10,550 results match your criteria Biologics : targets & therapy[Journal]


Interactions of antithrombotic herbal medicines with Western cardiovascular drugs.

Pharmacol Res 2020 Jun 1:104963. Epub 2020 Jun 1.

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao SAR, 999078, China. Electronic address:

Thrombotic events act as a critical factor that interferes with Cardiovascular Diseases (CVDs), and antithrombotic herbal medicine is a long-standing controversial issue. Although a dispute is involved in their clinical application, all parties unanimously agree that herbal products have been widely used in folk medicine, and their interactions with conventional drugs are of high concern. This study aims to investigate how antithrombotic herbal medicines interact with Western cardiovascular drugs on the molecular level by taking an example of the most frequently used herbal pair, Danshen-Chuanxiong (DS-CX), and to discover more scientific evidence on their potential herbal-drug interactions. Read More

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http://dx.doi.org/10.1016/j.phrs.2020.104963DOI Listing

Peripheral blood transcriptome identifies high-risk benign and malignant breast lesions.

PLoS One 2020 4;15(6):e0233713. Epub 2020 Jun 4.

Huaxia Bangfu Technology Incorporated, Beijing, People's Republic of China.

Background: Peripheral blood transcriptome profiling is a potentially important tool for disease detection. We utilize this technique in a case-control study to identify candidate transcriptomic biomarkers able to differentiate women with breast lesions from normal controls.

Methods: Whole blood samples were collected from 50 women with high-risk breast lesions, 57 with breast cancers and 44 controls (151 samples). Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0233713PLOS

Extracts and Marine Algae Polysaccharides in Therapy and Prevention of Inflammatory Diseases of the Intestine.

Mar Drugs 2020 May 31;18(6). Epub 2020 May 31.

G.B. Elyakov Pacific Institute of Bioorganic Chemistry, FEB RAS, Vladivostok 690022, Russia.

Inflammatory bowel disease (IBD) is a serious public health problem worldwide. Current therapeutic strategies that use anti-inflammatory drugs, immunosuppressants, and biological treatments are often ineffective and have adverse health effects. In this regard, the use of natural compounds aimed at key pathogenic therapeutic targets in IBD attracts universal attention. Read More

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http://dx.doi.org/10.3390/md18060289DOI Listing

Dithranol targets keratinocytes, their crosstalk with neutrophils and inhibits the IL-36 inflammatory loop in psoriasis.

Elife 2020 Jun 2;9. Epub 2020 Jun 2.

Department of Dermatology, Medical University of Graz, Graz, Austria.

Despite the introduction of biologics, topical dithranol (anthralin) has remained one of the most effective anti-psoriatic agents. Serial biopsies from human psoriatic lesions and both the c-Jun/JunB and imiquimod psoriasis mouse model allowed us to study the therapeutic mechanism of this drug. Top differentially expressed genes in the early response to dithranol belonged to keratinocyte and epidermal differentiation pathways and IL-1 family members (i. Read More

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http://dx.doi.org/10.7554/eLife.56991DOI Listing

Controlling the Reproducibility of AC50 Estimation during Compound Profiling through Bayesian β-Expectation Tolerance Intervals.

SLAS Discov 2020 May 29:2472555220918201. Epub 2020 May 29.

Janssen R&D, Translational Medicine and Early Development Statistics, Beerse, Antwerpen, Belgium.

During drug discovery, compounds/biologics are screened against biological targets of interest to find drug candidates with the most desirable activity profile. The compounds are tested at multiple concentrations to understand the dose-response relationship, often summarized as AC50 values and used directly in ranking compounds. Differences between compound repeats are inevitable because of experimental noise and/or systematic error; however, it is often desired to detect the latter when it occurs. Read More

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http://dx.doi.org/10.1177/2472555220918201DOI Listing

Interleukin-29 regulates T follicular helper cells by repressing BCL6 in rheumatoid arthritis patients.

Clin Rheumatol 2020 May 28. Epub 2020 May 28.

Department of Rheumatology and Immunology, China-Japan Union Hospital, Jilin University, No.126 Xiantai Street, Changchun, 130033, Jilin, China.

Introduction: We aimed to investigate whether Interleukin-29 (IL-29) directly affects T follicular helper (Tfh) cell frequency in rheumatoid arthritis (RA), which are both related to RA-specific antibody responses.

Methods: Here, we explored the effect of IL-29 on Tfh cell production in RA patients using a combination of enzyme-linked immunosorbent assay (ELISA), flow cytometry (FCM), CD4 T cell culture, western blotting, and reverse transcription-polymerase chain reaction (RT-PCR).

Results: We reported that serum IL-29 levels, peripheral blood CD4CXCR5 Tfh cell frequency, CD4CXCR5CD40L Tfh cell frequency, and IL-28 receptor (IL-28Rα) and IL-10 receptor (IL-10R2) levels in peripheral blood Tfh cells were higher in RA patients than in healthy controls (HCs). Read More

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http://dx.doi.org/10.1007/s10067-020-05151-yDOI Listing

Oral Biologic Delivery: Advances Towards Oral Subunit, DNA and mRNA Vaccines and the Potential for Mass Vaccination During Pandemics.

