9,404 results match your criteria Biologics : targets & therapy[Journal]


Antibiotic discovery with synthetic fermentation: library assembly, phenotypic screening, and mechanism of action of beta-peptides targeting penicillin-binding proteins.

ACS Chem Biol 2019 Apr 16. Epub 2019 Apr 16.

In analogy to biosynthetic pathways leading to bioactive natural products, synthetic fermentation generates mixtures of molecules from simple building blocks under aqueous, biocompatible conditions, allowing for the resulting cultures to be directly screened for biological activity. In this work, a novel beta-peptide antibiotic was successfully identified using the synthetic fermentation platform. Phenotypic screening was carried out in an initially random fashion, allowing for simple identification of active cultures. Read More

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http://pubs.acs.org/doi/10.1021/acschembio.9b00227
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http://dx.doi.org/10.1021/acschembio.9b00227DOI Listing
April 2019
4 Reads

Identification of atherosclerosis-related prioritizing metabolites based on a multi-omics composite network.

Exp Ther Med 2019 May 6;17(5):3391-3398. Epub 2019 Mar 6.

Department of Cardiology, Binzhou City Center Hospital, Binzhou, Shandong 251700, P.R. China.

Metabolites are the final products of cellular regulation processes, their level is the ultimate response of biological systems to environmental and genetic changes. Therefore, the identification of key metabolites is required for the diagnosis and therapy of diseases. In this study, atherosclerosis-related gene expression profile information was extracted from ArrayExpress database (GEOD-57691), and analyzed with limma package. Read More

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http://dx.doi.org/10.3892/etm.2019.7351DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6447794PMC

Strategies for the Development of Glycomimetic Drug Candidates.

Authors:
Rachel Hevey

Pharmaceuticals (Basel) 2019 Apr 11;12(2). Epub 2019 Apr 11.

Molecular Pharmacy, Dept. Pharmaceutical Sciences, University of Basel, Klingelbergstr. 50, 4056 Basel, Switzerland.

Carbohydrates are a structurally-diverse group of natural products which play an important role in numerous biological processes, including immune regulation, infection, and cancer metastasis. Many diseases have been correlated with changes in the composition of cell-surface glycans, highlighting their potential as a therapeutic target. Unfortunately, native carbohydrates suffer from inherently weak binding affinities and poor pharmacokinetic properties. Read More

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http://dx.doi.org/10.3390/ph12020055DOI Listing

Marine-Derived Natural Compounds for the Treatment of Parkinson's Disease.

Mar Drugs 2019 Apr 11;17(4). Epub 2019 Apr 11.

Ningbo Key Laboratory of Behavioral Neuroscience, Zhejiang Provincial Key Laboratory of Pathophysiology, School of Medicine, Ningbo University, Ningbo 315211, China.

Parkinson's disease (PD) is a neurodegenerative disorder caused by the loss of dopaminergic neurons, leading to the motor dysfunctions of patients. Although the etiology of PD is still unclear, the death of dopaminergic neurons during PD progress was revealed to be associated with the abnormal aggregation of α-synuclein, the elevation of oxidative stress, the dysfunction of mitochondrial functions, and the increase of neuroinflammation. However, current anti-PD therapies could only produce symptom-relieving effects, because they could not provide neuroprotective effects, stop or delay the degeneration of dopaminergic neurons. Read More

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http://dx.doi.org/10.3390/md17040221DOI Listing
April 2019
2 Reads

Drug survival of biological therapy is showing class effect: updated results from Slovenian National Registry of psoriasis.

Int J Dermatol 2019 Apr 11. Epub 2019 Apr 11.

Department of Dermatovenereology, University Medical Centre Maribor, Maribor, Slovenia.

Background: Drug survival is an important measure of successful treatment of patients with chronic diseases such as psoriasis. Therefore, the objective was to calculate drug survival and examine safety profile of biologics and immunomodulators (adalimumab, apremilast, etanercept, ixekizumab, infliximab, secukinumab, and ustekinumab) from the Slovenian National Registry of patients with moderate-to-severe psoriasis.

Methods: Data about the patients with moderate-to-severe plaque psoriasis treated with biologics were collected from 2005 until July 2018. Read More

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http://dx.doi.org/10.1111/ijd.14429DOI Listing

The natural product elegaphenone potentiates antibiotic effects against Pseudomonas aeruginosa.

Angew Chem Int Ed Engl 2019 Apr 10. Epub 2019 Apr 10.

Technische Universitat Munchen, Department of Chemistry, Lichtenbergstr. 4, 85747, Garching, GERMANY.

Natural products represent a rich source for antibiotics addressing versatile cellular targets. The deconvolution of their targets via chemical proteomics is often challenged by the introduction of large photocrosslinkers. Here we select elegaphenone, a largely uncharacterized natural product antibiotic bearing a native benzophenone core scaffold, for affinity-based protein profiling (AfBPP) in Gram-positive and Gram-negative bacteria. Read More

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http://doi.wiley.com/10.1002/anie.201903472
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http://dx.doi.org/10.1002/anie.201903472DOI Listing
April 2019
2 Reads

Target Prioritization of Novel Substituted 5-aryl-2-oxo-/thioxo-2,3-dihydro-1H-benzo[6,7]chromeno[2,3-d]pyrimidine-4,6,11(5H)-triones As Anti-cancer Agents Using In-silico Approach.

