9,232 results match your criteria Biologics: Targets & Therapy[Journal]


Network-based methods for predicting essential genes or proteins: a survey.

Brief Bioinform 2019 Feb 18. Epub 2019 Feb 18.

School of Computer Science and Engineering, Central South University, Changsha, Hunan, China.

Genes that are thought to be critical for the survival of organisms or cells are called essential genes. The prediction of essential genes and their products (essential proteins) is of great value in exploring the mechanism of complex diseases, the study of the minimal required genome for living cells and the development of new drug targets. As laboratory methods are often complicated, costly and time-consuming, a great many of computational methods have been proposed to identify essential genes/proteins from the perspective of the network level with the in-depth understanding of network biology and the rapid development of biotechnologies. Read More

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http://dx.doi.org/10.1093/bib/bbz017DOI Listing
February 2019

Structural and biochemical insights into the catalytic mechanisms of two insect chitin deacetylases of the carbohydrate esterase 4 family.

J Biol Chem 2019 Feb 12. Epub 2019 Feb 12.

Dalian University of Technology, China.

Insect chitin deacetylases (CDAs) catalyze the removal of acetyl groups from chitin and modify this polymer during its synthesis and reorganization. CDAs are essential for insect survival and therefore represent promising targets for insecticide development. However, the structural and biochemical characteristics of insect CDAs have remained elusive. Read More

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http://dx.doi.org/10.1074/jbc.RA119.007597DOI Listing
February 2019
4.573 Impact Factor

Regioselectivity Switch in Palladium-Catalyzed Allenylic Cycloadditions of Allenic Esters: [4+1] or [4+3] Cycloaddition/Cross-Coupling by Ligands.

Angew Chem Int Ed Engl 2019 Feb 11. Epub 2019 Feb 11.

CHINA.

The first Pd-catalyzed asymmetric allenylic [4+1] cycloaddition was successfully developed. Alternatively, tuning Pd catalysts switched the reactivity toward an unprecedented [4+3] cycloaddition/cross coupling. Ligands play a vital role in controlling the reaction pathway, allowing highly selective access to different products from identical substrates. Read More

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http://dx.doi.org/10.1002/anie.201901511DOI Listing
February 2019
1 Read

Non-volatile pungent compounds isolated from Zingiber officinale and their mechanisms of action.

Food Funct 2019 Feb 11. Epub 2019 Feb 11.

Institute of Traditional Chinese Medicine & Natural Products, and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, P. R. China.

In this study, an efficient strategy developed by integrating UPLC-Q/TOF-MS, network pharmacology, and molecular simulation, was proposed and applied for rapidly screening bioactive candidates from ginger. A UPLC-Q/TOF MS-guided isolation targeting non-volatile pungent compounds resulted in the isolation and identification of 19 compounds in the rhizome of Zingiber officinale, including six new compounds (1-6). Based on target prediction and Gene Ontology (GO), the primary biological function of compounds was predicted to be associated with cancer and the key target was VEGFR2 (vascular endothelial growth factor receptor 2). Read More

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http://xlink.rsc.org/?DOI=C8FO02019A
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http://dx.doi.org/10.1039/c8fo02019aDOI Listing
February 2019
2 Reads

The management of diabetes mellitus-imperative role of natural products against dipeptidyl peptidase-4, α-glucosidase and sodium-dependent glucose co-transporter 2 (SGLT2).

Bioorg Chem 2019 Feb 4;86:305-315. Epub 2019 Feb 4.

Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy. Electronic address:

Diabetes mellitus is a chronic metabolic disorder which is rapidly spreading worldwide. It is characterized by persistent elevated blood glucose level above normal values (hyperglycemia) due to defect in either insulin secretion or in insulin action or both of them. Currently approved oral synthetic antidiabetic drugs such as biguanides, thiazolidinediones, sulfonylureas, and meglitinides have shown undesirable side effects. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.02.009DOI Listing
February 2019
1 Read

The Use of Rheumatic Disease Comorbidity Index for Predicting Clinical Response and Retention Rate in a Cohort of Rheumatoid Arthritis Patients Receiving Tumor Necrosis Factor Alpha Inhibitors.

Biomed Res Int 2019 10;2019:6107217. Epub 2019 Jan 10.

Department of Rheumatology, Gaetano Pini Institute, Milan, Italy.

Introduction: To retrospectively evaluate the impact of comorbidities on treatment choice, 12-month clinical response, and 24-month retention rate in a cohort of patients with rheumatoid arthritis (RA) treated with a first-line tumor necrosis factor alpha inhibitor (TNFi), by using for the first time the Rheumatic Disease Comorbidity Index (RDCI).

Methods: The study population was extracted from a local registry of RA patients receiving adalimumab or etanercept as first-line biologics between January 2001 and December 2013. The prevalence of comorbidities was computed, and patients were stratified according to RDCI for evaluating the role of comorbidities on TNFi choice, concomitant methotrexate, clinical response (1-year DAS28-ESR remission and low disease activity [LDA] and EULAR good-moderate response), and the 24-month retention rate. Read More

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http://dx.doi.org/10.1155/2019/6107217DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6348828PMC
January 2019
1 Read

Antibodies and venom peptides: new modalities for ion channels.

