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https://www.readbyqxmd.com/read/30120841/tenofovir-alafenamide-taf-for-the-treatment-of-chronic-hepatitis-b-mono-infection
#1
Lindsey M Childs-Kean, Eric Egelund, Jacqueline Jourjy
Tenofovir alafenamide (TAF) is indicated for adult patients with chronic HBV infection with compensated liver disease at a dose of 25mg orally daily. TAF is a more stable prodrug in the plasma than tenofovir disoproxil fumarate (TDF), leading to decreased plasma exposure of tenofovir. Decreased exposure is thought to reduce the risk of long-term TDF toxicities, such as nephrotoxicity and decreased bone mineral density. TAF has the same mechanism of action as TDF: a nucleotide reverse transcriptase inhibitor...
August 18, 2018: Pharmacotherapy
https://www.readbyqxmd.com/read/30119633/selective-resistance-profiles-emerging-in-patient-derived-clinical-isolates-with-cabotegravir-bictegravir-dolutegravir-and-elvitegravir
#2
Maureen Oliveira, Ruxandra-Ilinca Ibanescu, Kaitlin Anstett, Thibault Mésplède, Jean-Pierre Routy, Marjorie A Robbins, Bluma G Brenner
BACKGROUND: Integrase strand transfer inhibitors (INSTIs) are recommended for first-line HIV therapy based on their relatively high genetic barrier to resistance. Although raltegravir (RAL) and elvitegravir (EVG) resistance profiles are well-characterized, resistance patterns for dolutegravir (DTG), bictegravir (BIC), and cabotegravir (CAB) remain largely unknown. Here, in vitro drug selections compared the development of resistance to DTG, BIC, CAB, EVG and RAL using clinical isolates from treatment-naïve primary HIV infection (PHI) cohort participants (n = 12), and pNL4...
August 17, 2018: Retrovirology
https://www.readbyqxmd.com/read/30119013/dual-regulation-of-l-selectin-cd62l-by-hiv-1-enhanced-expression-by-vpr-in-contrast-with-cell-surface-down-modulation-by-nef-and-vpu
#3
Erica Giuliani, Lia Vassena, Silvia Galardi, Alessandro Michienzi, Maria Giovanna Desimio, Margherita Doria
The HIV-1 accessory protein Vpr displays various activities that can favor viral replication such as G2 cell cycle arrest. Vpr also modulates host gene expression, although this property is poorly characterized. Here, we investigated the effect of Vpr on L-selectin (CD62L), which crucially controls leukocytes circulation and generation of immune responses against pathogens. We report that Vpr up-regulates CD62L mRNA level when individually expressed in Jurkat T cells as well as during HIV-1 infection of primary CD4+ T cells...
August 14, 2018: Virology
https://www.readbyqxmd.com/read/30118732/evaluation-of-antiviral-effects-of-novel-ns5a-inhibitors-in-hepatitis-c-virus-cell-culture-system-with-full-genome-infectious-clones
#4
Asako Murayama, Kei Fujiwara, Norie Yamada, Masaaki Shiina, Takahiro Masaki, Masamichi Muramatsu, Takaji Wakita, Takanobu Kato
Nonstructural protein 5A (NS5A) inhibitors of hepatitis C virus (HCV) are known to have potent anti-viral effects; however, these inhibitors have limited activities on strains with resistant-associated substitutions or non-genotype 1 strains. To overcome these shortcomings, novel NS5A inhibitors have been developed and approved for clinical application. The aim of this study was to evaluate the anti-viral effect of novel NS5A inhibitors (derivatives of odalasvir) on HCV genotype 2 strains in a cell culture system...
August 14, 2018: Antiviral Research
https://www.readbyqxmd.com/read/30116231/structural-implications-of-genotypic-variations-in-hiv-1-integrase-from-diverse-subtypes
#5
Leonard Rogers, Adetayo E Obasa, Graeme B Jacobs, Stefan G Sarafianos, Anders Sönnerborg, Ujjwal Neogi, Kamalendra Singh
Human immunodeficiency virus type 1 (HIV-1) integrase (IN) integrates viral DNA into the host genome using its 3'-end processing and strand-transfer activities. Due to the importance of HIV-1 IN, it is targeted by the newest class of approved drugs known as integrase strand transfer inhibitors (INSTIs). INSTIs are efficient in maintaining low viral load; however, as with other approved antivirals, resistance mutations emerge in patients receiving INSTI-containing therapy. As INSTIs are becoming increasingly accessible worldwide, it is important to understand the mechanism(s) of INSTI susceptibility...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/30114965/structure-based-virtual-screening-3d-qsar-molecular-dynamics-and-admet-studies-for-selection-of-natural-inhibitors-against-structural-and-non-structural-targets-of-chikungunya
#6
Jaykant Vora, Shivani Patel, Sonam Sinha, Sonal Sharma, Anshu Srivastava, Mahesh Chhabria, Neeta Shrivastava
The transmission of mosquito-borne Chikungunya virus (CHIKV) has large epidemics worldwide. Till date, there are neither anti-viral drugs nor vaccines available for the treatment of Chikungunya. Accumulated evidences suggest that some natural compounds i.e. Epigallocatechin gallate, Harringtonine, Apigenin, Chrysin, Silybin etc. have the capability to inhibit CHIKV replication in vitro. Natural compounds are known to possess less or no side effects. Therefore, natural compound in its purified or crude extracts form could be the preeminent and safe mode of therapies for Chikungunya...