Annu Rev Pharmacol Toxicol 2020 May 28. Epub 2020 May 28.

Division of Gastroenterology, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, USA; email:

Oral vaccination offers the promise of convenient, pain-free and self-administrable vaccine delivery. This is highly attractive in response to pandemic outbreaks where rapid mass vaccination is critical. Furthermore, oral vaccination produces mucosal, as well as systemic, immune responses, which protect against infection at mucosal surfaces. Read More

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http://dx.doi.org/10.1146/annurev-pharmtox-030320-092348DOI Listing

Collective Locomotion of Human Cells, Wound Healing and Their Control by Extracts and Isolated Compounds from Marine Invertebrates.

Molecules 2020 May 26;25(11). Epub 2020 May 26.

Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, 90128 Palermo, Italy.

The collective migration of cells is a complex integrated process that represents a common theme joining morphogenesis, tissue regeneration, and tumor biology. It is known that a remarkable amount of secondary metabolites produced by aquatic invertebrates displays active pharmacological properties against a variety of diseases. The aim of this review is to pick up selected studies that report the extraction and identification of crude extracts or isolated compounds that exert a modulatory effect on collective cell locomotion and/or skin tissue reconstitution and recapitulate the molecular, biochemical, and/or physiological aspects, where available, which are associated to the substances under examination, grouping the producing species according to their taxonomic hierarchy. Read More

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http://dx.doi.org/10.3390/molecules25112471DOI Listing

A Novel Vaccine Employing Non-Replicating Rabies Virus Expressing Chimeric SARS-CoV-2 Spike Protein Domains: Functional Inhibition of Viral/Nicotinic Acetylcholine Receptor Complexes.

Med Sci Monit 2020 May 28;26:e926016. Epub 2020 May 28.

Department of Psychiatry, First Faculty of Medicine Charles University in Prague and General University Hospital in Prague, Center for Cognitive and Molecular Neuroscience, Prague, Czech Republic.

The emergence of the novel ß-coronavirus, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has resulted in a global pandemic of coronavirus disease 2019 (COVID-19). Clinical studies have documented that potentially severe neurological symptoms are associated with SARS-CoV-2 infection, thereby suggesting direct CNS penetration by the virus. Prior studies have demonstrated that the destructive neurological effects of rabies virus (RABV) infections are mediated by CNS transport of the virus tightly bound to the nicotinic acetylcholine receptor (nAChR). Read More

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http://dx.doi.org/10.12659/MSM.926016DOI Listing

Matrix Metalloproteinases as New Targets in Alzheimer's Disease: Opportunities and Challenges.

J Med Chem 2020 May 27. Epub 2020 May 27.

Although matrix metalloproteinases (MMPs) are implicated in the regulation of numerous physiological processes, evidence of their pathological roles have also been obtained in the last decades, making MMPs attractive therapeutic targets for several diseases. Recent discoveries of their involvement in central nervous system (CNS) disorders, and in particular in Alzheimer's disease (AD), have paved the way to consider MMP modulators as promising therapeutic strategies. Over the past few decades, diverse approaches have been undertaken in the design of therapeutic agents targeting MMPs for various purposes, leading, more recently, to encouraging developments. Read More

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http://dx.doi.org/10.1021/acs.jmedchem.0c00352DOI Listing

The Effect of Short-Term Physical Activity on the Oxidative Stress in Rats with Different Stress Resistance Profiles in Cerebral Hypoperfusion.

Mol Neurobiol 2020 May 26. Epub 2020 May 26.

I. M. Sechenov First Moscow State Medical University of the Ministry of Health of the Russian Federation (Sechenov University), 8/2 Trubetskaya Str., Moscow, Russia, 119991.

Oxidative stress associated with chronic cerebral hypoperfusion is one of the fundamental factors leading to neurodegenerative diseases. To prevent oxidative stress, physical activity is effective. Physical exercise enables development of rehabilitation techniques that can progressively increase patients' stress resistance. Read More

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http://dx.doi.org/10.1007/s12035-020-01930-5DOI Listing

Complete Mitochondrial Genome of the Fungal Biocontrol Agent : Genomic Features, Comparative Analysis and Insight Into the Mitochondrial Evolution in .

Authors:
Yunyoung Kwak

Front Microbiol 2020 28;11:785. Epub 2020 Apr 28.

Écologie, Systématique et Évolution, CNRS, Université Paris Sud (Paris XI), Université Paris Saclay, AgroParisTech, Orsay, France.