Nat Rev Drug Discov 2019 Feb 6. Epub 2019 Feb 6.

Department of Physiology & Membrane Biology, University of California Davis, Davis, CA, USA.

Ion channels play fundamental roles in both excitable and non-excitable tissues and therefore constitute attractive drug targets for myriad neurological, cardiovascular and metabolic diseases as well as for cancer and immunomodulation. However, achieving selectivity for specific ion channel subtypes with small-molecule drugs has been challenging, and there currently is a growing trend to target ion channels with biologics. One approach is to improve the pharmacokinetics of existing or novel venom-derived peptides. Read More

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http://www.nature.com/articles/s41573-019-0013-8
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http://dx.doi.org/10.1038/s41573-019-0013-8DOI Listing
February 2019
7 Reads

Diet, Gut Microbiota, and Obesity: Links with Host Genetics and Epigenetics and Potential Applications.

Adv Nutr 2019 Jan;10(suppl_1):S17-S30

Department of Nutrition, Food Science, and Physiology and Center for Nutrition Research, University of Navarra, Pamplona, Spain.

Diverse evidence suggests that the gut microbiota is involved in the development of obesity and associated comorbidities. It has been reported that the composition of the gut microbiota differs in obese and lean subjects, suggesting that microbiota dysbiosis can contribute to changes in body weight. However, the mechanisms by which the gut microbiota participates in energy homeostasis are unclear. Read More

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http://dx.doi.org/10.1093/advances/nmy078DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6363528PMC
January 2019
2 Reads

A Novel T-Cell Engaging Bi-specific Antibody Targeting the Leukemia Antigen PR1/HLA-A2.

Front Immunol 2018 18;9:3153. Epub 2019 Jan 18.

Department of Stem Cell Transplantation and Cellular Therapy, University of Texas MD Anderson Cancer Center, Houston, TX, United States.

Despite substantial advances in the treatment of acute myeloid leukemia (AML), only 30% of patients survive more than 5 years. Therefore, new therapeutics are much needed. Here, we present a novel therapeutic strategy targeting PR1, an HLA-A2 restricted myeloid leukemia antigen. Read More

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http://dx.doi.org/10.3389/fimmu.2018.03153DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6345694PMC
January 2019
1 Read

Inhibition of HBV Transcription From cccDNA With Nitazoxanide by Targeting the HBx-DDB1 Interaction.

Cell Mol Gastroenterol Hepatol 2018 Oct 24;7(2):297-312. Epub 2018 Oct 24.

Department of Gastroenterology, Graduate School of Medicine, University of Tokyo, Tokyo, Japan.

Background & Aims: Hepatitis B virus (HBV) infection is a major health concern worldwide. Although currently used nucleos(t)ide analogs efficiently inhibit viral replication, viral proteins transcribed from the episomal viral covalently closed circular DNA (cccDNA) minichromosome continue to be expressed long-term. Because high viral RNA or antigen loads may play a biological role during this chronicity, the elimination of viral products is an ultimate goal of HBV treatment. Read More

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http://dx.doi.org/10.1016/j.jcmgh.2018.10.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6357790PMC
October 2018
2 Reads

Oxidative Response and Micronucleus Centromere Assay in HEp-2 Cells Exposed to Fungicide Iprodione.

Chem Res Toxicol 2019 Feb 14. Epub 2019 Feb 14.

GIBE (Grupo de Investigación en Biología Evolutiva), FCEyN-UBA, Facultad de Ciencias Exactas y Naturales, Instituto de Ecología, Genética y Evolución de Buenos Aires - Consejo de Investigaciones Científicas y Técnicas) , Universidad de Buenos Aires (IEGEBA-CONICET) , Ciudad Universitaria, Pabellón II, 4° Piso Laboratories. 43-46 , C1428EGA Buenos Aires , Argentina.

The fungicide agents are a key component in the fruits and vegetables production. The Iprodione residues are one of the pesticide more frequently found in food products. The available data about the cytotoxicity of iprodione and its metabolites are scarce and do not allow characterization of its genotoxic potential and define the risk assessment. Read More

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http://dx.doi.org/10.1021/acs.chemrestox.8b00405DOI Listing
February 2019
1 Read

Diagnose und Monitoring bei chronisch-entzündlicher Darmerkrankung.

Ther Umsch 2019 Jan;75(5):316-328

1 Gastroenterologie und Hepatologie, Medizinische Universitätsklinik, Kantonsspital Baselland.

Diagnosis and Monitoring of Inflammatory Bowel Disease Abstract. The diagnosis and monitoring of inflammatory bowel disease (IBD) is based on several factors: Clinical history, physical examination, laboratory values (blood and stool), endoscopy, histology and imaging. No single feature establishes the diagnosis alone. Read More

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http://dx.doi.org/10.1024/0040-5930/a001002DOI Listing
January 2019

Computational Studies Applied to Flavonoids against Alzheimer's and Parkinson's Diseases.

Oxid Med Cell Longev 2018 30;2018:7912765. Epub 2018 Dec 30.

Postgraduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, João Pessoa, PB, Brazil.

Neurodegenerative diseases, such as Parkinson's and Alzheimer's, are understood as occurring through genetic, cellular, and multifactor pathophysiological mechanisms. Several natural products such as flavonoids have been reported in the literature for having the capacity to cross the blood-brain barrier and slow the progression of such diseases. The present article reports on enzymatic target studies and natural products as inhibitors for the treatment of Parkinson's and Alzheimer's diseases. Read More

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http://dx.doi.org/10.1155/2018/7912765DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332933PMC
December 2018
2 Reads

The Pseudo Natural Product Myokinasib Is a Myosin Light Chain Kinase 1 Inhibitor with Unprecedented Chemotype.

Cell Chem Biol 2018 Dec 11. Epub 2018 Dec 11.

Max Planck Institute for Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, Dortmund 44227, Germany; Technische Universität Dortmund, Faculty of Chemistry and Chemical Biology, Otto-Hahn-Strasse 6, Dortmund 44227, Germany. Electronic address:

Small-molecule chemotypes with unexpected bioactivity may be identified by combining strategies built on the biological relevance of, e.g., natural products (NPs), such as biology-oriented synthesis, with principles that enable efficient coverage of chemical space, such as fragment-based compound design. Read More

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http://dx.doi.org/10.1016/j.chembiol.2018.11.014DOI Listing
December 2018

The Journey of Schinortriterpenoid Total Syntheses.

Authors:
Zhen Yang

Acc Chem Res 2019 Jan 25. Epub 2019 Jan 25.

Beijing National Laboratory for Molecular Science and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of the Ministry of Education, College of Chemistry and Molecular Engineering and Peking-Tsinghua Center for Life Sciences , Peking University , Beijing 100871 , China.

Plants in the Schisandraceae family are important components of the traditional Chinese herbal medicines and are often used to treat various illnesses. Therefore, these Schisandraceae plants are valuable sources for the discovery of new chemical entities for novel therapeutic development. Considerable progress has been made in the identification of bioactive and structurally novel triterpenoids from the Schisandraceae family in the past two decades. Read More

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http://dx.doi.org/10.1021/acs.accounts.8b00569DOI Listing
January 2019

Walnut oil improves spatial memory in rats and increases the expression of acid-sensing ion channel genes Asic2a and Asic4.

Food Sci Nutr 2019 Jan 28;7(1):293-301. Epub 2018 Nov 28.

College of Biological and Pharmaceutical Engineering Wuhan Polytechnic University Wuhan China.

Although Walnut oil (WO) has been reported to enhance cognitive function, the underlying molecular mechanisms are not well understood. This study was designed to assess the effects of WO on spatial memory in rats through modulation of the expression of acid-sensing ion channel genes, and . To investigate the effect of WO on cognitive performance, we supplemented the diet of female rats with WO. Read More

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http://doi.wiley.com/10.1002/fsn3.889
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http://dx.doi.org/10.1002/fsn3.889DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6341134PMC
January 2019
2 Reads

Biotransformed Metabolites of the Hop Prenylflavanone Isoxanthohumol.

Molecules 2019 Jan 22;24(3). Epub 2019 Jan 22.

College of Pharmacy, Chonnam National University, Gwangju 61186, Korea.

A metabolic conversion study on microbes is known as one of the most useful tools to predict the xenobiotic metabolism of organic compounds in mammalian systems. The microbial biotransformation of isoxanthohumol (1), a major hop prenylflavanone in beer, has resulted in the production of three diastereomeric pairs of oxygenated metabolites (⁻). The microbial metabolites of 1 were formed by epoxidation or hydroxylation of the prenyl group, and HPLC, NMR, and CD analyses revealed that all of the products were diastereomeric pairs composed of (2S)- and (2R)- isomers. Read More

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http://dx.doi.org/10.3390/molecules24030394DOI Listing
January 2019

Regulated Cell Death Signaling Pathways and Marine Natural Products That Target Them.

Authors:
Esther A Guzmán

Mar Drugs 2019 Jan 23;17(2). Epub 2019 Jan 23.

Marine Biomedical and Biotechnology Research, Harbor Branch Oceanographic Institute at Florida Atlantic University, 5600 US 1 North, Fort Pierce, FL 34946, USA.

Our understanding of cell death used to consist in necrosis, an unregulated form, and apoptosis, regulated cell death. That understanding expanded to acknowledge that apoptosis happens through the intrinsic or extrinsic pathways. Actually, many other regulated cell death processes exist, including necroptosis, a regulated form of necrosis, and autophagy-dependent cell death. Read More

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http://dx.doi.org/10.3390/md17020076DOI Listing
January 2019

Current state of knowledge on the health effects of engineered nanomaterials in workers: a systematic review of human studies and epidemiological investigations.

Scand J Work Environ Health 2019 Jan 17. Epub 2019 Jan 17.

National Institute for Occupational Safety and Health, Centers for Disease Control and Prevention, 1150 Tusculum Avenue, MS C-14, Cincinnati, OH 45226, USA.