August 16, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/30113675/interferon-alpha-triggers-autoimmune-thyroid-diseases-via-lysosomal-dependent-degradation-of-thyroglobulin
#7
Larissa C Faustino, Angela Lombardi, Julio Madrigal-Matute, Randall P Owen, Steven K Libutti, Yaron Tomer
Context: Autoimmune thyroid diseases (AITD) arise from complex interactions between genetic, epigenetic and environmental factors. Thyroglobulin (TG) is a major susceptibility gene for both Graves' disease and Hashimoto's thyroiditis. Interferon-alpha (IFNα), a cytokine secreted during viral infections, has recently emerged as a key trigger of AITD. We have previously shown that IFNα upregulates TG transcription, however, how the upregulation of TG transcription by IFNα triggers AITD is still unknown...
August 2, 2018: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/30113115/sofosbuvir-with-ns5a-inhibitors-in-hepatitis-c-virus-hcv-infection-with-severe-renal-insufficiency
#8
Akash Singh, Sunita Kumari, Pramod Kumar, Arka De, Virendra Singh
Treatment of Hepatitis C virus (HCV) in patients with severe renal insufficiency is cumbersome as sofosbuvir is mainly excreted by the kidneys. There is paucity of data on the use of sofosbuvir and NS5A inhibitors in these patients. We hereby report our experience of treating chronic hepatitis C in patients with severe renal insufficiency with full dose sofosbuvir and NS5A inhibitors.Forty-seven patients with severe renal insufficiency (on dialysis n=39, predialysis n=8) with HCV infection were treated between December 2015- August 2017 with full dose sofosbuvir with ledipasvir or daclatasvir for 12 /24 weeks depending on the genotype and presence or absence of cirrhosis...
August 16, 2018: Journal of Viral Hepatitis
https://www.readbyqxmd.com/read/30113067/limiting-respiratory-viral-infection-by-targeting-antiviral-and-immunological-functions-of-bst-2-tetherin-knowledge-and-gaps
#9
REVIEW
Kayla N Berry, Daniel L Kober, Alvin Su, Tom J Brett
Recent findings regarding the cellular biology and immunology of BST-2 (also known as tetherin) indicate that its function could be exploited as a universal replication inhibitor of enveloped respiratory viruses (e.g., influenza, respiratory syncytial virus, etc.). BST-2 inhibits viral replication by preventing virus budding from the plasma membrane and by inducing an antiviral state in cells adjacent to infection via unique inflammatory signaling mechanisms. This review presents the first comprehensive summary of what is currently known about BST-2 anti-viral function against respiratory viruses, how these viruses construct countermeasures to antagonize BST-2, and how BST-2 function might be targeted to develop therapies to treat respiratory virus infections...
August 16, 2018: BioEssays: News and Reviews in Molecular, Cellular and Developmental Biology
https://www.readbyqxmd.com/read/30112207/applications-of-click-chemistry-in-the-development-of-hiv-protease-inhibitors
#10
REVIEW
Mukesh M Mudgal, Nagaraju Birudukota, Mayur A Doke
Acquired Immunodeficiency Syndrome (AIDS) has been devastating for millions of people around the world. Inhibition of the human immunodeficiency virus (HIV) protease is among the most important approaches for the therapeutic intervention in HIV infection. Since the discovery of the HIV-1 protease, this enzyme has been considered as a key target for the inhibition of viral replication. A large body of research has been done to develop an effective HIV-1 protease inhibitor. There are to date 10 HIV-1 protease inhibitor drugs approved by the Food and Drug Administration (FDA) that have improved the survival and quality of life of HIV infected people...
