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Expert Opinion on Drug Discovery

Semih Calamak, Reza Shahbazi, Ipek Eroglu, Merve Gultekinoglu, Kezban Ulubayram
Introduction Conventional administration of antibacterial drugs to the human body can cause vital problems such as dose dependent systemic toxicity and bacterial resistance which prevent the healing process. In this regard, recent studies have been devoted to producing nanofiber based antibacterial drug delivery approaches which surpass bacterial resistance and toxicological issues. Areas covered This review summarizes latest developments in the production of antibacterial nanofibers, nanofiber based antibacterial action mechanisms and release profiles of nanofibers...
February 6, 2017: Expert Opinion on Drug Discovery
Mohammad-Reza Rashidi, Somaieh Soltani
Given the rising trend in medicinal chemistry strategy to reduce cytochrome P450-dependent metabolism, aldehyde oxidase (AOX) has recently gained increased attention in drug discovery programs and the number of drug candidates that are metabolized by AOX is steadily growing. Areas covered: Despite the emerging importance of AOX in drug discovery, there are certain major recognized problems associated with AOX-mediated metabolism of drugs. Intra- and inter-species variations in AOX activity, the lack of reliable and predictive animal models using the common experimental animals, and failure in the predictions of in vivo metabolic activity of AOX using traditional in vitro methods are among these issues that are covered in this article...
February 6, 2017: Expert Opinion on Drug Discovery
Aravindhan Ganesan, Khaled Barakat
Hepatitis C virus (HCV) is a global health problem that causes several chronic life-threatening liver diseases. The numbers of people affected by HCV are rising annually. Since 2011, the FDA has approved several anti-HCV drugs; while many other promising HCV drugs are currently in late clinical trials. Areas covered: This review discusses the applications of different computational approaches in HCV drug design. Expert opinion: Molecular docking and virtual screening approaches have emerged as a low-cost tool to screen large databases and identify potential small-molecule hits against HCV targets...
February 4, 2017: Expert Opinion on Drug Discovery
Nataraj S Pagadala, Khajamohiddin Syed, Rakesh Bhat
To date, various therapeutic strategies identified numerous anti-prion compounds and antibodies that stabilize PrP(C), block the conversion of PrP(C)-PrP(Sc) and increased effect on PrP(Sc) clearance. However, no suitable drug has been identified clinically so far due to the poor oral absorption, low blood-brain-barrier [BBB] penetration, and high toxicity. Although some of the drugs were proven to be effective in prion-infected cell culture and whole animal models, none of them increased the rate of survival compared to placebo...
February 2, 2017: Expert Opinion on Drug Discovery
Barbara Maino, Simona Paparone, Cinzia Severini, Maria Teresa Ciotti, Velia D'agata, Pietro Calissano, Sebastiano Cavallaro
Inappropriate activation of apoptosis may contribute to neurodegeneration, a multifaceted process that results in various chronic disorders, including Alzheimer's and Parkinson's diseases. Several in vitro and in vivo studies demonstrated that neuronal apoptosis is a multi-pathway cell-death program that requires RNA synthesis. Thus, transcriptionally activated genes whose products induce cell death can be triggered by different stimuli and antagonized by neurotrophic factors. Systems biology is now unveiling the series of intracellular signaling pathways and key drug targets at the intersection of neuronal apoptosis and survival...
January 23, 2017: Expert Opinion on Drug Discovery
Rajan Chaudhari, Zhi Tan, Beibei Huang, Shuxing Zhang
Over the past couple of years, the cost of drug development has sharply increased along with the high rate of clinical trial failures. Such increase in expenses is partially due to the inability of the "one drug - one target" approach to predict drug side effects and toxicities. To tackle this issue, an alternative approach, known as polypharmacology, is being adopted to study small molecule interactions with multiple targets. Apart from developing more potent and effective drugs, this approach allows for studies of off-target activities and the facilitation of drug repositioning...