Objectives The widespread application of nano-enabled products and the increasing likelihood for workplace exposures make understanding engineered nanomaterial (ENM) effects in exposed workers a public and occupational health priority. The aim of this study was to report on the current state of knowledge on possible adverse effects induced by ENM in humans to determine the toxicological profile of each type of ENM and potential biomarkers for early detection of such effects in workers. Methods A systematic review of human studies and epidemiological investigations of exposed workers relative to the possible adverse effects for the most widely used ENM was performed through searches of major scientific databases including Web of Science, Scopus, and PubMed. Read More

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http://www.sjweh.fi/show_abstract.php?abstract_id=3800
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http://dx.doi.org/10.5271/sjweh.3800DOI Listing
January 2019
7 Reads

Fasciola gigantica: Comparison of the tegumental ultrastructure in newly excysted metacercariae and in vitro penetrated juvenile flukes indicates intracellular sources of molecules with vaccinal and immunomodulatory potential.

Vet Parasitol 2019 Jan 7;265:38-47. Epub 2018 Dec 7.

School of Biological Sciences, The Queen's University of Belfast, Belfast, BT9 7BL, United Kingdom.

Using in vitro procedures to prepare newly excysted metacercariae and gut-penetrated juvenile Fasciola gigantica, the ultrastructural features of the tegumental syncytium and perikarya of these ephemeral stages in the host-invasion process were compared. The T0-type tegumental cells in newly excysted metacercariae are packed with stored T0 granules which, following transport to the surface membrane of the syncytium, discharge by exocytosis to maintain the glycocalyx. The T0 cells become depleted of T0 granules during the penetration process, shrink in size, and initiate autophagy in the cytoplasm to facilitate metamorphosis from a storage function to active biosynthesis. Read More

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http://dx.doi.org/10.1016/j.vetpar.2018.11.019DOI Listing
January 2019
2 Reads

Efficacy and safety of Yinchen Sini decoction in treating biliary atresia patients after Kasai portoenterostomy: A systematic review and meta-analysis protocol.

Medicine (Baltimore) 2019 Jan;98(2):e13935

Department of paediatrics, First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, China.

Background: Biliary atresia (BA) is a neonatal obstructive biliary tract disease in which the intrahepatic and extrahepatic bile ducts are obstructed and can lead to congenital biliary atresia of cholestatic cirrhosis and eventually liver failure. It has been confirmed that the Kasai portoenterostomy is an effective treatment for BA. But most patients still face complications, such as cholangitis and liver fibrosis. Read More

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http://dx.doi.org/10.1097/MD.0000000000013935DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6336556PMC
January 2019
2 Reads

Studying the mechanisms and targets of glycation and advanced glycation end-products in simple eukaryotic model systems.

Int J Biol Macromol 2019 Jan 8;127:85-94. Epub 2019 Jan 8.

Centro de Investigación y de Estudios Avanzados del IPN - Unidad Monterrey, Parque de Investigación e Innovación Tecnológica, Apodaca, Nuevo León CP 66600, Mexico. Electronic address:

Biological systems are usually astonishingly complex. This complexity makes it often difficult if not impossible to study their inner workings. In order to address complex research questions more simply structured models (e. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S01418130183526
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http://dx.doi.org/10.1016/j.ijbiomac.2019.01.032DOI Listing
January 2019
2 Reads

Using the drug-protein interactome to identify anti-ageing compounds for humans.

PLoS Comput Biol 2019 Jan 9;15(1):e1006639. Epub 2019 Jan 9.

Institute of Healthy Ageing, Department of Genetics, Evolution and Environment, University College London, London, United Kingdom.

Advancing age is the dominant risk factor for most of the major killer diseases in developed countries. Hence, ameliorating the effects of ageing may prevent multiple diseases simultaneously. Drugs licensed for human use against specific diseases have proved to be effective in extending lifespan and healthspan in animal models, suggesting that there is scope for drug repurposing in humans. Read More

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http://dx.doi.org/10.1371/journal.pcbi.1006639DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6342327PMC
January 2019
3 Reads

Biological Products: Cellular Therapy and FDA Approved Products.

Stem Cell Rev 2019 Jan 9. Epub 2019 Jan 9.

Department of Biology, School of Advanced Technologies in Medicine, Islamic Azad University Medical Branch of Tehran, Tehran, Iran.

The pace of advances in the world of science have created new opportunities and insights that give us new and more understanding of our nature and environment. Among the different fields of science, new medical sciences have drawn a great deal of attention among medical science researchers and the society. The hope for finding treatments for incurable diseases and further improvement of man's health is growing thanks to new medical technologies. Read More

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http://dx.doi.org/10.1007/s12015-018-9866-1DOI Listing
January 2019
2 Reads

Colorectal cancer vaccines: Tumor-associated antigens neoantigens.

World J Gastroenterol 2018 Dec;24(48):5418-5432

Section of Molecular Oncology and Immunotherapy, General Surgery, University Medical Center, Rostock D-18057, Germany.