2018: International Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/30111572/sirtuin-2-isoform-1-enhances-hepatitis-b-virus-rna-transcription-and-dna-synthesis-via-the-akt-gsk-3%C3%AE-%C3%AE-catenin-signaling-pathway
#11
Zahra Zahid Piracha, Hyeon Joong Kwon, Umar Saeed, Jumi Kim, Jaesung Jung, Yong-Joon Chwae, Sun Park, Ho-Joon Shin, Kyongmin Kim
Sirtuin 2 (Sirt2), a NAD+ -dependent protein deacetylase, is overexpressed in many hepatocellular carcinomas (HCCs) and can deacetylate many proteins, including tubulins and AKT prior to AKT activation. Here, we found that endogenous Sirt2 was upregulated in hepatitis B virus (HBV) WT-replicating cells, leading to tubulin deacetylation; however, this was not the case in HBV replication-deficient mutant-transfected cells and 1.3mer HBV WT-transfected plus reverse transcriptase inhibitor (entecavir or lamivudine) treated cells but all HBV proteins are expressed...
August 15, 2018: Journal of Virology
https://www.readbyqxmd.com/read/30108949/conformationally-restricted-benzothienoazepine-respiratory-syncytial-virus-inhibitors-their-synthesis-structural-analysis-and-biological-activities
#12
Euan A F Fordyce, S Fraser Hunt, Damien Crepin, Stuart T Onions, Guillaume F Parra, Chris J Sleigh, John King-Underwood, Harry Finch, John Murray
Atropisomeric drug substances are known to have different biological properties. Compounds containing the N -benzoylbenzazepine motif have been shown to exhibit energetically restricted rotation around the Ar(CO)N axis. Herein we report, for the first time, the synthesis, physical characterisation and anti-viral profiles of a series of C-4 and C-5 methylated thieno-benzazepines. NMR analysis reveals that incorporation of a single additional substituent at either of these loci influences the conformational dynamics of the azepine ring system...
March 1, 2018: MedChemComm
https://www.readbyqxmd.com/read/30108947/structure-guided-approach-identifies-a-novel-class-of-hiv-1-ribonuclease-h-inhibitors-binding-mode-insights-through-magnesium-complexation-and-site-directed-mutagenesis-studies
#13
Vasanthanathan Poongavanam, Angela Corona, Casper Steinmann, Luigi Scipione, Nicole Grandi, Fabiana Pandolfi, Roberto Di Santo, Roberta Costi, Francesca Esposito, Enzo Tramontano, Jacob Kongsted
Persistent HIV infection requires lifelong treatment and among the 2.1 million new HIV infections that occur every year there is an increased rate of transmitted drug-resistant mutations. This fact requires a constant and timely effort in order to identify and develop new HIV inhibitors with innovative mechanisms. The HIV-1 reverse transcriptase (RT) associated ribonuclease H (RNase H) is the only viral encoded enzyme that still lacks an efficient inhibitor despite the fact that it is a well-validated target whose functional abrogation compromises viral infectivity...
March 1, 2018: MedChemComm
https://www.readbyqxmd.com/read/30107464/hsp90-inhibitor-at-533-blocks-hsv-1-nuclear-egress-and-assembly
#14
Feng Li, Fujun Jin, Yiliang Wang, Danlin Zheng, Junwei Liu, Zhen Zhang, Rongze Wang, Dong Dong, Kai Zheng, Yifei Wang
Heat shock protein 90 (Hsp90) has been identified as an essential host factor for the infection and replication of several viruses, including HSV-1. Recent works have clearly shown that Hsp90 plays a role in the early stages of HSV-1 infection, including nuclear import and DNA replication. However, the role of Hsp90 in the late stages of HSV-1 infection remains unclear. In this study, we found that Hsp90 was up-regulated during late viral infection. Treatment with the Hsp90 inhibitor AT-533 significantly decreased the intracellular and extracellular virus titer, and strongly inhibited nucleocapsid egress from the nucleus...
August 10, 2018: Journal of Biochemistry
https://www.readbyqxmd.com/read/30107298/resistance-of-high-fitness-hepatitis-c-virus-to-lethal-mutagenesis
#15
Isabel Gallego, Josep Gregori, María Eugenia Soria, Carlos García-Crespo, Mónica García-Álvarez, Alfonso Gómez-González, Rosalie Valiergue, Jordi Gómez, Juan Ignacio Esteban, Josep Quer, Esteban Domingo, Celia Perales
Viral fitness quantifies the degree of virus adaptation to a given environment. How viral fitness can influence the mutant spectrum complexity of a viral quasispecies subjected to lethal mutagenesis has not been investigated. Here we document that two high fitness hepatitis C virus populations display higher resistance to the mutagenic nucleoside analogues favipiravir and ribavirin than their parental, low fitness HCV. All populations, however, exhibited a mutation transition bias indicative of active mutagenesis...