The improvement of biopesticides for use in the agriculture industry requires an understanding of the biological- and ecological principles underlying their behavior in natural environments. The nuclear genomes of members of the genus , which are representative fungal biocontrol agents, have been actively studied in relation to the unique characteristics of these species as effective producers of CAZymes/secondary metabolites and biopesticides, but their mitochondrial genomes have received much less attention. In this study, the mitochondrial genome of (Hypocreales, Sordariomycetes), which targets wood-decaying fungal pathogens and has the ability to degrade chemical fungicides, was assembled . Read More

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http://dx.doi.org/10.3389/fmicb.2020.00785DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7228111PMC

Comprehensive analysis of the secreted proteome of adult Necator americanus hookworms.

PLoS Negl Trop Dis 2020 May 26;14(5):e0008237. Epub 2020 May 26.

Centre for Molecular Therapeutics, Australian Institute of Tropical Health and Medicine, James Cook University, Cairns, QLD, Australia.

The human hookworm Necator americanus infects more than 400 million people worldwide, contributing substantially to the poverty in these regions. Adult stage N. americanus live in the small intestine of the human host where they inject excretory/secretory (ES) products into the mucosa. Read More

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http://dx.doi.org/10.1371/journal.pntd.0008237DOI Listing

Fine-tuning bispecific therapeutics.

Authors:
Sung In Lim

Pharmacol Ther 2020 May 22:107582. Epub 2020 May 22.

Department of Chemical Engineering, Pukyong National University, Yongso-ro 45, Nam-gu, Busan, South Korea. Electronic address:

Bispecific therapeutics target two distinct antigens simultaneously and provide novel functionalities that are not attainable with single monospecific molecules or combinations of them. The unique potential of bispecific therapeutics is driving extensive efforts to discover synergistic dual targets, design molecular formats to integrate bispecific elements, and accelerate successful clinical translation. In particular, the past decade has witnessed a boom in the design and development of bispecific antibody formats with more than 100 collections to date. Read More

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http://dx.doi.org/10.1016/j.pharmthera.2020.107582DOI Listing

Venom-derived modulators of epilepsy-related ion channels.

Biochem Pharmacol 2020 May 20:114043. Epub 2020 May 20.

Griffith Institute for Drug Discovery, Griffith University, Nathan, QLD 4111, Australia. Electronic address:

Epilepsy is characterised by spontaneous recurrent seizures that are caused by an imbalance between neuronal excitability and inhibition. Since ion channels play fundamental roles in the generation and propagation of action potentials as well as neurotransmitter release at a subset of excitatory and inhibitory synapses, their dysfunction has been linked to a wide variety of epilepsies. Indeed, these unique proteins are the major biological targets for antiepileptic drugs. Read More

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http://dx.doi.org/10.1016/j.bcp.2020.114043DOI Listing

Role of microRNAs in Hemophilia and Thrombosis in Humans.

Int J Mol Sci 2020 May 20;21(10). Epub 2020 May 20.

OBRR/DBCD/LCH in the Center for Biologics Evaluation and Research, US Food and Drug Administration, Silver Spring, MD 20993, USA.

MicroRNAs (miRNA) play an important role in gene expression at the posttranscriptional level by targeting the untranslated regions of messenger RNA (mRNAs). These small RNAs have been shown to control cellular physiological processes including cell differentiation and proliferation. Dysregulation of miRNAs have been associated with numerous diseases. Read More

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http://dx.doi.org/10.3390/ijms21103598DOI Listing

An interim internal Threshold of Toxicologic Concern (iTTC) for chemicals in consumer products, with support from an automated assessment of ToxCast™ dose response data.

Regul Toxicol Pharmacol 2020 May 11;114:104656. Epub 2020 May 11.

The Procter & Gamble Company, Mason Business Center, 8700 Mason Montgomery Road, Cincinnati, OH, 45040, United States.

Additional non-animal methods are urgently needed to meet regulatory and animal welfare goals. TTC is a broadly used risk assessment tool. TTC based on external dose has limited utility for multi-route exposure and some types of structure activity relationship assessments. Read More

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http://dx.doi.org/10.1016/j.yrtph.2020.104656DOI Listing

Emerging roles of long non-coding RNAs in the p53 network.

Authors:
Abhinav K Jain

RNA Biol 2020 Jun 4:1-9. Epub 2020 Jun 4.

Department of Epigenetics and Molecular Carcinogenesis, Center for Cancer Epigenetics, The University of Texas MD Anderson UT Health Graduate School of Biomedical Sciences, The University of Texas MD Anderson Cancer Center , Houston, TX, USA.

Transcription factor p53 is activated in response to numerous stress stimuli in order to promote repair and survival or death of abnormal cells. For decades, regulatory mechanisms and downstream targets that execute the many biological functions of tumour suppressor p53 largely focused on the products of protein-coding genes. Recently, an entirely new class of molecules, termed long non-coding RNAs (lncRNAs), were discovered as key regulatory players in shaping p53 activity and biological outcomes. Read More

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http://dx.doi.org/10.1080/15476286.2020.1770981DOI Listing

Protein-Templated Hit Identification via an Ugi Four-Component Reaction.