Therapeutic options for the treatment of colorectal cancer (CRC) are diverse but still not always satisfying. Recent success of immune checkpoint inhibition treatment for the subgroup of CRC patients suffering from hyper-mutated tumors suggests a permanent role of immune therapy in the clinical management of CRC. Substantial improvement in treatment outcome could be achieved by development of efficient patient-individual CRC vaccination strategies. Read More

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https://www.wjgnet.com/1007-9327/full/v24/i48/5418.htm
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http://dx.doi.org/10.3748/wjg.v24.i48.5418DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6319136PMC
December 2018
11 Reads

Slt, MltD, and MltG of Pseudomonas aeruginosa as Targets of Bulgecin A in Potentiation of β-Lactam Antibiotics.

ACS Chem Biol 2019 Feb 18;14(2):296-303. Epub 2019 Jan 18.

Department of Chemistry and Biochemistry , University of Notre Dame , 352 McCourtney Hall , Notre Dame , Indiana 46556 , United States.

The interplay between the activities of lytic transglycosylases (LTs) and penicillin-binding proteins (PBPs) is critical for the health of the bacterial cell wall. Bulgecin A (a natural-product inhibitor of LTs) potentiates the activity of β-lactam antibiotics (inhibitors of PBPs), underscoring this intimate mechanistic interdependence. Bulgecin A in the presence of an appropriate β-lactam causes bulge deformation due to the formation of aberrant peptidoglycan at the division site of the bacterium. Read More

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http://dx.doi.org/10.1021/acschembio.8b01025DOI Listing
February 2019
2 Reads

Bicyclic acetals: biological relevance, scaffold analysis, and applications in diversity-oriented synthesis.

Org Biomol Chem 2019 01;17(5):1037-1052

Department of Chemistry "Ugo Schiff", University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy.

Natural products (NPs) have been shown to be an extraordinary source of bioactive compounds and three-dimensional complex frameworks that can be useful to produce high-value molecular collections that are able to address "undruggable" and difficult therapeutic targets. Bicyclic acetals are particularly relevant for these purposes, given their key role in several biological interactions and the structural and stereochemical diversity that comes from the many possible ring combinations. To investigate this topological diversity, we have systematically characterized in a systematic and detailed manner fused, spiro and bridged bicyclic acetals in a large set of NPs, highlighting the great potential of bicyclic acetals in Diversity-Oriented Synthesis (DOS). Read More

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http://dx.doi.org/10.1039/c8ob02808gDOI Listing
January 2019
1 Read

Herbal Medicines with Antiviral Activity Against the Influenza Virus, a Systematic Review.

Am J Chin Med 2018 ;46(8):1663-1700

* Food Animal Health Research Program, Ohio Agricultural Research and Development Center, The Ohio State University, Columbus, Ohio, USA.

The rapidly changing influenza virus has remained a consistent threat to the well-being of a variety of species on the planet. Influenza virus' high mutation rate has allowed the virus to rapidly and continuously evolve, as well as generate new strains that are resistant to the current commercially available antivirals. Thus, the increased resistance has compelled the scientific community to explore alternative compounds that have antiviral effects against influenza virus. Read More

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https://www.worldscientific.com/doi/abs/10.1142/S0192415X185
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http://dx.doi.org/10.1142/S0192415X18500854DOI Listing
February 2019
2 Reads

Multi-target natural products as alternatives against oxidative stress in Chronic Obstructive Pulmonary Disease (COPD).

Eur J Med Chem 2019 Feb 11;163:911-931. Epub 2018 Dec 11.

Programa de Pós-Graduação em Produtos Bioativos e Biociências - PPG-PRODBIO, Universidade Federal do Rio de Janeiro - Campus Macaé, NUPEM/UFRJ - Núcleo em Ecologia e Desenvolvimento Sócio-Ambiental de Macaé, Av. São José do Barreto, 764, 27965-045, Macaé, RJ, Brazil. Electronic address:

Chronic Obstructive Pulmonary Disease (COPD) is a major global health problem. Among other conditions, it has been associated with chronic airway and lung parenchyma inflammation. At present, the available therapies are not capable of reducing the progression or suppressing inflammation associated to COPD. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S02235234183105
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http://dx.doi.org/10.1016/j.ejmech.2018.12.020DOI Listing
February 2019
8 Reads

MicroRNAs and Long Non-coding RNAs in Genetic Diseases.

Mol Diagn Ther 2019 Jan 4. Epub 2019 Jan 4.

Department of Life Sciences and Biotechnology, Section of Biochemistry and Molecular Biology, University of Ferrara, Via Fossato di Mortara n.74, 44121, Ferrara, Italy.

Since the discovery and classification of non-coding RNAs, their roles have gained great attention. In this respect, microRNAs and long non-coding RNAs have been firmly demonstrated to be linked to regulation of gene expression and onset of human diseases, including rare genetic diseases; therefore they are suitable targets for therapeutic intervention. This issue, in the context of rare genetic diseases, is being considered by an increasing number of research groups and is of key interest to the health community. Read More

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http://link.springer.com/10.1007/s40291-018-0380-6
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http://dx.doi.org/10.1007/s40291-018-0380-6DOI Listing
January 2019
7 Reads

The Multiple Biological Targets of Hops and Bioactive Compounds.

