...
May 25, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28535469/novel-propanamides-as-fatty-acid-amide-hydrolase-inhibitors
#11
Alessandro Deplano, Carmine Marco Morgillo, Monica Demurtas, Emmelie Björklund, Mariateresa Cipriano, Mona Svensson, Sanaz Hashemian, Giovanni Smaldone, Emilia Pedone, F Javier Luque, Maria G Cabiddu, Ettore Novellino, Christopher J Fowler, Bruno Catalanotti, Valentina Onnis
Fatty acid amide hydrolase (FAAH) has a key role in the control of the cannabinoid signaling, through the hydrolysis of the endocannabinoids anandamide and in some tissues 2-arachidonoylglycerol. FAAH inhibition represents a promising strategy to activate the cannabinoid system, since it does not result in the psychotropic and peripheral side effects characterizing the agonists of the cannabinoid receptors. Here we present the discovery of a novel class of profen derivatives, the N-(heteroaryl)-2-(4-((2-(trifluoromethyl)pyridin-4-yl)amino)phenyl)propanamides, as FAAH inhibitors...
May 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28535455/the-effectiveness-of-telemedicine-delivered-opioid-agonist-therapy-in-a-supervised-clinical-setting
#12
Joseph K Eibl, Graham Gauthier, David Pellegrini, Jeffery Daiter, Michael Varenbut, John C Hogenbirk, David C Marsh
OBJECTIVE: Opioid use disorder has been declared a public health crisis across North America and opioid agonist therapy (OAT) is the standard of care for these patients. Despite the increasing adoption of telemedicine as a delivery method for OAT, its effectiveness has not yet been evaluated against traditional in-person treatment. This study compared treatment outcomes for in-person versus telemedicine-delivered OAT. METHODS: We conducted a non-randomized cohort comparison study using an administrative database for patients who commenced OAT between 2011 and 2012 across 58 clinic sites in the province of Ontario, Canada...
May 17, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28535137/the-effect-of-heart-disease-on-anesthetic-complications-during-routine-dental-procedures-in-dogs
#13
Jennifer E Carter, Alison A Motsinger-Reif, William V Krug, Bruce W Keene
Dental procedures are a common reason for general anesthesia, and there is widespread concern among veterinarians that heart disease increases the occurrence of anesthetic complications. Anxiety about anesthetizing dogs with heart disease is a common cause of referral to specialty centers. To begin to address the potential effect of heart disease on anesthetic complications in dogs undergoing anesthesia for routine dental procedures, we compared anesthetic complications in 100 dogs with heart disease severe enough to trigger referral to a specialty center (cases) to those found in 100 dogs without cardiac disease (controls) that underwent similar procedures at the same teaching hospital...
May 23, 2017: Journal of the American Animal Hospital Association
https://www.readbyqxmd.com/read/28534854/methodical-challenges-and-a-possible-resolution-in-the-assessment-of-receptor-reserve-for-adenosine-an-agonist-with-short-half-life
#14
Judit Zsuga, Tamas Erdei, Katalin Szabó, Nora Lampe, Csaba Papp, Akos Pinter, Andras Jozsef Szentmiklosi, Bela Juhasz, Zoltán Szilvássy, Rudolf Gesztelyi
The term receptor reserve, first introduced and used in the traditional receptor theory, is an integrative measure of response-inducing ability of the interaction between an agonist and a receptor system (consisting of a receptor and its downstream signaling). The underlying phenomenon, i.e., stimulation of a submaximal fraction of receptors can apparently elicit the maximal effect (in certain cases), provides an opportunity to assess the receptor reserve. However, determining receptor reserve is challenging for agonists with short half-lives, such as adenosine...
May 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28534263/n-acetylaspartylglutamate-inhibits-heroin-self-administration-and-heroin-seeking-behaviors-induced-by-cue-or-priming-in-rats
#15
Huaqiang Zhu, Miaojun Lai, Weisheng Chen, Disen Mei, Fuqiang Zhang, Huifeng Liu, Wenhua Zhou
Activation of presynaptic group II metabotropic glutamate receptors (mGluR2/3) inhibits drug reward and drug-seeking behavior, but the role of N-acetylaspartylglutamate (NAAG), an agonist of endogenous mGluR2/3, in heroin reward and heroin-seeking behavior remained unclear. Here, we aimed to explore the effects of exogenous NAAG on heroin self-administration and heroin-seeking behavior. First, rats were trained to self-administer heroin under a fixed ratio 1 (FR1) schedule for 10 days, then received NAAG (50 or 100 μg/10 μL in each nostril) in the absence or presence of LY341495 (1 mg/kg, i...