J Biomol Struct Dyn 2019 Apr 10:1-15. Epub 2019 Apr 10.

d Drug Theoretics and Cheminformatics Laboratory , Jadavpur University , Kolkata 700032 , India.

Cancer is a multi-origin collection of diseases attributed by abnormal and uncontrolled cell growth spread from origin to other parts of body eventually leading to death. After decades of research, anti-cancer drug therapy is still very much limited to inhibiting growth and controlling spared of tumor cells. Finding novel molecular targets and drug candidates using assimilation of experimental and computational approaches is among the recent strategies adopted by researchers to speed up the anti-cancer drug discovery process. Read More

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http://dx.doi.org/10.1080/07391102.2019.1606735DOI Listing
April 2019
1 Read

CCAAT-displacement protein/cut homeobox transcription factor (CUX1) represses estrogen receptor-alpha (ER-α) in triple-negative breast cancer cells and can be antagonized by muscadine grape skin extract (MSKE).

PLoS One 2019 9;14(4):e0214844. Epub 2019 Apr 9.

Center for Cancer Research and Therapeutic Development, Department of Biological Sciences, Clark Atlanta University, Atlanta, Georgia, United States of America.

Triple-Negative Breast Cancers (TNBCs) are the most difficult to treat subtype of breast cancer and are often associated with high nuclear expression of Snail and Cathepsin L (Cat L) protease. We have previously shown that Snail can increase Cat L expression/activity in prostate and breast cancer cells. This study investigated the role of CUX1 (a downstream substrate of Cat L) in TNBC. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0214844PLOS
April 2019
2 Reads

A Robust Strategy for Sustainable Organic Chemicals Utilizing Bioprivileged Molecules.

ChemSusChem 2019 Apr 9. Epub 2019 Apr 9.

Center for Biorenewable Chemicals (CBiRC), Iowa State University, Ames, Iowa, 50011, USA.

Biobased chemicals will inevitably be an important part of a sustainable organic chemical industry. Current efforts in biobased chemicals are largely driven by opportunistic chemical product targets requiring complete technology development from feedstock to final product for a specific molecule. To enhance the development of biobased chemicals, it is important to create strategies that can be more systematic and can leverage advancements across multiple final products. Read More

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http://dx.doi.org/10.1002/cssc.201900323DOI Listing

Systemic rheumatic diseases: From biological agents to small molecules.

Autoimmun Rev 2019 Apr 5. Epub 2019 Apr 5.

Rheumatology Unit, University of Messina, Messina, Italy.

The development of biologics and small oral molecules has recently changed the scenario of pharmacologic treatment of systemic rheumatic diseases and it has become a real revolution. These drugs have innovative mechanisms of action, based on the inhibition of specific molecular or cellular targets directly involved in disease pathogenesis. This new scenario has lead to a regular update of the management recommendations of several institututions, such as those for Rheumatoid Arthritis treatment that address the use of conventional and biologic therapies including TNFin (adalimumab, certolizumab pegol, etanercept, golimumab, infliximab), abatacept, rituximab, IL-6 inhibitors (tocilizumab and sarilumab), biosimilars and small oral molecules (the JAK inhibitors tofacitinib and baricitinib). Read More

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https://linkinghub.elsevier.com/retrieve/pii/S15689972193008
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http://dx.doi.org/10.1016/j.autrev.2018.12.009DOI Listing
April 2019
3 Reads

[Modeling and theoretical analysis of ring specific mimicry in view of isomerism within medicinal promising oligomers of "DIVEMA"].

Biomed Khim 2019 Feb;65(2):133-151

Topchiev Institute of Petrochemical Synthesis, RAS, Moscow, Russia; Research Center for Biomodulators, Health Research and Development Foundation, Moscow, Russia.

The furan or pyran related hetero cycles play basic role in structural units of nucleic acids (NA) and polysaccharides (PS), significantly predetermining their functional specifics. Some of such properties, in great relevancy for medicine, can be imitated through mimicry of polymers synthetic. Particularly, a formation of similar cycloisomeric chains is possible in process of free-radical cyclocopolymerization of divinyl ether (DVE) and maleic anhydride (MA). Read More

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http://dx.doi.org/10.18097/PBMC20196502133DOI Listing
February 2019
1 Read

Anti-TNF and postoperative complications in abdominal Crohn's disease surgery.

Curr Drug Targets 2019 Apr 4. Epub 2019 Apr 4.

IBD Center, Department of Gastroenterology, Humanitas Clinical and Research Centre, Rozzano, Milan. Italy.

Background: Biological therapy with anti-tumour necrosis factor (TNF)-α agents revolutionised the treatment of inflammatory bowel disease over the last decades. However, there may be an increased risk of postoperative complications in Crohn's disease (CD) patients treated with anti-TNF-α agents prior to abdominal surgery.

