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https://www.readbyqxmd.com/read/28215166/seaweed-polysaccharides-new-therapeutic-insights-against-the-inflammatory-response-in-diabetic-nephropathy
#1
Vaishnu Devi Da, Pragasam Viswanathan
BACKGROUND: The higher risk of diabetic nephropathy (DN) leads to end stage renal diseases in worldwide, which is associated with chronic inflammation. Currently, the available treatments are limited, lack of efficacy and safety. Therefore, we are in need of novel targets and advanced treatments to reduce the necessity for the renal replacement therapy and burden of this disease management. In this review, we performed through an inflammatory mechanism that contribute to DN, will provide a key point to the finding off novel therapeutic agents...
February 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28198666/design-connecting-gene-expression-with-therapeutics-for-drug-repurposing-and-development
#2
Bernard Kok Bang Lee, Kai Hung Tiong, Jit Kang Chang, Chee Sun Liew, Zainal Ariff Abdul Rahman, Aik Choon Tan, Tsung Fei Khang, Sok Ching Cheong
BACKGROUND: The drug discovery and development pipeline is a long and arduous process that inevitably hampers rapid drug development. Therefore, strategies to improve the efficiency of drug development are urgently needed to enable effective drugs to enter the clinic. Precision medicine has demonstrated that genetic features of cancer cells can be used for predicting drug response, and emerging evidence suggest that gene-drug connections could be predicted more accurately by exploring the cumulative effects of many genes simultaneously...
January 25, 2017: BMC Genomics
https://www.readbyqxmd.com/read/28195646/ns1209-spd-502-a-novel-selective-ampa-antagonist-for-stroke-neuropathic-pain-or-epilepsy-drug-development-lessons-learned
#3
Jan M Keppel Hesselink
Preclinical Research The selective AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor antagonist, NS1209 (also known as SPD 502) has been explored in several research and development campaigns since its selection as a lead drug candidate in the early 1990s by the Danish biotechnology company, NeuroSearch. The compound was successively tested in animal models of stroke, neuropathic pain and epilepsy. The preclinical data to support development for the treatment of stroke were incomplete, as the compound was administered after the stroke episode, and did not protect subcortical areas of the brain...
February 13, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28188812/epigenetics-in-cancer-fundamentals-and-beyond
#4
REVIEW
Subhankar Biswas, C Mallikarjuna Rao
Activation of oncogenes or the deactivation of tumor suppressor genes has long been established as the fundamental mechanism leading towards carcinogenesis. Although this age old axiom is vastly accurate, thorough study over the last 15years has given us unprecedented information on the involvement of epigenetic in cancer. Various biochemical pathways that are essential towards tumorigenesis are regulated by the epigenetic phenomenons like remodeling of nucleosome by histone modifications, DNA methylation and miRNA mediated targeting of various genes...
February 8, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28178257/drug-pipeline-4q16
#5
Laura DeFrancesco
No abstract text is available yet for this article.
February 8, 2017: Nature Biotechnology
https://www.readbyqxmd.com/read/28169001/emerging-approaches-to-tuberculosis-drug-development-at-home-in-the-metabolome
#6
REVIEW
Robert S Jansen, Kyu Y Rhee
Once considered a crowning achievement of modern drug development, tuberculosis (TB) chemotherapy has proven increasingly unable to keep pace with the spread of the pandemic and rise of drug resistance. Efforts to revive the TB drug development pipeline have, in the meantime, faltered. Closer analysis reveals key experimental deficiencies that have hindered our ability to 'reverse engineer' knowledge of antibiotic mechanisms into rational drug development. Here, we discuss the emerging potential of metabolomics; the systems level study of small molecule metabolites, to help overcome these gaps and serve as a unique biochemical bridge between the phenotypic properties of chemical compounds and biological targets...