Chemistry 2020 May 19. Epub 2020 May 19.

Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Drug Design and Optimization, Campus E8.1, 66123, Saarbrücken, GERMANY.

Kinetic target-guided synthesis represents an efficient hit-identification strategy, in which the protein assembles its own inhibitors from a pool of complementary building blocks via an irreversible reaction. Herein, we pioneered an in situ Ugi reaction for the identification of novel inhibitors of a model enzyme and binders for an important drug target, namely, the aspartic protease endothiapepsin and the bacterial β-sliding clamp DnaN, respectively. Highly sensitive mass-spectrometry methods enabled monitoring of the protein-templated reaction of four complementary reaction partners, which occurred in a background-free manner for endothiapepsin or with a clear amplification of two binders in the presence of DnaN. Read More

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http://dx.doi.org/10.1002/chem.202002250DOI Listing

Relationship between tRNA-derived fragments and human cancers.

Int J Cancer 2020 May 19. Epub 2020 May 19.

Department of Oncology, First Affiliated Hospital of Nanjing Medical University, Nanjing, China.

tRNA-derived fragments, a class of small noncoding RNAs (sncRNAs), have been identified in numerous studies in recent years. tRNA-derived fragments are classified into two main groups, including tRNA halves (tiRNAs) and tRNA-derived small RNA fragments (tRFs), according to different cleavage positions of the precursor or mature tRNAs. Instead of random tRNA degradation debris, a growing body of evidence has shown that tRNA-derived fragments are precise products of specific tRNA modifications and play important roles in biological activities, such as regulating protein translation, affecting gene expression, and altering immune signaling. Read More

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http://dx.doi.org/10.1002/ijc.33107DOI Listing

Biochemical evaluation and molecular docking assessment of the anti-inflammatory potential of leaf against ulcerative colitis.

Heliyon 2020 May 12;6(5):e03893. Epub 2020 May 12.

Department of Biochemistry, Faculty of Medical Sciences, University of Jos, Jos, Nigeria.

Ulcerative colitis (UC) is an inflammation of the colon that can progress to colorectal cancer if left untreated. No medication completely cures UC and natural products are sources of alternative approaches. This study aimed to determine the anti-inflammatory potential of leaf extract and fractions in a rat model of ulcerative colitis and to identify the active ingredients. Read More

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http://dx.doi.org/10.1016/j.heliyon.2020.e03893DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7226661PMC

The manzamine alkaloids.

Alkaloids Chem Biol 2020 23;84:1-124. Epub 2020 Apr 23.

Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan.

The manzamine alkaloids are absolutely one of the most fascinating marine natural products. The representative manzamine alkaloids, manzamines A-C, were isolated from a marine sponge Haliclona sp. collected off Cape Manzamo, Okinawa, Japan. Read More

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http://dx.doi.org/10.1016/bs.alkal.2020.03.001DOI Listing

The Effect of Subcutaneous Brodalumab upon Clinical Disease Activity in Hidradenitis Suppurativa: An Open Label Cohort Study.

J Am Acad Dermatol 2020 May 13. Epub 2020 May 13.

Laboratory of Investigative Dermatology, The Rockefeller University, New York. Electronic address:

Background: Hidradenitis Suppurativa is an autoinflammatory disorder of keratinization, with dysregulation of Th17 cytokines. Brodalumab is a monoclonal antibody which targets the IL-17RA receptor.

Objectives: To assess safety and tolerability and clinical response at Week 12 & 24 of Brodalumab in moderate-to-severe HS. Read More

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http://dx.doi.org/10.1016/j.jaad.2020.05.007DOI Listing

Promising Use Of The New Biologics In The Management Of Drug-Induced Hypersensitivity Reactions: Preliminary Approaches.

Endocr Metab Immune Disord Drug Targets 2020 May 15. Epub 2020 May 15.

Department of Internal Medicine and Clinical Oncology, University of Bari Medical School, Bari. Italy.

Biologics are an innovative class of drugs that can selectively influence immunological responses at a cellular level. Although their use is usually restricted to some specific diseases such as autoimmune pathologies and tumors, their "off-label" administration has increased widely in the last years. Drug treatment may induce hypersensitivity reactions which currently lack any gold standard therapy but may be a future field of application for biologics. Read More

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http://dx.doi.org/10.2174/1871530320666200515113736DOI Listing

Novel malaria antigen Plasmodium yoelii E140 induces antibody-mediated sterile protection in mice against malaria challenge.

PLoS One 2020 14;15(5):e0232234. Epub 2020 May 14.

Malaria Department, Naval Medical Research Center, Silver Spring, Maryland, United States of America.

Only a small fraction of the antigens expressed by malaria parasites have been evaluated as vaccine candidates. A successful malaria subunit vaccine will likely require multiple antigenic targets to achieve broad protection with high protective efficacy. Here we describe protective efficacy of a novel antigen, Plasmodium yoelii (Py) E140 (PyE140), evaluated against P. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0232234PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7224506PMC

Discovery of Targeted Covalent Natural Products against PLK1 by Herb-Based Screening.