Objective: To evaluate the effects of preoperative anti-TNF-α therapy on the incidence of complications after surgery. Read More

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http://dx.doi.org/10.2174/1389450120666190404144048DOI Listing
April 2019
1 Read

Comprehensive Structure-Activity Relationship Studies of Macrocyclic Natural Products Enabled by Their Total Syntheses.

Chem Rev 2019 Apr 4. Epub 2019 Apr 4.

Graduate School of Pharmaceutical Sciences , The University of Tokyo , 7-3-1 Hongo , Bunkyo-ku, Tokyo 113-0033 , Japan.

Macrocyclic natural products have been recognized and utilized as new platforms for designing drugs in pharmaceutical research because the constrained three-dimensional shapes and the large surface areas of these complex structures enable selective binding to conventionally undruggable targets. Since natural products are not necessarily ideal for medicinal use, structural optimization is required to obtain superior drug candidates. However, the modifications to macrocyclic natural products that will afford the best pharmacological characteristics cannot be known a priori. Read More

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http://pubs.acs.org/doi/10.1021/acs.chemrev.9b00063
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http://dx.doi.org/10.1021/acs.chemrev.9b00063DOI Listing
April 2019
1 Read

Wolfberry-Derived Zeaxanthin Dipalmitate Attenuates Ethanol-Induced Hepatic Damage.

Mol Nutr Food Res 2019 Apr 1:e1801339. Epub 2019 Apr 1.

Clinical Medicine Research Institute, The First Affiliated Hospital of Jinan University, Guangzhou, China.

Scope: Besides abstinence and nutritional support, there is no proven clinical treatment for patients with alcoholic fatty liver disease (AFLD). Here, the therapeutic effects and mechanisms of action of wolfberry-derived zeaxanthin dipalmitate (ZD) on AFLD models are demonstrated.

Methods And Results: The hepatoprotective effects of ZD are evaluated in vitro and in vivo. Read More

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http://dx.doi.org/10.1002/mnfr.201801339DOI Listing
April 2019
8 Reads
4.603 Impact Factor

A Strategy toward Icetexane Natural Products.

European J Org Chem 2018 Jul 16;2018(25):3348-3351. Epub 2018 May 16.

Department of Chemistry & Biochemistry, University of Delaware, Newark, DE 19176, United States.

Icetexane diterpenoids are richly complex polycyclic natural products that have been described with a variety of biological activities. We report here a general synthetic approach toward the 6-7-6 tricyclic core structure of these interesting synthetic targets based on a two-step enolate alkylation and ring-closing metathesis reaction sequence. Read More

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http://dx.doi.org/10.1002/ejoc.201800707DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6433415PMC

Anti-TNF and pouch surgery for ulcerative colitis: the ones who blame for more complications?

Curr Drug Targets 2019 Mar 28. Epub 2019 Mar 28.

Department of Abdominal Surgery, University Hospitals Leuven, KU Leuven, Leuven. Belgium.

Since the approval in 2005 of anti-TNF drugs for the treatment of ulcerative colitis, concerns have been raised about the potential detrimental effect of these agents on postoperative infectious complications related to pouch surgery. Data on this topic are controversial and mostly derived from retrospective underpowered cohort studies largely affected by relevant bias. Three meta-analyses have been published with contradictory results. Read More

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http://dx.doi.org/10.2174/1389450120666190328153200DOI Listing

Globally important islands where eradicating invasive mammals will benefit highly threatened vertebrates.

PLoS One 2019 27;14(3):e0212128. Epub 2019 Mar 27.

BirdLife International, Cambridge, United Kigndom.

Invasive alien species are a major threat to native insular species. Eradicating invasive mammals from islands is a feasible and proven approach to prevent biodiversity loss. We developed a conceptual framework to identify globally important islands for invasive mammal eradications to prevent imminent extinctions of highly threatened species using biogeographic and technical factors, plus a novel approach to consider socio-political feasibility. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0212128PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6436766PMC

Prediction of potential cancer-related molecular targets of North African plants constituents using network pharmacology-based analysis.

Authors:
Eman Shawky

J Ethnopharmacol 2019 Mar 22:111826. Epub 2019 Mar 22.

Department of Pharmacognosy, Faculty of Pharmacy, Alexandria University, Alexandria, 21521, Egypt. Electronic address:

Ethnopharmacological Relevance: Nowadays, cancer is considered one of the leading causes of death in developing countries. Due to mediocre socioeconomic status of many of the North African countries, people resort to traditional medicine from natural products for cancer therapy which are of great chemical complexity, interacting with several protein targets leading to synergistic effects. A holistic network pharmacology approach is needed for understanding the molecular mechanism of North African plants constituents in the different cancer-related pathways. Read More

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http://dx.doi.org/10.1016/j.jep.2019.111826DOI Listing
March 2019
1 Read

Distinct Fractions of an Extract Contain Compounds With Novel Adipogenic Bioactivity.

Front Nutr 2019 8;6:18. Epub 2019 Mar 8.

Pennington Biomedical Research Center, Baton Rouge, LA, United States.