February 3, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28161807/what-we-may-expect-from-novel-antibacterial-agents-in-the-pipeline-with-respect-to-resistance-and-pharmacodynamic-principles
#7
REVIEW
Karen Bush, Malcolm G P Page
There are some 43 small molecules in the antibiotic development pipeline from late preclinical stage (7 compounds) through Phase 1 (11 molecules), Phase 2 (13 molecules) to Phase 3 (12 molecules). The majority of these are representatives of established antibiotic classes that have been modified to address problems of resistance. In addition, there is considerable activity around the discovery of novel classes of β-lactamase inhibitors with 10 combinations representing 4 inhibitor classes, at different stages of development...
February 4, 2017: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/28159738/therapeutic-targeting-of-acute-myeloid-leukemia-stem-cells
#8
Daniel A Pollyea, Craig T Jordan
For over 50 years investigators have considered a malignant stem cell as the potential origin of and a key therapeutic target for acute myeloid leukemia (AML) and other forms of cancer(1-4) The nature and existence of tumor-initiating cells for leukemia and other malignancies has long been the subject of intense and rigorous study; indeed, the promise of the potential to eradicate such cells is clear. However, until recently, deficiencies in our understanding of the nature of these cell populations, coupled with a limited ability to therapeutically exploit their weaknesses, have been limiting factors towards realizing the goal of targeting leukemia stem cells (LSCs)...
February 3, 2017: Blood
https://www.readbyqxmd.com/read/28155846/rationalizing-the-permeation-of-polar-antibiotics-into-gram-negative-bacteria
#9
Mariano Andrea Scorciapino, Silvia Acosta-Gutierrez, Dehbia Benkerrou, Tommaso D'Agostino, Giuliano Malloci, Susruta Samanta, Igor Bodrenko, Matteo Ceccarelli
The increasing level of antibiotic resistance in Gram-negative bacteria, together with the lack of new potential drug scaffolds in the pipeline, make the problem of infectious diseases a global challenge for modern medicine. The main reason that Gram-negative bacteria are particularly challenging is the presence of an outer cell-protecting membrane, which is not present in Gram-positive species. Such an asymmetric bilayer is a highly effective barrier for polar molecules. Several protein systems are expressed in the outer membrane to control the internal concentration of both nutrients and noxious species, in particular: (i) water-filled channels that modulate the permeation of polar molecules and ions according to concentration gradients, and (ii) efflux pumps to actively expel toxic compounds...
March 22, 2017: Journal of Physics. Condensed Matter: An Institute of Physics Journal
https://www.readbyqxmd.com/read/28139976/an-aging-independent-replicative-lifespan-in-a-symmetrically-dividing-eukaryote
#10
Eric C Spivey, Stephen K Jones, James R Rybarski, Fatema A Saifuddin, Ilya J Finkelstein
The replicative lifespan (RLS) of a cell-defined as the number of cell divisions before death-has informed our understanding of the mechanisms of cellular aging. However, little is known about aging and longevity in symmetrically dividing eukaryotic cells because most prior studies have used budding yeast for RLS studies. Here, we describe a multiplexed fission yeast lifespan micro-dissector (multFYLM) and an associated image processing pipeline for performing high-throughput and automated single-cell micro-dissection...
January 31, 2017: ELife
https://www.readbyqxmd.com/read/28137721/transcriptional-functional-and-mechanistic-comparisons-of-stem-cell-derived-hepatocytes-heparg-cells-and-3d-human-hepatocyte-spheroids-as-predictive-in-vitro-systems-for-drug-induced-liver-injury
#11
Catherine C Bell, Volker M Lauschke, Sabine U Vorrink, Henrik Palmgren, Roger Duffin, Tommy B Andersson, Magnus Ingelman-Sundberg
Reliable and versatile hepatic in vitro systems for the prediction of drug pharmacokinetics and toxicity are essential constituents of preclinical safety assessment pipelines for new medicines. Here, we compared three emerging cell systems, hepatocytes derived from induced pluripotent stem cells (hiPS-Hep), HepaRG cells and 3D primary human hepatocyte (PHH) spheroids at transcriptional and functional levels in a multi-center study to evaluate their potential as predictive models for drug-induced hepatotoxicity...