J Chem Inf Model 2020 May 28. Epub 2020 May 28.

BNLMS, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.

Natural products (NPs) are a rich source of drug discovery, and some of them act by covalently binding to the targets. Recently, targeted covalent natural product (TCNP) design has gained considerable attention since this approach offers significant benefits in improving biological efficacy and decreasing the off-target side effects. However, most of the known TCNPs were discovered by chance. Read More

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http://dx.doi.org/10.1021/acs.jcim.0c00074DOI Listing

Overview of the anticancer activity of withaferin A, an active constituent of the Indian ginseng Withania somnifera.

Environ Sci Pollut Res Int 2020 May 13. Epub 2020 May 13.

Department of Pharmacy, Faculty of Medicine and Pharmacy,, University of Oradea, 410028, Oradea, Romania.

Cancer is still considered a "hopeless case", besides all of the advancements in oncology research. On the other hand, the natural products, as effective lead molecules, have gained significant interest for research due to the absence of toxic and harmful side effects usually associated with conventional treatment methods. Medicinal properties of herbal plants are strongly evidenced in traditional medicine from ancient times. Read More

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http://dx.doi.org/10.1007/s11356-020-09028-0DOI Listing

Detection of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Is Comparable in Clinical Samples Preserved in Saline or Viral Transport Medium.

J Mol Diagn 2020 May 13. Epub 2020 May 13.

Department of Medicine, Rutgers Robert Wood Johnson Medical School, New Brunswick, New Jersey; Center for Advanced Biotechnology and Medicine, Rutgers University, Piscataway, New Jersey. Electronic address:

As the coronavirus disease 2019 (COVID-19) pandemic sweeps across the world, the availability of viral transport medium (VTM) has become severely limited, contributing to delays in diagnosis and rationing of diagnostic testing. Given that severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral RNA has demonstrated stability, we posited that phosphate-buffered saline (PBS) may be a viable transport medium, as an alternative to VTM, for clinical real-time quantitative PCR (qPCR) testing. The intra-individual reliability and interindividual reliability of SARS-CoV-2 qPCR were assessed in clinical endotracheal secretion samples transported in VTM or PBS to evaluate the stability of the qPCR signal for three viral targets (N gene, ORF1ab, and S gene) when samples were stored in these media at room temperature for up to 18 hours. Read More

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http://dx.doi.org/10.1016/j.jmoldx.2020.04.209DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7219422PMC

The potential role of lncRNAs in diabetes and diabetic microvascular complications.

Endocr J 2020 May 12. Epub 2020 May 12.

Department of Endocrinology, The Second Hospital of Hebei Medical University, Shijiazhuang, Hebei, 050000, PR China.

Long noncoding RNAs (lncRNAs) are a group of noncoding RNAs that are longer than 200 nucleotides without protein-coding potential. Becasuse of which these RNAs have no significant protein-coding potential, they were initially considered as "junk-products" of transcription without biological meaning. Nevertheless, recent research advancements have shown that lncRNAs are involved in many physiological processes such as cell cycle regulation, cell apoptosis and survival, cancer migration and metabolism. Read More

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http://dx.doi.org/10.1507/endocrj.EJ19-0574DOI Listing

identification of vaccine targets for 2019-nCoV.

F1000Res 2020 25;9:145. Epub 2020 Feb 25.

MRC Human Immunology Unit, Medical Research Council (MRC) Human Immunology Unit, MRC Weatherall Institute of Molecular Medicine (WIMM), John Radcliffe Hospital, University of Oxford, Oxford, UK, Oxford, UK.

The newly identified coronavirus known as 2019-nCoV has posed a serious global health threat. According to the latest report (18-February-2020), it has infected more than 72,000 people globally and led to deaths of more than 1,016 people in China. The 2019 novel coronavirus proteome was aligned to a curated database of viral immunogenic peptides. Read More

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http://dx.doi.org/10.12688/f1000research.22507.2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7111504.2PMC

Mabs for treating asthma: omalizumab, mepolizumab, reslizumab, benralizumab, dupilumab.

Hum Vaccin Immunother 2020 May 13:1-8. Epub 2020 May 13.

Cardiac/Pulmonary Rehabilitation, ASST Pini-CTO, Milan, Italy.

The introduction of biologics for the treatment of patients with refractory asthma represented a marked therapeutic advance. For more than 10 y, the only biologic available has been the monoclonal anti-IgE antibody omalizumab, reserved for patients with asthma caused by perennial allergen. In recent years, other biologics have been licensed for the treatment of severe eosinophilic asthma. Read More

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http://dx.doi.org/10.1080/21645515.2020.1753440DOI Listing
May 2020
2.131 Impact Factor

Isolation of Secreted and Tegumental Surface Proteins from Fasciola hepatica.