Chem Res Toxicol 2019 Feb 22;32(2):222-233. Epub 2019 Jan 22.

Linus Pauling Institute , Oregon State University , 305 Linus Pauling Science Center , Corvallis , Oregon 97331 , United States.

Botanical dietary supplements for women's health are increasingly popular. Older women tend to take botanical supplements such as hops as natural alternatives to traditional hormone therapy to relieve menopausal symptoms. Especially extracts from spent hops, the plant material remaining after beer brewing, are enriched in bioactive prenylated flavonoids that correlate with the health benefits of the plant. Read More

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http://dx.doi.org/10.1021/acs.chemrestox.8b00345DOI Listing
February 2019
2 Reads

Cytoplasmic glycoengineering of Apx toxin fragments in the development of Actinobacillus pleuropneumoniae glycoconjugate vaccines.

BMC Vet Res 2019 Jan 3;15(1). Epub 2019 Jan 3.

Department of Pathogen Molecular Biology, London School of Hygiene and Tropical Medicine, Keppel Street, London, WC1E 7HT, UK.

Background: Actinobacillus pleuropneumoniae is the causative agent of porcine pleuropneumonia and represents a major burden to the livestock industry. Virulence can largely be attributed to the secretion of a series of haemolytic toxins, which are highly immunogenic. A. Read More

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http://dx.doi.org/10.1186/s12917-018-1751-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6318927PMC
January 2019
2 Reads

Bio-guided profiling and HPLC-DAD finger printing of Atriplex lasiantha Boiss.

BMC Complement Altern Med 2019 Jan 3;19(1). Epub 2019 Jan 3.

Department of Chemistry, University of Malakand, Khyber Pakhtunkhwa, 18000, Pakistan.

Background: Plants represent an intricate and innovative source for the discovery of novel therapeutic remedies for the management of various ailments. The current study has been aimed to validate the therapeutic potential of ethnomedicinally significant plant Atriplex lasiantha Boiss.

Methods: The polarity based extraction process was carried out using fourteen solvents to figure out best extraction solvent and bioactive fractions. Read More

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http://dx.doi.org/10.1186/s12906-018-2416-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6318930PMC
January 2019
2 Reads
2.020 Impact Factor

Natural voltage-gated sodium channel ligands: Biosynthesis and biology.

Chembiochem 2019 Jan 3. Epub 2019 Jan 3.

UNITED STATES.

Natural product biosynthetic pathways are composed of enzymes that use powerful chemistry to assemble complex molecules. Small molecule neurotoxins are examples of natural products with intricate scaffolds which often have high affinities for their biological targets. The focus of this review is small molecule neurotoxins targeting voltage-gated sodium channels (VGSCs) and the state of knowledge on their associated biosynthetic pathways. Read More

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http://dx.doi.org/10.1002/cbic.201800754DOI Listing
January 2019
1 Read

Effect of Acceptor Chain Length and Hydrophobicity on Polymerization Kinetics of the Neisseria meningitidis Group C Polysialyltransferase.

Biochemistry 2019 Feb 16;58(6):679-686. Epub 2019 Jan 16.

Laboratory of Bacterial Polysaccharides , Center for Biologics Evaluation and Research , Silver Spring , Maryland 20993 , United States.

Polysialic acids (PSA) are important extracellular virulence factors of the human pathogens Neisseria meningitidis and Escherichia coli. The importance of these polysaccharides in virulence make the polysialyltransferases (PST) targets for therapeutic drugs and protein engineering to facilitate efficient vaccine production. Here, we have generated recombinant bovine nucleotide monophosphate kinase to facilitate steady state kinetic assays of the PST. Read More

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http://dx.doi.org/10.1021/acs.biochem.8b01114DOI Listing
February 2019
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Comparative analysis of the compatibility effects of Danggui-Sini Decoction on a blood stasis syndrome rat model using untargeted metabolomics.

J Chromatogr B Analyt Technol Biomed Life Sci 2019 Jan 22;1105:164-175. Epub 2018 Dec 22.

Pharmaceutical College, Guangxi Medical University, Nanning 530021, China. Electronic address:

Danggui-Sini Decoction (DSD) is one of the most widely used traditional Chinese medicine formulae (TCMF) for treating various diseases caused by cold coagulation and blood stasis due to its effect of nourishing blood to warm meridians in clinical use. However, studies of the mechanism of how it dispels blood stasis and its compatible regularity are challenging because of the complex pathophysiology of blood stasis syndrome (BSS) and the complexity of DSD, with multiple active ingredients acting on different targets. Observing variations of endogenous metabolites in rats with BSS after administering DSD may further our understanding of the mechanism of BSS and the compatible regularity of DSD. Read More

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http://dx.doi.org/10.1016/j.jchromb.2018.12.017DOI Listing
January 2019

Crosstalk between tumor necrosis factor-alpha signaling and aryl hydrocarbon receptor signaling in nuclear factor -kappa B activation: A possible molecular mechanism underlying the reduced efficacy of TNF-inhibitors in rheumatoid arthritis by smoking.

J Autoimmun 2018 Dec 24. Epub 2018 Dec 24.