August 11, 2018: Virology
https://www.readbyqxmd.com/read/30104275/nitazoxanide-inhibits-human-norovirus-replication-and-synergizes-with-ribavirin-by-activation-of-cellular-antiviral-response
#16
Wen Dang, Lei Xu, Buyun Ma, Sunrui Chen, Yuebang Yin, Kyeong-Ok Chang, Maikel P Peppelenbosch, Qiuwei Pan
Norovirus is the main cause of viral gastroenteritis worldwide. Although norovirus gastroenteritis is self-limiting in immunocompetent individuals, chronic infections with debilitating and life-threatening complications occur in immunocompromised patients. Nitazoxanide (NTZ) has been empirically used in the clinic and demonstrated effectiveness against norovirus gastroenteritis. In this study we aimed at uncovering the antiviral potential and mechanisms of NTZ and its active metabolite, tizoxanide (TIZ) using a human norovirus (HuNV) replicon...
August 13, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/30104246/glucagon-like-peptide-1-and-its-cleavage-products-are-renoprotective-in-murine-diabetic-nephropathy
#17
Moellmann Julia, Klinkhammer Barbara Mara, Onstein Julia, Stöhr Robert, Jankowski Vera, Jankowski Joachim, Lebherz Corinna, Tacke Frank, Marx Nikolaus, Boor Peter, Lehrke Michael
Incretin based therapies, including GLP-1 receptor agonists and dipeptidylpeptidase 4 (DPP-4) inhibitors, are potent glucose lowering drugs. Still, only GLP-1 receptor agonists with close peptide homology to GLP-1 (liraglutide and semaglutide) but neither exenatide based GLP-1 receptor agonists nor DPP-4 inhibitors were found to reduce cardiovascular events. This different response might relate to GLP-1 receptor independent actions of GLP-1 caused by cleavage products only liberated by GLP-1 receptor agonists with close peptide structure to GLP-1...
August 13, 2018: Diabetes
https://www.readbyqxmd.com/read/30103947/role-of-c-myb-in-the-regulation-of-natural-killer-cell-activity
#18
Hee-Wook Shin, Yoo-Jin Lee, Jongsun Kim
The regulation of natural killer (NK) cell activity is an important research goal for the development of immunotherapies. In this study, we identified transcription factors affecting NK cell activity. In particular, we screened transcription factors affected by interleukin-2 (IL-2) and transforming growth factor-beta (TGF-β) by protein/DNA arrays using primary NK cells. We found that celastrol, a c-Myb inhibitor, inhibited NK-92 cells more strongly than any other inhibitors of transcription factor candidates...
August 10, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/30102858/a-small-molecule-compound-has-anti-influenza-a-virus-activity-by-acting-as-a-pb2-inhibitor
#19
Teng Liu, Miaomiao Liu, Feimin Chen, Fangzhao Chen, Yuanxin Tian, Qi Huang, Shu-Wen Liu, Jie Yang
With regular influenza epidemics and the emergence of drug-resistant virus strains, it is extremely crucial to develop effective and low-toxicity anti-influenza A virus drugs that act on conserved sites of novel targets. Here, we identified a novel anti-influenza compound, 1,3-dihydroxy-6-benzo [c] chromene (D715-2441), from a library of 8,026 small molecule compounds using cell-based influenza A infection assays and explored the underlying mechanisms. Our results revealed that D715-2441 possessed antiviral activities against multiple subtypes of influenza A viruses, including H1N1, H3N2, H5N1, H7N9, the clinical isolate 690 (H3 subtype) and oseltamivir-resistant strains with an NA-H274Y mutation, and suppressed the early steps in the virus replication cycle...
August 13, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/30102144/evaluation-of-anticoagulant-agents-for-the-treatment-of-human-metapneumovirus-infection-in-mice
#20
Ba Vuong Lê, Martine Jandrot-Perrus, Christian Couture, Liva Checkmahomed, Marie-Christine Venable, Marie-Ève Hamelin, Guy Boivin
Thrombin has been demonstrated to be involved in several viral diseases including human metapneumovirus (hMPV) infections. We previously showed that immediate administration of thrombin inhibitor argatroban post-infection protected mice against hMPV disease. This current work aims at determining whether warfarin and heparin, two other anticoagulants inhibiting thrombin formation and activities, may also be used for treatment against hMPV in vivo. We found that immediate injections of argatroban, warfarin or heparin after virus challenge protected mice against hMPV infection, as evidenced by decreased or no mortality, less weight loss, reduced viral load and attenuated inflammation...
August 10, 2018: Journal of General Virology
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