Methods Mol Biol 2020 ;2137:27-36

Institute for Global Food Security, School of Biological Sciences, Queen's University Belfast, Belfast, UK.

Proteins secreted by, or displayed on the surface tegument of, trematodes have key functions in the host-parasite interaction. As such, they are often leading targets for diagnostic tests or vaccine candidates. Here we describe methods for the isolation and analysis of soluble secreted proteins (i. Read More

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http://dx.doi.org/10.1007/978-1-0716-0475-5_3DOI Listing
January 2020

Promises and challenges of biologics for severe asthma.

Biochem Pharmacol 2020 May 8:114012. Epub 2020 May 8.

Department of Pharmacology, Yong Loo Lin School of Medicine, National University Health System, 117600, Singapore; Immunology Program, Life Science Institute, National University of Singapore, 117456, Singapore; Singapore-HUJ Alliance for Research and Enterprise, National University of Singapore, 138602, Singapore. Electronic address:

Patients with severe asthma that remain uncontrolled incur significant medical burden and healthcare costs. Severe asthma is a heterogeneous airway disorder with complex pathophysiological mechanisms which can be broadly divided into type 2 (T2)-high and T2-low inflammatory pathways. Recent advances in asthma therapeutics with the advent of biologics have heralded an era of promising targeted therapy in this group of patients. Read More

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http://dx.doi.org/10.1016/j.bcp.2020.114012DOI Listing
May 2020
5.009 Impact Factor

A capillary electrophoresis based approach for the identification of anti-drug antibodies against camelid VHH biologics (Nanobodies®).

J Pharmacol Toxicol Methods 2020 May - Jun;103:106872. Epub 2020 May 7.

PPDM ADME Biologics, Merck & Co., Inc., 213 E. Grand Avenue, South San Francisco, CA 94080, USA. Electronic address:

Undesired immune responses against protein therapeutics may adversely affect the pharmacokinetics, efficacy, and safety of the product. The presence of anti-drug-antibodies (ADA) has been the key determinant of immunogenic responses. Here we describe the use of a capillary electrophoresis platform for the identification of ADAs against several experimental camelid VHH biologics (Nanobodies®). Read More

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http://dx.doi.org/10.1016/j.vascn.2020.106872DOI Listing

A DNA-encoded library for the identification of natural product binders that modulate poly (ADP-ribose) polymerase 1, a validated anti-cancer target.

Biochem Biophys Res Commun 2020 May 4. Epub 2020 May 4.

Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 201210, Shanghai, China. Electronic address:

Natural products have been an invaluable source of drug discovery, but their targets remain largely unknown. Natural products enriched DNA-encoded chemical libraries (nDELs) empower the researchers to rapidly and economically screen numerous natural products against various protein targets, and therefore promote the elucidation of the molecular mechanisms. In this work, we used poly (ADP-ribose) polymerase 1 (PARP1), as an example to explore the usage of nDEL for the functional natural products selection. Read More

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http://dx.doi.org/10.1016/j.bbrc.2020.04.022DOI Listing
May 2020
2.297 Impact Factor

Discovery of 1,3-Disubstituted 2,5-Diketopiperazine Derivatives as Potent Class I HDACs Inhibitors.

Chem Pharm Bull (Tokyo) 2020 ;68(5):466-472

Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University.

Histone deacetylases (HDACs) as attractive targets in many diseases therapies has been studied extensively, and its application in cancer research is the most important. Here, we developed a series of derivatives containing natural 2,5-diketopiperazine (DKP) skeleton. Several compounds exhibited distinct HDAC1 inhibitory activities, in particular 2a (IC = 405 nM). Read More

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http://dx.doi.org/10.1248/cpb.c20-00056DOI Listing
January 2020

Identifying potential treatments of COVID-19 from Traditional Chinese Medicine (TCM) by using a data-driven approach.

J Ethnopharmacol 2020 Aug 4;258:112932. Epub 2020 May 4.

Shandong University of Traditional Chinese Medicine, Jinan, 250355, China; Marine Traditional Chinese Medicine Research Center, Qingdao Academy of Traditional Chinese Medicine, Shandong University of Traditional Chinese Medicine, Qingdao, 266114, China; Shandong Engineering and Technology Research Center of Traditional Chinese Medicine, Jinan, 250355, China. Electronic address:

Ethnopharmacological Relevance: Traditional Chinese Medicine (TCM) has been widely used as an approach worldwide. Chinese Medicines (CMs) had been used to treat and prevent viral infection pneumonia diseases for thousands of years and had accumulated a large number of clinical experiences and effective prescriptions.

Aim Of The Study: This research aimed to systematically excavate the classical prescriptions of Chinese Medicine (CM), which have been used to prevent and treat Pestilence (Wenbing, Wenyi, Shiyi or Yibing) for long history in China, to obtain the potential prescriptions and ingredients to alternatively treat COVID-19. Read More

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http://dx.doi.org/10.1016/j.jep.2020.112932DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7196535PMC
August 2020
2.998 Impact Factor

Trends using biological target-based assays for drug detection in complex sample matrices.