January 30, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28137645/how-can-nanoparticles-contribute-to-antituberculosis-therapy
#12
REVIEW
Joana Costa-Gouveia, José A Aínsa, Priscille Brodin, Ainhoa Lucía
Therapeutic approaches using nanoparticles are being successfully used in foods and in several fields of medicine, including infectious diseases. Regarding tuberculosis (TB) treatment, nanoparticles can be a useful strategy for two distinct applications: (i) for their intrinsic antimycobacterial activity; (ii) as vehicles for known antitubercular drugs to allow reduction of dose- and drug-associated side-effects and administration via user-friendly administration routes such as pulmonary or oral ones. Promising results were obtained in vitro and in animal Mycobacterium tuberculosis models and need now to be translated into clinical drug candidates...
January 27, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28128554/discovery-of-c-glycosylpyranonaphthoquinones-in-streptomyces-sp-mbt76-by-a-combined-nmr-based-metabolomics-and-bioinformatics-workflow
#13
Changsheng Wu, Chao Du, Koji Ichinose, Young Hae Choi, Gilles P van Wezel
Mining of microbial genomes has revealed that actinomycetes harbor far more biosynthetic potential for bioactive natural products than anticipated. Activation of (cryptic) biosynthetic gene clusters and identification of the corresponding metabolites has become a focal point for drug discovery. Here, we applied NMR-based metabolomics combined with bioinformatics to identify novel C-glycosylpyranonaphthoquinones in Streptomyces sp. MBT76 and to elucidate the biosynthetic pathway. Following activation of the cryptic qin gene cluster for a type II polyketide synthase (PKS) by constitutive expression of its pathway-specific activator, bioinformatics coupled to NMR profiling facilitated the chromatographic isolation and structural elucidation of qinimycins A-C (1-3)...
January 27, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28126288/medicinal-attributes-of-1-2-3-triazoles-current-developments
#14
REVIEW
Divya Dheer, Virender Singh, Ravi Shankar
1,2,3-Triazoles are important five-membered heterocyclic scaffold due to their extensive biological activities. This framework can be readily obtained in good to excellent yields on the multigram scale through click chemistry via reaction of aryl/alkyl halides, alkynes and NaN3 under ambient conditions. It has been an emerging area of interest for many researchers throughout the globe owing to its immense pharmacological scope. The present work aims to summarize the current approaches adopted for the synthesis of the 1,2,3-triazole and medicinal significance of these architectures as a lead structure for the discovery of drug molecules such as COX-1/COX-2 inhibitors (celecoxib, pyrazofurin), HIV protease inhibitors, CB1 cannabinoid receptor antagonist and much more which are in the pipeline of clinical trials...
January 18, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28124597/pimping-up-drugs-recovered-superannuated-and-under-exploited-drugs-an-introduction-to-the-basics-of-drug-reprofiling
#15
Suzanne Jane Dilly, George Stephen Morris
Drug development has moved along way forward from the days of with doctors peddling cauldrons of herbs and spices, however the process can still miss opportunities for full exploitation of a drug's potential. Drug reprofiling provides a chance for an established or a forgotten drug to move into a new area of therapy, whether related to the known effects or in a completely new area. In an era of environmental awareness and spiraling costs for traditional drug development, a strategy to squeeze every benefit out of drugs with known safety, tolerability and pharmacological parameters must be a strategically sound desire...
