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Drug Discovery Today

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https://www.readbyqxmd.com/read/28713054/aggregation-induced-emission-probes-for-cancer-theranostics
#1
Meng Gao, Ben Zhong Tang
Conventional cancer therapy usually suffers from poor treatment efficiency and adverse effects. To improve the treatment efficiency, it is critical to precisely diagnose specific cancer types and monitor the therapy process in situ. Fluorescence imaging has the advantages of high sensitivity and easy operation, but conventional fluorophores suffer from aggregation-caused quenching (ACQ) and, therefore, their applications for imaging or diagnosis are severely impeded. By contrast, aggregation-induced emission (AIE) probes have significant advantages in terms of excellent photostability and a lack of self-quenching, and can be conveniently incorporated into theranostic platforms by combining them with various therapeutic modalities...
July 13, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28711364/curcumin-and-its-topical-formulations-for-wound-healing-applications
#2
REVIEW
Chandana Mohanty, Sanjeeb K Sahoo
Oxidative damage and inflammation have been identified, through clinical and preclinical studies, as the main causes of nonhealing chronic wounds. Reduction of persistent chronic inflammation by application of antioxidant and anti-inflammatory agents such as curcumin has been well studied. However, low aqueous solubility, poor tissue absorption, rapid metabolism and short plasma half-life have made curcumin unsuitable for systemic administration for better wound healing. Recently, various topical formulations of curcumin such as films, fibers, emulsion, hydrogels and different nanoformulations have been developed for targeted delivery of curcumin at wounded sites...
July 12, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28709991/drugs-as-habitable-planets-in-the-space-of-dark-chemical-matter
#3
Vishal B Siramshetty, Robert Preissner
A recent study demonstrated antifungal activity of dark chemical matter (DCM) compounds that were otherwise inactive in more than 100 HTS assays. These compounds were proposed to possess unique activity and 'clean' safety profiles. Here, we present an outlook of the promiscuity and safety of these compounds by retrospectively comparing their chemical and biological spaces with those of drugs. Significant amounts of marketed drugs (16%), withdrawn drugs (16.5%) and natural compounds (3.5%) share structural identity with DCM...
July 11, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28697371/dendrimer-nanohybrid-carrier-systems-an-expanding-horizon-for-targeted-drug-and-gene-delivery
#4
REVIEW
Prashant Kesharwani, Avinash Gothwal, Arun K Iyer, Keerti Jain, Manish K Chourasia, Umesh Gupta
Highly controllable dendritic structural design means dendrimers are a leading carrier in drug delivery applications. Dendrimer- and other nanocarrier-based hybrid systems are an emerging platform in the field of drug delivery. This review is a compilation of increasing reports of dendrimer interactions, such as dendrimer-liposome, dendrimer-carbon-nanotube, among others, known as hybrid carriers. This should prompt entirely new research with promising results for these hybrid carriers. It is assumed that such emerging hybrid nanosystems - from combining two already-established drug delivery platforms - could lead the way for the development of newer delivery systems with multiple applicability for latent theranostic applications in the future...
July 8, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28692826/efficacy-of-non-vitamin-k-antagonist-oral-anticoagulants-for-intracardiac-thrombi-resolution-in-nonvalvular-atrial-fibrillation
#5
Esteban Orenes-Piñero, María A Esteve-Pastor, Mariano Valdés, Gregory Y H Lip, Francisco Marín
Intracardiac thrombus is a potentially life-threatening condition associated with atrial fibrillation (AF), with a high risk of embolic complications. Oral anticoagulation (OAC) therapy is the first-line treatment for its prevention or resolution. For many patients, traditional OAC treatment using vitamin K antagonists (VKAs; e.g., warfarin) is limited by several factors and the advent of non-VKA oral anticoagulants (NOACs), with improved efficacy and safety profiles, has provided additional treatment options...
July 7, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28689054/implementing-qm-in-docking-calculations-is-it-a-waste-of-computational-time
#6
Adebayo A Adeniyi, Mahmoud E S Soliman
The greatest challenge in molecular docking (MD) is the deficiency of scoring functions (SFs), which limits their reliability. SFs are too simplified to represent the true features of the complex free energy of protein-ligand interactions. Investigations of docking functions have traded accuracy for speed through the use of approximations and simplifications. Consequently, there has been an increase in the popularity of quantum-mechanical (QM)-based methods as reference points for the development of fast, reliable, valuable, yet inexpensive, tools...
July 5, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28687460/2016-in-review-fda-approvals-of-new-molecular-entities
#7
Rebekah H Griesenauer, Michael S Kinch
An overview of drugs approved by FDA in 2016 reveals dramatic disruptions in long-term trends. The number of new molecular entities (NMEs) dropped, reflecting the lowest rate of small-molecule approvals observed in almost five decades. In addition, the pace of industry consolidation slowed substantially. The impact of mergers and acquisitions decreased the total number of organizations with past approval experience and continued research and development (R&D) activities to 102, divided evenly between more established pharmaceutical and newer biotechnology companies...