Anal Bioanal Chem 2020 May 6. Epub 2020 May 6.

Division of Toxicology, Office of Applied Research and Safety Assessment, Center for Food Safety and Applied Nutrition, U.S. Food and Drug Administration (FDA), 8301 Muirkirk Rd, Laurel, MD, 20708, USA.

In vivo, drug molecules interact with their biological targets (e.g., enzymes, receptors, ion channels, transporters), thereby eliciting therapeutic effects. Read More

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http://dx.doi.org/10.1007/s00216-020-02681-xDOI Listing

Structure-Activity Analysis and Molecular Docking Studies of Coumarins from as Multifunctional Agents for Alzheimer's Disease.

Biomedicines 2020 May 2;8(5). Epub 2020 May 2.

Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.

Coumarins, naturally occurring phytochemicals, display a wide spectrum of biological activities by acting on multiple targets. Herein, nine coumarins from the root of were evaluated for activities related to pathogenesis of Alzheimer's disease (AD). They were examined for acetylcholinesterase (AChE) and AChE- or self-induced amyloid beta (Aβ) aggregation inhibitory activities, as well as neuroprotection against HO- and Aβ-induced human neuroblastoma SH-SY5Y cell damage. Read More

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http://dx.doi.org/10.3390/biomedicines8050107DOI Listing

Novel therapeutic approaches and targets for treatment of Suppurativa Hidradenitis.

Curr Pharm Biotechnol 2020 05 4. Epub 2020 May 4.

Department of Biomedical and Dental Sciences and Morphofunctional Images at the University of Messina. Italy.

Background: Hidradenitis suppurativa (HS) is a chronic, recurrent and disabling inflammatory skin condition, clinically characterized by nodules, bullae, abscesses, fistulae, and draining sinus tracts mainly located in axillae, inguinal folds, inframammary region and buttocks, often leading to pain, scarring, disfigurement and decreased quality of life. Due to its complex nature, with still no completely elucidated etiology and pathogenesis, the management of HS can be challenging. In fact, many patients do not respond to the traditionally available systemic treatments, including anti-inflammatories, antibiotics and surgery. Read More

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http://dx.doi.org/10.2174/1389201021666200505100556DOI Listing

Benzoxazine Dimer Analogue Targets Integrin β3 in Lung Cancer Cells and Suppresses Anoikis Resistance and Migration.

Anticancer Res 2020 May;40(5):2583-2589

Department of Pharmacology and Physiology, and Cell-based Drug and Health Products Development Research Unit, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok, Thailand

Background/aim: Certain integrins including integrin β3 facilitate movement and survival of metastatic cancer cells. We examined whether benzoxazine dimer analogue N,N-bis(5-ethyl-2-hydroxybenzyl) methylamine (HM) has anti-metastatic effects.

Materials And Methods: Cell viability was examined by the 3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide (MTT) assay. Read More

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http://dx.doi.org/10.21873/anticanres.14229DOI Listing

Lead Anti-obesity Compounds from Nature.

Endocr Metab Immune Disord Drug Targets 2020 May 3. Epub 2020 May 3.

Pharmacognosy Department, University of Rhode Island, Kingston, Rhode Island. United States.

Background - Obesity has become a global disease, leading to the enhanced risk of metabolic syndrome which includes diabetes, cardiovascular disease, stroke, hypertension and certain cancers but it is difficult to control only by diet and exercise as they are difficult to implement. Objective- The objective of this review is to bring into light the active constituents that can be obtained from various natural sources which act as anti-obesity agents because with a global rise in the prevalence of obesity, an urgent need to prevent and control it has arisen. Method- For this review, we have compiled information about natural anti-obesity products, by an electronic search of the articles available on PubMed, Scopus and other internet sources for the duration of1975-2019and added my own research too. Read More

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http://dx.doi.org/10.2174/1871530320666200504092012DOI Listing

Discovery of new potential CDK2/VEGFR2 type II inhibitors by fragmentation and virtual screening of natural products.

J Biomol Struct Dyn 2020 May 13:1-15. Epub 2020 May 13.

Grupo de Diseño de Productos y Procesos (GDPP), Department of Chemical Engineering, Universidad de los Andes, Bogotá, Colombia.

Cyclin-Dependent Kinase 2 (CDK2) and Vascular Endothelial Growth Factor Receptor (VEGFR2) have largely been considered as attractive targets for developing anticancer agents. However, there is no dual inhibitor commercially available in the market that interacts simultaneously with the allosteric back pocket of these enzymes. We applied a combined computational strategy that started with the generation of two overlapping pharmacophore models of both kinases at 'inactive' conformation. Read More

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http://dx.doi.org/10.1080/07391102.2020.1763839DOI Listing

Molecular and Immunological Mechanisms Underlying the Various Pharmacological Properties of the Potent Bioflavonoid, Rutin.