Adipocytes are important players in metabolic health and disease, and disruption of adipocyte development or function contributes to metabolic dysregulation. Hence, adipocytes are significant targets for therapeutic intervention in obesity and metabolic syndrome. Plants have long been sources for bioactive compounds and drugs. Read More

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https://www.frontiersin.org/article/10.3389/fnut.2019.00018/
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http://dx.doi.org/10.3389/fnut.2019.00018DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6418310PMC
March 2019
3 Reads

The endothelial tip-stalk cell selection and shuffling during angiogenesis.

J Cell Commun Signal 2019 Mar 22. Epub 2019 Mar 22.

The Key Laboratory of Pathobiology, Ministry of Education, College of Basic Medical Sciences, Jilin University, Changchun, China.

Angiogenesis is a critical, fine-tuned, multi-staged biological process. Tip-stalk cell selection and shuffling are the building blocks of sprouting angiogenesis. Accumulated evidences show that tip-stalk cell selection and shuffling are regulated by a variety of physical, chemical and biological factors, especially the interaction among multiple genes, their products and environments. Read More

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http://dx.doi.org/10.1007/s12079-019-00511-zDOI Listing

Redox lipidomics to better understand brain aging and function.

Free Radic Biol Med 2019 Mar 18. Epub 2019 Mar 18.

Freshage Research Group-Department of Physiology, Faculty of Medicine, University of Valencia, CIBERFES, INCLIVA, Spain.

Human prefrontal cortex (PFC) is a recently evolutionary emerged brain region involved in cognitive functions. Human cognitive abilities decline during aging. Yet the molecular mechanisms that sustain the preservation or deterioration of neurons and PFC functions are unknown. Read More

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http://dx.doi.org/10.1016/j.freeradbiomed.2019.03.016DOI Listing
March 2019
1 Read

Biological mechanisms and related natural modulators of liver X receptor in nonalcoholic fatty liver disease.

Biomed Pharmacother 2019 May 18;113:108778. Epub 2019 Mar 18.

Key Laboratory of Liver and Kidney Diseases (Ministry of Education), Institute of Liver Diseases, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Shanghai Key laboratory of Traditional Chinese Medicine, Shanghai 201203, China. Electronic address:

Nonalcoholic fatty liver disease (NAFLD) is becoming a worldwide health problem, but no approved medical treatment exists so far. Nuclear receptors are one of the drug targets for nonalcoholic steatohepatitis (NASH). Among them, liver X receptor (LXR) has been studied in recent years in tumors, metabolic diseases and inflammatory diseases, but its physiological and pharmacological effects in the treatment of NASH are controversial. Read More

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http://dx.doi.org/10.1016/j.biopha.2019.108778DOI Listing
May 2019
2 Reads
2.023 Impact Factor

Optimal Biologic Selection for Treatment of Psoriatic Arthritis: the Approach to Precision Medicine.

Curr Rheumatol Rep 2019 Mar 20;21(5):21. Epub 2019 Mar 20.

The First Department of Internal Medicine, University of Occupational and Environmental Health, Japan, 1-1 Iseigaoka, Yahata-nishi, Kitakyushu, 807-8555, Japan.

Purpose Of Review: This review describes previously reported findings on optimal biologic agent selection for psoriatic arthritis (PsA) treatment and outlines our approach to developing precision medicine techniques for targeted treatment of this disease.

Recent Findings: Clinical trials have reported the effectiveness of numerous biologics with different targets, such as tumor necrosis factor-α, interleukin (IL)-17A, IL-17 receptor, IL-12/23(p40), and IL-23(p19) for the treatment of PsA. Although several studies have suggested specific predictors of treatment responses to each biologic, how biologics are differentially chosen in each patient remains unclear. Read More

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http://dx.doi.org/10.1007/s11926-019-0817-xDOI Listing
March 2019
1 Read

[Mechanism of Ⅲ in the treatment of proteinuria in chronic kidney disease: a network pharmacology-based study].

Nan Fang Yi Ke Da Xue Xue Bao 2019 02;39(2):227-234

School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China.

Objective: To identify the main active components in Ⅲ and their targets and explore the mechanism by which Ⅲ alleviates proteinuria in chronic kidney disease (CKD) based on network pharmacology.

Methods: The active components of Ⅲ and their potential targets, along with the oral bioavailability and drug-like properties of each component were searched in the TCMSP database. The proteinuria-related targets were searched in the GeneCards database. Read More

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http://dx.doi.org/10.12122/j.issn.1673-4254.2019.02.16DOI Listing
February 2019
1 Read

Early arthritis clinic is cost-effective, improves outcomes and reduces biologic use.

Authors:
M K Nisar

Clin Rheumatol 2019 Mar 19. Epub 2019 Mar 19.

Rheumatology Department, Luton & Dunstable University Hospital NHSFT, Lewsey Road, Luton, LU4 0DZ, UK.