July 4, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28687459/mouse-models-of-nonalcoholic-steatohepatitis-in-preclinical-drug-development
#8
REVIEW
Henrik H Hansen, Michael Feigh, Sanne S Veidal, Kristoffer T Rigbolt, Niels Vrang, Keld Fosgerau
Nonalcoholic fatty liver disease (NAFLD) has become the most common cause of chronic liver disease in the Western world. NAFLD is a complex spectrum of liver diseases ranging from benign hepatic steatosis to its more aggressive necroinflammatory manifestation, nonalcoholic steatohepatitis (NASH). NASH pathogenesis is multifactorial and risk factors are almost identical to those of the metabolic syndrome. This has prompted substantial efforts to identify novel drug therapies for correcting underlying metabolic deficits, and to prevent or alleviate hepatic fibrosis in NASH...
July 4, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28684326/microfluidic-technologies-for-anticancer-drug-studies
#9
REVIEW
Karolina P Valente, Sultan Khetani, Ahmad R Kolahchi, Amir Sanati-Nezhad, Afzal Suleman, Mohsen Akbari
The study of cancer growth mechanisms and the determination of the efficacy of experimental therapeutics are usually performed in two-dimensional (2D) cell culture models. However, these models are incapable of mimicking complex interactions between cancer cells and the environment. With the advent of microfluidic technologies, the combination of multiple cell cultures with mechanical and biochemical stimuli has enabled a better recapitulation of the three-dimensional (3D) tumor environment using minute amounts of reagents...
July 4, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28683256/a-comprehensive-review-on-polyelectrolyte-complexes
#10
REVIEW
Venkata S Meka, Manprit K G Sing, Mallikarjuna R Pichika, Srinivasa R Nali, Venkata R M Kolapalli, Prashant Kesharwani
Global research on polyelectrolytes at a fundamental and applied level is intensifying because the advantages of sustainability are being accepted in academia and industrial research settings. During recent decades, polyelectrolytes became one of the most attractive subjects of scientific research owing to their great potential in the areas of advanced technologies. Polyelectrolytes are a type of polymer that have multitudinous ionizable functional groups. Ionized polyelectrolytes in solution can form a complex with oppositely charged polyelectrolytes - a polyelectrolyte complex (PEC)...
July 3, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28676407/the-1-2-3-triazole-ring-as-a-bioisostere-in-medicinal-chemistry
#11
Elisa Bonandi, Michael S Christodoulou, Gaia Fumagalli, Dario Perdicchia, Giulio Rastelli, Daniele Passarella
1,2,3-Triazole is a well-known scaffold that has a widespread occurrence in different compounds characterized by several bioactivities, such as antimicrobial, antiviral, and antitumor effects. Moreover, the structural features of 1,2,3-triazole enable it to mimic different functional groups, justifying its wide use as a bioisostere for the synthesis of new active molecules. Here, we provide an overview of the 1,2,3-triazole ring as a bioisostere for the design of drug analogs, highlighting relevant recent examples...
July 1, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28676406/switching-off-cd73-a-way-to-boost-the-activity-of-conventional-and-targeted-antineoplastic-therapies
#12
Luca Antonioli, Sergey V Novitskiy, Kris F Sachsenmeier, Matteo Fornai, Corrado Blandizzi, György Haskó
Over the past few years, several preclinical studies have highlighted the value of CD73 (ecto-5'-nucleotidase) as a potential therapeutic target for cancer therapy. Indeed, the pharmacological blockade of CD73, via monoclonal antibodies or small molecules, has promise in counteracting cancer development, growth and spread. Synergistic combinations of anti-CD73 drugs with conventional cancer treatments (i.e., chemotherapy, radiation therapy, immunotherapy, targeted therapy) have increased therapeutic potential...
July 1, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28676405/pan-assay-interference-compounds-pains-that-may-not-be-too-painful-for-chemical-biology-projects
#13
EDITORIAL
David Lagorce, Natacha Oliveira, Maria A Miteva, Bruno O Villoutreix
No abstract text is available yet for this article.
July 1, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28669605/industrial-medicinal-chemistry-insights-neuroscience-hit-generation-at-janssen
#14
REVIEW
Gary Tresadern, Frederik J R Rombouts, Daniel Oehlrich, Gregor Macdonald, Andres A Trabanco
The role of medicinal chemistry has changed over the past 10 years. Chemistry had become one step in a process; funneling the output of high-throughput screening (HTS) on to the next stage. The goal to identify the ideal clinical compound remains, but the means to achieve this have changed. Modern medicinal chemistry is responsible for integrating innovation throughout early drug discovery, including new screening paradigms, computational approaches, novel synthetic chemistry, gene-family screening, investigating routes of delivery, and so on...