May 22, 2017: Neuroscience Bulletin
https://www.readbyqxmd.com/read/28534197/pcmt1-ameliorates-neuronal-apoptosis-by-inhibiting-the-activation-of-mst1-after-subarachnoid-hemorrhage-in-rats
#16
Ligen Shi, Ammar Al-Baadani, Keren Zhou, Anwen Shao, Shenbin Xu, Sheng Chen, Jianmin Zhang
Mammalian sterile 20-like kinase 1 (MST1) is found to promote neuronal apoptosis. Protein-L-isoaspartate (D-aspartate) O-methyltransferase (PCMT1), an anti-apoptosis factor, was recently identified as an MST1-interacting protein. This study aims to explore the potential role of PCMT1 in reducing MST1-induced neuronal apoptosis after subarachnoid hemorrhage (SAH) in rats. One hundred ninety-eight male Sprague-Dawley rats were used. An exogenous PCMT1 agonist, CGP 3466B, was injected subcutaneously 1 h after the SAH induced by endovascular perforation...
May 22, 2017: Translational Stroke Research
https://www.readbyqxmd.com/read/28534193/antagonist-perturbation-mechanism-for-activation-function-2-fixed-motifs-active-conformation-and-docking-mode-of-retinoid-x-receptor-antagonists
#17
Motonori Tsuji
HX531, which contains a dibenzodiazepine skeleton, is one of the first retinoid X receptor (RXR) antagonists. Functioning via RXR-PPARγ heterodimer, this compound is receiving a lot of attention as a therapeutic drug candidate for diabetic disease controlling differentiation of adipose tissue. However, the active conformation of HX531 for RXRs is not well established. In the present study, quantum mechanics calculations and molecular mechanical docking simulations were carried out to precisely study the docking mode of HX531 with the human RXRα ligand-binding domain, as well as to provide a new approach to drug design using a structure-based perspective...
May 22, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28534145/alterations-in-gene-expression-after-gamma-hydroxybutyric-acid-intake-a-pilot-study
#18
Lena-Maria Mehling, Annika Spottke, Anna Heidbreder, Peter Young, Burkhard Madea, Cornelius Hess, Cornelius Courts
Gamma-hydroxybutyric acid (GHB) acts as an agonist of the GABAB receptor, where GHB induces a depressant effect in the central nervous system. Besides its therapeutic application, GHB is also used as a date rape drug. However, the detection of GHB ingestion proves to be difficult due to its narrow detection window. The aim of this pilot study was to assess differential gene expressions after GHB intake to identify potential biomarkers for the detection of GHB intake. To this aim, alteration in gene expression of ALDH5A1, AKR7A2, EREG, and PEA15 was investigated via quantitative PCR (qPCR)...
May 22, 2017: International Journal of Legal Medicine
https://www.readbyqxmd.com/read/28533737/the-alpha-1a-adrenergic-receptor-agonist-a61603-reduces-cardiac-polyunsaturated-fatty-acid-and-endocannabinoid-metabolites-associated-with-inflammation-in-vivo
#19
Monte S Willis, Amro Ilaiwy, Megan D Montgomery, Paul C Simpson, Brian C Jensen
INTRODUCTION: Alpha-1-adrenergic receptors (α1-ARs) are G-protein coupled receptors (GPCRs) with three highly homologous subtypes (α1A, α1B, and α1D). Of these three subtypes, only the α1A and α1B are expressed in the heart. Multiple pre-clinical models of heart injury demonstrate cardioprotective roles for the α1A. Non-selective α1-AR activation promotes glycolysis in the heart, but the functional α1-AR subtype and broader metabolic effects have not been studied. OBJECTIVES: Given the high metabolic demands of the heart and previous evidence indicating benefit from α1A activation, we chose to investigate the effects of α1A activation on the cardiac metabolome in vivo...
October 2016: Metabolomics: Official Journal of the Metabolomic Society
https://www.readbyqxmd.com/read/28533461/interspecific-visual-signalling-in-animals-and-plants-a-functional-classification
#20
REVIEW
Tim Caro, William L Allen
Organisms frequently gain advantages when they engage in signalling with individuals of other species. Here, we provide a functionally structured framework of the great variety of interspecific visual signals seen in nature, and then describe the different signalling mechanisms that have evolved in response to each of these functional requirements. We propose that interspecific visual signalling can be divided into six major functional categories: anti-predator, food acquisition, anti-parasite, host acquisition, reproductive and agonistic signalling, with each function enabled by several distinct mechanisms...
July 5, 2017: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
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