There is good evidence that dedicated early arthritis clinics (EACs) improve referral lag time and reduce delay in establishing disease-modifying therapy. However, it remains arguable whether such clinics improve relevant disease outcomes. Nationally, only 57% of units have dedicated EACs. Read More

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http://dx.doi.org/10.1007/s10067-019-04515-3DOI Listing

In Vitro Tumor Cell Rechallenge For Predictive Evaluation of Chimeric Antigen Receptor T Cell Antitumor Function.

J Vis Exp 2019 Feb 27(144). Epub 2019 Feb 27.

Department of Hematology & Hematopoietic Cell Transplantation, T Cell Therapeutics Research Laboratory, City of Hope Beckman Research Institute and Medical Center;

The field of chimeric antigen receptor (CAR) T cell therapy is rapidly advancing with improvements in CAR design, gene-engineering approaches and manufacturing optimizations. One challenge for these development efforts, however, has been the establishment of in vitro assays that can robustly inform selection of the optimal CAR T cell products for in vivo therapeutic success. Standard in vitro tumor-lysis assays often fail to reflect the true antitumor potential of the CAR T cells due to the relatively short co-culture time and high T cell to tumor ratio. Read More

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http://dx.doi.org/10.3791/59275DOI Listing
February 2019

Predicting and preventing complications in children with inflammatory bowel disease.

Authors:
Zubin Grover

Transl Pediatr 2019 Jan;8(1):70-76

Department of Gastroenterology, Perth Children's Hospital, Perth, Australia.

Paediatric-onset inflammatory bowel disease (IBD) is associated with greater disease burden and morbidity compared to adult-onset IBD. Accurate risk prediction for a complicated disease course in childhood onset IBD is essential for making the best treatment choices. Complicating course in IBD is closely linked with choice of therapies and treatment targets. Read More

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http://dx.doi.org/10.21037/tp.2019.01.03DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6382500PMC
January 2019
2 Reads

Exosomes in gastric cancer: roles, mechanisms, and applications.

Mol Cancer 2019 03 15;18(1):41. Epub 2019 Mar 15.

Institute of Digestive Diseases, The Affiliated People's Hospital of Jiangsu University, Zhenjiang, 212002, Jiangsu, China.

Exosomes are nanosized extracellular vesicles that can be released by almost all types of cells. Initially considered as the garbage bins acting to discard unwanted products of cells, exosomes are now recognized as an important way for cellular communication by transmitting bioactive molecules including proteins, DNA, mRNAs, and non-coding RNAs. The recent studies have shown that exosomes are critically involved in human health and diseases including cancer. Read More

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http://dx.doi.org/10.1186/s12943-019-1001-7DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6419325PMC

Systematic analysis of Type I-E Escherichia coli CRISPR-Cas PAM sequences ability to promote interference and primed adaptation.

Mol Microbiol 2019 Mar 15. Epub 2019 Mar 15.

Center of Life Sciences, Skolkovo Institute of Science and Technology, Moscow, 121205, Russia.

CRISPR interference occurs when a protospacer recognized by the CRISPR RNA is destroyed by Cas effectors. In Type I CRISPR-Cas systems, protospacer recognition can lead to «primed adaptation» - acquisition of new spacers from in cis located sequences. Type I CRISPR-Cas systems require the presence of a trinucleotide protospacer adjacent motif (PAM) for efficient interference. Read More

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http://dx.doi.org/10.1111/mmi.14237DOI Listing
March 2019
1 Read

Cross-linking structure-induced strong blue emissive gold nanoclusters for intracellular sensing.

Analyst 2019 Apr;144(8):2765-2772

School of Food and Biological Engineering, Engineering Research Center of Bio-process, Ministry of Education, Hefei University of Technology, Hefei, China.

Fluorescent gold nanoclusters (Au NCs) are new emerging fluorescent nanomaterials with broad application prospects but limited by the complicated preparation, low quantum yield (QY) and poor biological applications. Here we develop a one pot etching approach for synthesizing fluorescent Au NCs by using the common citrate-capped gold nanoparticles (Au NPs) as the precursor and the poly(amidoamine) (PAMAM) dendrimer as the etching and templating agent. The synthesis conditions are optimized and products are characterized in detail. Read More

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http://dx.doi.org/10.1039/c9an00132hDOI Listing

Stapled Peptides Inhibitors: A New Window for Target Drug Discovery.

Comput Struct Biotechnol J 2019 19;17:263-281. Epub 2019 Feb 19.

Department of Drug Design, University of Groningen, Antonius Deusinglaan1, 9700AD Groningen, the Netherlands.

Protein-protein interaction (PPI) is a hot topic in clinical research as protein networking has a major impact in human disease. Such PPIs are potential drugs targets, leading to the need to inhibit/block specific PPIs. While small molecule inhibitors have had some success and reached clinical trials, they have generally failed to address the flat and large nature of PPI surfaces. Read More

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http://dx.doi.org/10.1016/j.csbj.2019.01.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6396041PMC
February 2019

Endothelins in cardiovascular biology and therapeutics.

Nat Rev Cardiol 2019 Mar 13. Epub 2019 Mar 13.

University of Edinburgh/British Heart Foundation Centre of Research Excellence, Centre for Cardiovascular Science, Queen's Medical Research Institute, Edinburgh, UK.