January 17, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28120901/patient-specific-hepatocyte-like-cells-derived-from-induced-pluripotent-stem-cells-model-pazopanib-mediated-hepatotoxicity
#16
Yukti Choudhury, Yi Chin Toh, Jiangwa Xing, Yinghua Qu, Jonathan Poh, Li Huan, Hui Shan Tan, Ravindran Kanesvaran, Hanry Yu, Min-Han Tan
Idiosyncratic drug-induced hepatotoxicity is a major cause of liver damage and drug pipeline failure, and is difficult to study as patient-specific features are not readily incorporated in traditional hepatotoxicity testing approaches using population pooled cell sources. Here we demonstrate the use of patient-specific hepatocyte-like cells (HLCs) derived from induced pluripotent stem cells for modeling idiosyncratic hepatotoxicity to pazopanib (PZ), a tyrosine kinase inhibitor drug associated with significant hepatotoxicity of unknown mechanistic basis...
January 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28120254/application-of-pharmacokinetics-and-pharmacodynamics-in-product-life-cycle-management-a-case-study-with-a-carbidopa-levodopa-extended-release-formulation
#17
Nishit B Modi
Increasing costs in discovering and developing new molecular entities and the continuing debate on limited company pipelines mean that pharmaceutical companies are under significant pressure to maximize the value of approved products. Life cycle management in the context of drug development comprises activities to maximize the effective life of a product. Life cycle approaches can involve new formulations, new routes of delivery, new indications or expansion of the population for whom the product is indicated, or development of combination products...
January 24, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28114255/novel-targeted-therapies-for-metastatic-melanoma
#18
Wade T Iams, Jeffrey A Sosman, Sunandana Chandra
Oncogene-targeted therapy is a major component of precision oncology, and although patients with metastatic melanoma have experienced improved outcomes with this strategy, there are a number of potential therapeutic targets currently under study that may further increase the drug armamentarium for this patient population. In this review, we discuss the landscape of targeted therapies for patients with advanced melanoma, focusing on oncogene mutation-specific targets. In patients with typical BRAF V600-mutant melanoma, combination BRAF and MEK inhibition has surpassed outcomes compared with monotherapy with BRAF or MEK inhibition alone, and current strategies seek to address inevitable resistance mechanisms...
January 2017: Cancer Journal
https://www.readbyqxmd.com/read/28110506/antibiotic-discovery-throughout-the-small-world-initiative-a-molecular-strategy-to-identify-biosynthetic-gene-clusters-involved-in-antagonistic-activity
#19
Elizabeth Davis, Tyler Sloan, Krista Aurelius, Angela Barbour, Elijah Bodey, Brigette Clark, Celeste Dennis, Rachel Drown, Megan Fleming, Allison Humbert, Elizabeth Glasgo, Trent Kerns, Kelly Lingro, MacKenzie McMillin, Aaron Meyer, Breanna Pope, April Stalevicz, Brittney Steffen, Austin Steindl, Carolyn Williams, Carmen Wimberley, Robert Zenas, Kristen Butela, Hans Wildschutte
The emergence of bacterial pathogens resistant to all known antibiotics is a global health crisis. Adding to this problem is that major pharmaceutical companies have shifted away from antibiotic discovery due to low profitability. As a result, the pipeline of new antibiotics is essentially dry and many bacteria now resist the effects of most commonly used drugs. To address this global health concern, citizen science through the Small World Initiative (SWI) was formed in 2012. As part of SWI, students isolate bacteria from their local environments, characterize the strains, and assay for antibiotic production...
January 22, 2017: MicrobiologyOpen
https://www.readbyqxmd.com/read/28109622/genetics-for-the-identification-of-lipid-targets-beyond-pcsk9
#20
REVIEW
Linda R Wang, Robert A Hegele
From studies of rare families to genome-wide associations in populations, understanding of human genetics has accelerated the search for new drug targets for the prevention of atherosclerotic cardiovascular disease. DNA sequencing and genome-wide analyses of DNA markers have illuminated rare as well as common variants in genes that regulate lipids and ultimately atherosclerosis risk. A recent innovative approach called Mendelian randomization can endorse specific genes and variants as causative not just for lipid disturbances, but also for clinical cardiovascular end points...
November 11, 2016: Canadian Journal of Cardiology
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