Endocr Metab Immune Disord Drug Targets 2020 May 2. Epub 2020 May 2.

Department of Pharmaceutical Technology, School of Pharmacy, International Medical University (IMU), Bukit Jalil, Kuala Lumpur, 57000. Malaysia.

The application of medicinal plants has captured the interest of researchers in recent times due to their potent therapeutic properties and a better safety profile. The prominent role of herbal products in treating and preventing multiple diseases dates back to ancient history and most of the modern drugs today originated from its significant sources owing to their ability to control multiple targets via different signalling pathways. Among them, flavonoids consist of a large group of polyphenols, which are well known for their various therapeutic benefits. Read More

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http://dx.doi.org/10.2174/1871530320666200503053846DOI Listing

Breeding Crops for Enhanced Food Safety.

Front Plant Sci 2020 15;11:428. Epub 2020 Apr 15.

Plant Breeding Center, Department of Plant Sciences, University of California, Davis, Davis, CA, United States.

An increasing global population demands a continuous supply of nutritious and safe food. Edible products can be contaminated with biological (, bacteria, virus, protozoa), chemical (, heavy metals, mycotoxins), and physical hazards during production, storage, transport, processing, and/or meal preparation. The substantial impact of foodborne disease outbreaks on public health and the economy has led to multidisciplinary research aimed to understand the biology underlying the different contamination processes and how to mitigate food hazards. Read More

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http://dx.doi.org/10.3389/fpls.2020.00428DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7176021PMC

Novel biosensor platforms for the detection of coronavirus infection and SARS-CoV-2.

J Chin Med Assoc 2020 Apr 27. Epub 2020 Apr 27.

Microscopy Service Laboratory, Basic Research Division, Department of Medical Research, Taipei Veterans General Hospital, Taipei, Taiwan, ROC.

The recent outbreak of the SARS-CoV-2 pandemic has been causing respiratory diseases globally, damaging wide-ranges of social-economical activities. This virus is transmitted through personal contact and possibly also through ambient air. Effective biosensor platforms for the detection of this virus and the related host response are in urgent demand. Read More

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http://dx.doi.org/10.1097/JCMA.0000000000000337DOI Listing

Review of biologics in allergic contact dermatitis.

Contact Dermatitis 2020 Apr 29. Epub 2020 Apr 29.

Department of Dermatology, University Hospital Basel, Basel, Switzerland.

The resistant and recalcitrant nature of severe allergic contact dermatitis (ACD) makes its management challenging. With the advances in understanding of the cellular and molecular pathogenesis of ACD, newer therapeutic targets are becoming apparent. In particular, the use of biologics has gained momentum, given the specificity of their action. Read More

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http://dx.doi.org/10.1111/cod.13584DOI Listing

Exosomes in Inflammatory Bowel Disease: What We Learnt So Far?

Curr Drug Targets 2020 Apr 27. Epub 2020 Apr 27.

Department of Gastroenterology, Shanghai Tenth People's Hospital, Tongji University, Shanghai 200072. China.

Inflammatory bowel disease (IBD) is an immune-mediated chronic inflammatory disease. Although the uncertain etiology, there is marked dysbalanced of mucosal immune responses in part shaped with genetic susceptibility and intestinal microbial dysbiosis. To suppress inflammatory activity adequately and maintain it are the main goals for current therapies. Read More

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http://dx.doi.org/10.2174/1389450121666200428102330DOI Listing

Current Clinical Trials for Tinnitus: Drugs and Biologics.

Otolaryngol Clin North Am 2020 Apr 22. Epub 2020 Apr 22.

Department of Physiology and Pharmacology, KarolinskaInstitutet, Solnavägen 9, Stockholm, Sweden.

Despite recent, major steps forward in our understanding of tinnitus pathophysiology and improved research methodology, tinnitus remains a clear unmet clinical need. Here, the authors identify current active clinical and preclinical development programs of tinnitus drug candidates using publications, databases, and company communications. The current drug development programs hold promise for new therapeutic options for tinnitus patients, but further fundamental research is needed to validate additional targets for treating tinnitus. Read More

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http://dx.doi.org/10.1016/j.otc.2020.03.012DOI Listing

Synthesis, In Vitro Antitumor Activity and Molecular Mechanism of Novel Furan Derivatives and their Precursors.

Anticancer Agents Med Chem 2020 Apr 24. Epub 2020 Apr 24.

College of Pharmacy, Center for Lab Teaching and Management, Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, No.1 Yixueyuan Road, Chongqing 400016. China.

Background: Compounds featuring furan nucleus exhibit diverse biological properties. Lots of furan derivatives have been explored as pharmaceutical compounds. Hence it is of great interest to explore furan derivatives and their precursors as antitumor agents. Read More

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http://dx.doi.org/10.2174/1871520620666200424130204DOI Listing