Cardiovascular disease is a major contributor to global morbidity and mortality and is the common end point of many chronic diseases. The endothelins comprise three structurally similar peptides of 21 amino acids in length. Endothelin 1 (ET-1) and ET-2 activate two G protein-coupled receptors - endothelin receptor type A (ET) and endothelin receptor type B (ET) - with equal affinity, whereas ET-3 has a lower affinity for ET. Read More

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http://www.nature.com/articles/s41569-019-0176-3
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http://dx.doi.org/10.1038/s41569-019-0176-3DOI Listing
March 2019
3 Reads

Inflammatory bowel disease therapies adversely affect fertility in men- A systematic review and meta-analysis.

Endocr Metab Immune Disord Drug Targets 2019 Mar 12. Epub 2019 Mar 12.

Department of Surgery, Oncology and Gastroenterology, Gastroenterology/Multivisceral Transplant Unit, University Hospital Padova. Italy.

Background And Aims: Sexual functions are sometimes adversely affected by the therapeutic drugs delivered for treating IBD. Much attention has been focused on pregnancy/sexual issues in women. Relatively less attention has been poured in to address this issue in men. Read More

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http://dx.doi.org/10.2174/1871530319666190313112110DOI Listing
March 2019
3 Reads

Circular RNAs in Cancer.

Mol Ther Nucleic Acids 2019 Feb 16;16:118-129. Epub 2019 Feb 16.

Department of Gynecologic Oncology and Reproductive Medicine, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA; Department of Cancer Biology, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA; Center for RNA Interference and Non-Coding RNA, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA. Electronic address:

Circular RNAs (circRNAs) are a class of single-stranded closed RNA molecules that are formed by precursor mRNA back-splicing or skipping events of thousands of genes in eukaryotes as covalently closed continuous loops. High-throughput sequencing and bioinformatics approaches have uncovered the broad expression of circRNAs across species. Their high stability, abundance, and evolutionary conservation among species points to their distinct properties and diverse cellular functions as efficient microRNAs and protein sponges; they also play important roles in modulating transcription and splicing. Read More

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http://dx.doi.org/10.1016/j.omtn.2019.02.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6411617PMC
February 2019
2 Reads

Synthesis, biological function and evaluation of Shikonin in cancer therapy.

Fitoterapia 2019 Mar 8;134:329-339. Epub 2019 Mar 8.

Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, China; Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research, Jinan University, Guangzhou 510632, China. Electronic address:

Shikonin is a natural compound isolated from herbs and traditional medicines that have been used in a number of countries to treat various illnesses including inflammation, virus infection and cancer for centuries. Recent studies have shed light on the molecular mechanisms underlying these biological activities of Shikonin. Here we review the latest advances in our understanding of this compound class in the anti-cancer regimen. Read More

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http://dx.doi.org/10.1016/j.fitote.2019.03.005DOI Listing

Binding site comparisons for target-centered drug discovery.

Authors:
Janez Konc

Expert Opin Drug Discov 2019 May 11;14(5):445-454. Epub 2019 Mar 11.

a Theory Department , National Institute of Chemistry , Ljubljana , Slovenia.

Introduction: The success of binding site comparisons in drug discovery is based on the recognized fact that many different proteins have similar binding sites. Indeed, binding site comparisons have found many uses in drug development and have the potential to dramatically cut the cost and shorten the time necessary for the development of new drugs. Areas covered: The authors review recent methods for comparing protein binding sites and their use in drug repurposing and polypharmacology. Read More

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http://dx.doi.org/10.1080/17460441.2019.1588883DOI Listing

Topical, systemic and biologic therapies in hidradenitis suppurativa: pathogenic insights by examining therapeutic mechanisms.

Ther Adv Chronic Dis 2019 1;10:2040622319830646. Epub 2019 Mar 1.

Laboratory of Investigative Dermatology, The Rockefeller University, New York, NY, USA.

Hidradenitis suppurativa (HS) is a chronic inflammatory disease of the skin, manifesting in chronic, recurrent painful pustules, nodules, boils and purulent draining abscesses. Our current understanding of the pathogenesis of the disease is incomplete. This review aims to identify available treatment options in HS and discuss the pharmacological mechanisms through which such agents function. Read More

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http://dx.doi.org/10.1177/2040622319830646DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6399757PMC
March 2019
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Integrated Proteomics, Biological Functional Assessments, and Metabolomics Reveal Toosendanin-Induced Hepatic Energy Metabolic Disorders.

Chem Res Toxicol 2019 Apr 19;32(4):668-680. Epub 2019 Mar 19.

State Key Laboratory for Quality Research of Chinese Medicines , Macau University of Science and Technology , Avenida Wai Long , Taipa , Macao.