Rheumatology and Allergology, NHO Osaka Minami Medical Center, Kidohigasi-machi, Kawachinagano, Osaka, 586-8521, Japan; Clinical Research, NHO Osaka Minami Medical Center, Kidohigasi-machi, Kawachinagano, Osaka, 586-8521, Japan. Electronic address:

Objectives: To examine the influence of smoking on biologics treatment against different therapeutic targets, such as TNFα, IL-6, and T cell, in rheumatoid arthritis (RA) and elucidate the underlying molecular mechanism.

Methods: The association between drug-discontinuation due to poor therapeutic response and smoking status was analyzed individually in biologics against different therapeutic targets by a multivariable logistic regression analysis using the "NinJa" Registry, one of the largest cohorts of Japanese RA patients. In vitro enhancement of TNFα-induced NF-κB activation and subsequent proinflammatory cytokine production by cigarette chemical components was examined by RT-PCR, qPCR, ELISA, and western blotting using an immortalized rheumatoid synovial cell line, MH7A. Read More

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http://dx.doi.org/10.1016/j.jaut.2018.12.004DOI Listing
December 2018
3 Reads

Targeting triple negative breast cancer heterogeneity with chalcones: a molecular insight.

J Drug Target 2018 Dec 24:1-9. Epub 2018 Dec 24.

a College of Pharmacy , Qatar University , Doha , Qatar.

Triple negative breast cancers (TNBCs) are aggressive heterogeneous cancers with not yet determined conventional targeted medication. Therefore, identification of new alternatives or improved treatment options to combat this deadly disease is highly needed. On the other hand, various derived products with chalcone scaffold were historically considered excellent candidates for the development of anticancer drugs. Read More

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http://dx.doi.org/10.1080/1061186X.2018.1561889DOI Listing
December 2018
2 Reads

Saponins as modulators of nuclear receptors.

Crit Rev Food Sci Nutr 2018 Dec 22:1-14. Epub 2018 Dec 22.

a College of Food Science and Engineering, Jilin University , Changchun , China.

As plant-derived natural products, saponins have been widely applied for the dietary modification of metabolic syndrome. However, the underlying mechanisms of their preventive and therapeutic effects are still largely unclear. Nuclear receptors have been identified as potential pharmaceutical targets for treating various types of metabolic disorders. Read More

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https://www.tandfonline.com/doi/full/10.1080/10408398.2018.1
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http://dx.doi.org/10.1080/10408398.2018.1514580DOI Listing
December 2018
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A review of lipidation in the development of advanced protein and peptide therapeutics.

J Control Release 2019 Feb 21;295:1-12. Epub 2018 Dec 21.

Department of Biomedical Engineering, Duke University, Durham, NC, USA. Electronic address:

The use of biologics (peptide and protein based drugs) has increased significantly over the past few decades. However, their development has been limited by their short half-life, immunogenicity and low membrane permeability, restricting most therapies to extracellular targets and administration by injection. Lipidation is a clinically-proven post-translational modification that has shown great promise to address these issues: improving half-life, reducing immunogenicity and enabling intracellular uptake and delivery across epithelia. Read More

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http://dx.doi.org/10.1016/j.jconrel.2018.12.032DOI Listing
February 2019
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Lipoproteins as targets and markers of lipoxidation.

Redox Biol 2018 Dec 6:101066. Epub 2018 Dec 6.

School of Life and Health Sciences, Aston University, Aston Triangle, Aston University, Birmingham B4 7ET, UK. Electronic address:

Lipoproteins are essential systemic lipid transport particles, composed of apolipoproteins embedded in a phospholipid and cholesterol monolayer surrounding a cargo of diverse lipid species. Many of the lipids present are susceptible to oxidative damage by lipid peroxidation, giving rise to the formation of reactive lipid peroxidation products (rLPPs). In view of the close proximity of the protein and lipid moieties within lipoproteins, the probability of adduct formation between rLPPs and amino acid residues of the proteins, a process called lipoxidation, is high. Read More

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http://dx.doi.org/10.1016/j.redox.2018.101066DOI Listing
December 2018
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Bispecific antibodies: The next generation of targeted inflammatory bowel disease therapies.

Autoimmun Rev 2019 Feb 17;18(2):123-128. Epub 2018 Dec 17.

Eli Lilly Biotechnology Center, Eli Lilly and Co, San Diego, CA, USA.

Targeting various disease pathways using monoclonal antibodies (mAbs) has transformed the treatment paradigm for inflammatory bowel disease (IBD), with these agents exhibiting improved efficacy over corticosteroids or immunosuppressive therapies. Antibodies targeting tumor necrosis factor α (TNF-α) were the first approved biologics for IBD, followed by the more recent approval of antibodies targeting the α4β7 integrin heterodimer and ustekinumab, which targets the p40 subunit of interleukin-23. Current efforts are focused on the development of additional biologics targeting these known and other newly discovered pathways. Read More

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http://dx.doi.org/10.1016/j.autrev.2018.07.014DOI Listing
February 2019
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Trimethylamine-N-oxide (TMAO)-induced atherosclerosis is associated with bile acid metabolism.