June 29, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28651064/progranulin-as-a-biomarker-and-potential-therapeutic-agent
#15
REVIEW
Vanessa Abella, Jesús Pino, Morena Scotece, Javier Conde, Francisca Lago, Miguel Angel Gonzalez-Gay, Antonio Mera, Rodolfo Gómez, Ali Mobasheri, Oreste Gualillo
Progranulin is a cysteine-rich secreted protein with diverse pleiotropic actions and participates in several processes, such as inflammation or tumorigenesis. Progranulin was first identified as a growth factor and, recently, it was characterised as an adipokine implicated in obesity, insulin resistance and rheumatic disease. At a central level, progranulin acts as a neurotropic and neuroprotective factor and protects from neural degeneration. In this review, we summarise the most recent research advances concerning the potential role of progranulin as a therapeutic target and biomarker in cancer, neurodegenerative and inflammatory diseases...
June 23, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28647378/leishmaniasis-drug-discovery-recent-progress-and-challenges-in-assay-development
#16
REVIEW
Bilal Zulfiqar, Todd B Shelper, Vicky M Avery
Leishmaniasis, caused by the trypanosomatid protozoan Leishmania, is endemic in 98 countries worldwide, with morbidity and mortality increasing daily. Despite available drugs, leishmaniasis faces the challenge of emerging resistance and toxicity concerns for current drug regimes. Identification of anti-leishmanial compounds representing new chemistry and novel mechanisms of action is essential to populate the drug discovery pipeline. The in vitro assays currently available have shown poor translational outcomes, with high compound attrition rates...
June 21, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28647377/establishing-rarity-in-the-context-of-orphan-medicinal-product-designation-in-the-european-union
#17
REVIEW
Stelios Tsigkos, Matthias Hoffer, Maria Sheean, Segundo Mariz, Kristina Larsson, Frauke Naumann-Winter, Laura Fregonese, Bruno Sepodes
In the European Union (EU) legislative framework for orphan medicinal product designation, establishing that a condition affects not more than five in 10,000 people is a prerequisite for applications based on rarity. Demonstrating this requirement to the Committee of Orphan Medicinal Products (COMP) can be a particularly challenging task for sponsors. Here, we identify and examine three common issues with the estimation of prevalence in orphan drug applications in the EU (the discernment between diagnosed and undiagnosed cases; the duration of the disease; and the need for an explicit contemporary conclusion) as critical factors for acceptable prevalence estimation...
June 21, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28646641/do-large-mergers-increase-or-decrease-the-productivity-of-pharmaceutical-r-d
#18
Michael S Ringel, Michael K Choy
There is current uncertainty regarding the effects of mergers on pharmaceutical R&D productivity, with various mechanisms reported by which mergers could either help or harm R&D, and mixed empirical findings in prior analyses. Here, we present an analysis that is novel in several ways: we use downstream measures of R&D productivity, account for both inputs and outputs in our calculations, and use a self-controlled design. We find that recent large pharmaceutical mergers are associated with statistically significant increases in R&D productivity...
June 21, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28625610/current-progress-in-antivascular-tumor-therapy
#19
REVIEW
Yi-Ju Ho, Tzu-Chia Wang, Ching-Hsiang Fan, Chih-Kuang Yeh
The tumor vasculature transports oxygen, nutrients and drugs for crucial roles in tumor therapy. Antivascular therapy directly targets existing tumor vessels to reduce blood perfusion and then inhibit tumor growth. Vascular disrupting agents and ultrasound-stimulated microbubble destruction use chemical toxicity and physical effect, respectively, to damage vascular endothelial cells for antivascular therapy. Moreover, antivascular therapy can break vessel wall barriers and change the tumor microenvironment to compensate for the limitations of conventional chemotherapy or radiotherapy...
June 16, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28624633/from-flamingo-dance-to-desirable-drug-discovery-a-nature-inspired-approach
#20
REVIEW
Aminael Sánchez-Rodríguez, Yunierkis Pérez-Castillo, Stephan C Schürer, Orazio Nicolotti, Giuseppe Felice Mangiatordi, Fernanda Borges, M Natalia D S Cordeiro, Eduardo Tejera, José L Medina-Franco, Maykel Cruz-Monteagudo
The therapeutic effects of drugs are well known to result from their interaction with multiple intracellular targets. Accordingly, the pharma industry is currently moving from a reductionist approach based on a 'one-target fixation' to a holistic multitarget approach. However, many drug discovery practices are still procedural abstractions resulting from the attempt to understand and address the action of biologically active compounds while preventing adverse effects. Here, we discuss how drug discovery can benefit from the principles of evolutionary biology and report two real-life case studies...
June 15, 2017: Drug Discovery Today
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