Toosendanin (TSN), a compound from Melia toosendan, exhibits severe hepatotoxicity, which restricts its clinical application. However, the mechanism is not clear. Our previous research found that covalent modification of TSN for proteins might be a possible reason using human liver microsomes, and the glycolytic enzymes, triosephosphate isomerase 1 (TPIS) and α-enolase (ENOA), were responsible for the hepatotoxicity. Read More

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http://pubs.acs.org/doi/10.1021/acs.chemrestox.8b00350
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http://dx.doi.org/10.1021/acs.chemrestox.8b00350DOI Listing
April 2019
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Novel Targets For Therapeutic Intervention in Inflammatory Bowel Disease What is the best way to assess the safety profile of a drug?

Curr Pharm Des 2019 Mar 7. Epub 2019 Mar 7.

Division of Gastroenterology, Icahn School of Medicine, Mount Sinai, New York, NY. France.

The emergence of biologic therapies has revolutionized the management of inflammatory bowel disease (IBD) by halting disease progression, increasing remission rates and improving long-term clinical outcomes. Despite these well-described benefits, many patients are reluctant to commence therapy due to drug safety concerns. Adverse events can be detected at each stage of drug development and during the post-marketing period. Read More

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http://dx.doi.org/10.2174/1381612825666190308102021DOI Listing
March 2019
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Advances in the Total Synthesis of Xanthanolide-Type Sesquiterpenoids.

Chem Asian J 2019 Mar 5. Epub 2019 Mar 5.

School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Tsinghua University, Beijing, 100084, China.

Xanthanolide-type sesquiterpenoids are a diverse family of natural products isolated primarily from the genus Xanthium (Compositae). The intriguing molecular architectures and biological profiles of these natural products have rendered them attractive targets for total synthesis. This focus review aims to provide an up-to-date summary of progress in the chemical synthesis of xanthanolide-type sesquiterpenoids. Read More

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http://dx.doi.org/10.1002/asia.201900040DOI Listing

Lipoxidation in cardiovascular diseases.

Redox Biol 2019 Feb 25:101119. Epub 2019 Feb 25.

Centro Cardiologico Monzino, IRCCS, Milano, Italy. Electronic address:

Lipids can go through lipid peroxidation, an endogenous chain reaction that consists in the oxidative degradation of lipids leading to the generation of a wide variety of highly reactive carbonyl species (RCS), such as short-chain carbonyl derivatives and oxidized truncated phospholipids. RCS exert a wide range of biological effects due to their ability to interact and covalently bind to nucleophilic groups on other macromolecules, such as nucleic acids, phospholipids, and proteins, forming reversible and/or irreversible modifications and generating the so-called advanced lipoxidation end-products (ALEs). Lipoxidation plays a relevant role in the onset of cardiovascular diseases (CVD), mainly in the atherosclerosis-based diseases in which oxidized lipids and their adducts have been extensively characterized and associated with several processes responsible for the onset and development of atherosclerosis, such as endothelial dysfunction and inflammation. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S22132317183088
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http://dx.doi.org/10.1016/j.redox.2019.101119DOI Listing
February 2019
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Biologics for chronic inflammatory skin diseases: an update for the clinician.

J Dermatolog Treat 2019 Mar 2:1-23. Epub 2019 Mar 2.

a Department of Dermato-Venereology and Wound Healing Centre , Bispebjerg Hospital , Copenhagen , Denmark.

The introduction and continuous development in biological drugs has greatly improved the therapeutic quality for patients with chronic inflammatory skin conditions. Current approaches to the biologic treatment of psoriasis, atopic dermatitis, chronic spontaneous urticaria, and hidradenitis suppurativa include licensed use of traditional antitumor necrosis factor agents, selective interleukin antagonists (IL-4, IL-12/23, IL-17), and the IgE inhibitor omalizumab, and as the knowledge on the pathogenesis of these diseases expands, off-label uses of the currently available biologics are becoming increasingly attractive, and the number of investigational drugs is growing progressively plentiful. In recent years, small molecule inhibitors, many of which are used in cancer therapy, have emerged as valuable future prospects in the treatment of inflammatory diseases. Read More

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http://dx.doi.org/10.1080/09546634.2019.1589643DOI Listing
March 2019
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Design, synthesis and biological evaluation of novel α-acyloxy carboxamides via Passerini reaction as caspase 3/7 activators.

Eur J Med Chem 2019 Apr 22;168:340-356. Epub 2019 Feb 22.

Department of Microbiology and Immunology, Faculty of Pharmacy, Pharos University in Alexandria, Alexandria, 21311, Egypt.

Evasion of apoptosis is a hallmark of cancer. Caspases; the key executors of apoptotic cascade are attractive targets for selective induction of apoptosis in cancer cells. Within this approach, various caspase activators were introduced as lead anticancer agents. Read More

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http://dx.doi.org/10.1016/j.ejmech.2019.02.051DOI Listing
April 2019
5 Reads
3.447 Impact Factor

Screening techniques for the identification of bioactive compounds in natural products.

J Pharm Biomed Anal 2019 May 19;168:189-200. Epub 2019 Feb 19.

Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing, 100193, China. Electronic address:

Natural products (NPs) have a long history of clinical use and are rich source of bioactive compounds. The development of tools and techniques for identifying and analyzing NP bioactive compounds to ensure their quality and discover new drugs is thus very important and still in demand. Screening techniques have proven highly useful for screening and analyzing active components in complex mixtures, which rely on cell culture, dialysis, ultrafiltration, chromatographic methods and target molecule immobilization, using biological targets to identify the active compounds. Read More

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http://dx.doi.org/10.1016/j.jpba.2019.02.027DOI Listing
May 2019
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Understanding the immune landscape in atopic dermatitis: The era of biologics and emerging therapeutic approaches.

Exp Dermatol 2019 Mar 2. Epub 2019 Mar 2.

Icahn School of Medicine at Mount Sinai, New York City, New York.

Atopic dermatitis (AD) is a chronic, systemic, inflammatory disease that affects the skin and is characterized by persistent itch and marked redness. AD is associated with an increased risk of skin infections and a reduced quality of life. Most AD treatment options to date were not designed to selectively target disease-causing pathways that have been established for this indication. Read More

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http://dx.doi.org/10.1111/exd.13911DOI Listing
March 2019
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Progress Toward Hepatitis B Control and Elimination of Mother-to-Child Transmission of Hepatitis B Virus - Western Pacific Region, 2005-2017.

MMWR Morb Mortal Wkly Rep 2019 Mar 1;68(8):195-200. Epub 2019 Mar 1.

Hepatitis B vaccine (HepB), which has been available since 1982, provides lifelong protection against hepatitis B virus (HBV) infection and the associated 20%-30% increased lifetime risk for developing cirrhosis or hepatocellular carcinoma among >95% of vaccine recipients (1). Before HepB introduction into national childhood immunization schedules, the estimated hepatitis B surface antigen (HBsAg) prevalence in the World Health Organization (WHO) Western Pacific Region (WPR)* was >8% in 1990 (2). In 2005, the WPR was the first WHO region to establish a hepatitis B control goal, with an initial target of reducing HBsAg prevalence to <2% among children aged 5 years by 2012. Read More

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http://dx.doi.org/10.15585/mmwr.mm6808a2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6394384PMC
March 2019
4 Reads

Rationally designed carbohydrate-occluded epitopes elicit HIV-1 Env-specific antibodies.

Nat Commun 2019 02 27;10(1):948. Epub 2019 Feb 27.

Department of Biochemistry and Biophysics, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA.

An array of carbohydrates masks the HIV-1 surface protein Env, contributing to the evasion of humoral immunity. In most HIV-1 isolates 'glycan holes' occur due to natural sequence variation, potentially revealing the underlying protein surface to the immune system. Here we computationally design epitopes that mimic such surface features (carbohydrate-occluded neutralization epitopes or CONE) of Env through 'epitope transplantation', in which the target region is presented on a carrier protein scaffold with preserved structural properties. Read More

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http://dx.doi.org/10.1038/s41467-019-08876-wDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6393580PMC
February 2019
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Evolved Proteins Inhibit Entry of Enfuvirtide-Resistant HIV-1.

ACS Infect Dis 2019 Apr 12;5(4):634-640. Epub 2019 Mar 12.

Department of Chemistry , Colorado State University , 200 W. Lake Street , Fort Collins , Colorado 80523 , United States.

Drugs that block HIV-1 entry are relatively limited. Enfuvirtide is a 36-residue synthetic peptide that targets gp41 and blocks viral fusion. However, Enfuvirtide-resistant HIV has been reported, and this peptide drug requires daily injection. Read More

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http://dx.doi.org/10.1021/acsinfecdis.8b00362DOI Listing

Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors.

Eur J Med Chem 2019 Apr 14;168:110-122. Epub 2019 Feb 14.

School of Science, China Pharmaceutical University, Nanjing, 210009, PR China. Electronic address:

Histone deacetylases (HDACs) as appealing targets for the treatment of many diseases has been studied extensively and its use in cancer care is the most important. Here, we developed a series of novel derivatives containing isoindolinone skeleton. Twelve compounds demonstrated nanomolar IC values against HDAC1, and the best compounds were 5a (65. Read More

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http://dx.doi.org/10.1016/j.ejmech.2019.02.032DOI Listing
April 2019
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Preclinical Models of Alzheimer's Disease: Relevance and Translational Validity.

Curr Protoc Pharmacol 2019 03 25;84(1):e57. Epub 2019 Feb 25.

Department of Biological Chemistry and Pharmacology, College of Medicine, Ohio State University, Columbus, Ohio.

The only drugs currently approved for the treatment of Alzheimer's Disease (AD) are four acetylcholinesterase inhibitors and the NMDA antagonist memantine. Apart from these drugs, which have minimal to no clinical benefit, the 40-year search for effective therapeutics to treat AD has resulted in a clinical failure rate of 100% not only for compounds that prevent brain amyloid deposition or remove existing amyloid plaques but also those acting by a variety of other putative disease-associated mechanisms. This indicates that the preclinical data generated from current AD targets to support the selection, optimization, and translation of new chemical entities (NCEs) and biologics to clinical trials is seriously compromised. Read More

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http://dx.doi.org/10.1002/cpph.57DOI Listing
March 2019
3 Reads