Lipids Health Dis 2018 Dec 19;17(1):286. Epub 2018 Dec 19.

College of Food Science and Engineering, Ocean University of China, No.5 Yushan Road, Qingdao, Shandong Province, 266003, People's Republic of China.

Background: Recently, trimethylamine-N-oxide (TMAO) plasma levels have been proved to be associated with atherosclerosis development. Among the targets aimed to ameliorating atherosclerotic lesions, inducing bile acid synthesis to eliminate excess cholesterol in body is an effective way. Individual bile acid as endogenous ligands for the nuclear receptor has differential effects on regulating bile acid metabolism. Read More

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http://dx.doi.org/10.1186/s12944-018-0939-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6300890PMC
December 2018
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Molecular Targets of Epigallocatechin-Gallate (EGCG): A Special Focus on Signal Transduction and Cancer.

Nutrients 2018 Dec 6;10(12). Epub 2018 Dec 6.

Department of Medicine and Surgery, University of Parma, Via Gramsci 14, 43126 Parma, Italy.

Green tea is a beverage that is widely consumed worldwide and is believed to exert effects on different diseases, including cancer. The major components of green tea are catechins, a family of polyphenols. Among them, epigallocatechin-gallate (EGCG) is the most abundant and biologically active. Read More

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http://dx.doi.org/10.3390/nu10121936DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6315581PMC
December 2018
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Design, synthesis and biological activity of hydrogen peroxide responsive arylboronate melatonin hybrids.

Chem Res Toxicol 2018 Dec 18. Epub 2018 Dec 18.

Stimulus-responsive cleavage reactions have found broad use to direct drug release at a particular target disease area. Increased levels of reactive oxygen species (ROS) have been associated with the development and progression of cancer and several other disease states, motivating the development of drug conjugates that can undergo a chemoselective ROS-triggered release. Melatonin (MLT) and the reactive electrophile p-benzoquinone methide (p-QM) have evidenced either cytoprotective and cytotoxic effects in biological systems, depending on the dose, cellular targets, and time of exposure. Read More

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http://dx.doi.org/10.1021/acs.chemrestox.8b00216DOI Listing
December 2018
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Multi-Target Drugs Against Metabolic Disorders.

Endocr Metab Immune Disord Drug Targets 2018 Dec 17. Epub 2018 Dec 17.

Postgraduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, João Pessoa - PB. Brazil.

In silico studies are increasingly being applied by researchers due to reductions in time and costs for new prototype synthesis; obtaining substances that present better therapeutic profiles. In the present work, in addition to discussing multi-target drug discovery and the contributions of in silico studies to rational bioactive planning against metabolic disorders such as diabetes and obesity, we review various in silico study contributions to the fight against human metabolic pathologies. Read More

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http://dx.doi.org/10.2174/1871530319666181217123357DOI Listing
December 2018
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Epidermal mTORC1 Signaling Contributes to the Pathogenesis of Psoriasis and Could Serve as a Therapeutic Target.

Authors:
Claudia Buerger

Front Immunol 2018 30;9:2786. Epub 2018 Nov 30.

Department of Dermatology, Venerology and Allergology, Clinic of the Goethe University, Frankfurt am Main, Germany.

Although modern biologics targeting different inflammatory mediators show promising therapeutic success, comprehensive knowledge about the molecular events in psoriatic keratinocytes that contribute to the pathogenesis and could serve as therapeutic targets is still scarce. However, recent efforts to understand the deregulated signal transduction pathways have led to the development of small molecule inhibitors e.g. Read More

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http://dx.doi.org/10.3389/fimmu.2018.02786DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6284005PMC
November 2018
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Erythrofordins D and E, two new cassaine-type diterpenes from Erythrophleum suaveolens.

Bioorg Med Chem Lett 2019 Jan 10;29(2):134-137. Epub 2018 Dec 10.

Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States; Molecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, United States. Electronic address:

Two new cassaine-type diterpenoids, namely erythrofordins D (1) and E (2), sourced from a Cameroon collection of Erythrophleum suaveolens were isolated and assessed for anti-tumor activity. In the NCI-60 cancer cell assay, erythrofordins D (1) and E (2) were found to be cytotoxic in the low micro molar ranges with a mean GI value of 2.45 and 0. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S0960894X183095
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http://dx.doi.org/10.1016/j.bmcl.2018.12.019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6330894PMC
January 2019
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Checkpoint-modulating immunotherapies in tumor treatment: Targets, drugs, and mechanisms.

Int Immunopharmacol 2019 Feb 12;67:160-175. Epub 2018 Dec 12.

Wuya College of Innovation, Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China; Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China. Electronic address:

Tumor immunotherapy, as a new treatment of cancer, has been developing on the basis of tumor immunology. Tumor immunotherapy stimulates and enhances the function of immune system in human bodies, in order to control and kill tumor cells. It is often used as an adjuvant therapy combined with surgery, chemotherapy, radiotherapy and other conventional methods. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S15675769183092
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http://dx.doi.org/10.1016/j.intimp.2018.12.006DOI Listing
February 2019
8 Reads