January 23, 2017: Expert Opinion on Drug Discovery
Sehee Choi, Kang-Yell Choi
Protein-protein interactions (PPIs) are very attractive targets for drug development as they play important roles in regulating many aspects of pathophysiologies. It has recently been revealed that the functionally important region of most PPIs is small enough to be modulated by small molecules. Thus, many studies in this field have achieved amazing progress, together with diverse and advanced screening technologies. Areas covered: This article presents screening technologies to identify small molecule inhibitors of PPIs in addition to discussing the suitability of PPIs as molecular targets...
January 20, 2017: Expert Opinion on Drug Discovery
Renu Agarwal, Puneet Agarwal
Rodents have widely been used to represent glaucomatous changes both in the presence and absence of elevated intraocular pressure (IOP) as they offer clear advantages over other animal species. IOP elevation is commonly achieved by creating an obstruction in the aqueous outflow pathways, consequently leading to retinal ganglion cell and optic nerve (ON) damage, the hallmark of glaucoma. These changes may also be achieved in the absence of elevated IOP by directly inflicting injury to retina or ON. Areas covered: This paper presents a summary of currently used rodent models of glaucoma...
January 18, 2017: Expert Opinion on Drug Discovery
Ramin Rezaee, Mohammad Abdollahi
No abstract text is available yet for this article.
January 17, 2017: Expert Opinion on Drug Discovery
James E Pease
By virtue of its specificity for chemokines induced in Th1-associated pathologies, CXCR3 has attracted considerable attention as a target for therapeutic intervention. Several pharmacologically distinct small molecules with in vitro and in vivo potency have been described in the literature, although to date, none have shown efficacy in clinical trials. Areas covered: In this article, the author outlines the rationale for targeting CXCR3 and discusses the potential pitfalls in targeting receptors in poorly understood areas of chemokine biology...
December 30, 2016: Expert Opinion on Drug Discovery
Gisbert Schneider, Petra Schneider
Rational drug discovery would greatly benefit from a more nuanced appreciation of the activity of pharmacologically active compounds against a diverse panel of macromolecular targets. Already, computational target-prediction models assist medicinal chemists in library screening, de novo molecular design, optimization of active chemical agents, drug re-purposing, in the spotting of potential undesired off-target activities, and in the 'de-orphaning' of phenotypic screening hits. The self-organizing map (SOM) algorithm has been employed successfully for these and other purposes...
December 27, 2016: Expert Opinion on Drug Discovery
Annalucia Serafino, Gianluca Sferrazza, Arianna Colini Baldeschi, Giuseppe Nicotera, Federica Andreola, Eugenia Pittaluga, Pasquale Pierimarchi
Wnt/β-catenin signaling is an evolutionarily conserved pathway that has a crucial role in embryonic and adult life. Dysregulation of Wnt/β-catenin pathway has been associated with various diseases, including cancer and neurodegenerative disorders, including Parkinson's disease (PD). Several molecular components of the signaling have been proposed as innovative targets for cancer therapy, and very recently, some of them have been also evaluated as potential therapeutic targets for PD. Areas covered: This review focuses on the role of Wnt/β-catenin pathway in the pathogenensis of cancer and PD, examining some recent therapeutic approaches that are ongoing in preclinical and clinical studies...
December 26, 2016: Expert Opinion on Drug Discovery
Debby Van Dam, Peter Paul De Deyn
Pathophysiological mechanisms underlying Alzheimer's disease (AD) remain insufficiently documented for the identification of accurate diagnostic markers and purposeful target discovery and development. Nonhuman primates (NHPs) have important translational value given their close phylogenetic relationship to humans and similar developmental paths in (neuro)anatomy, physiology, genetics, and neural functions, as well as cognition, emotion, and social behavior. Areas covered: This review deals with the past and future role of NHP-based research in AD pathophysiology, diagnosis and drug discovery, and touches upon ethical and legal aspects...
December 25, 2016: Expert Opinion on Drug Discovery
Hong Yao, Junkai Liu, Shengtao Xu, Zheying Zhu, Jinyi Xu
Throughout history, natural products (NPs) have provided a rich source of compounds that have wide applications in the fields of medicine, health sciences, pharmacy and biology. Although naturally active substances are good lead compounds for the discovery of new drugs, most of them suffer from various deficiencies or shortcomings, such as complex structures, poor stability and solubility. Therefore, structural modification of NPs is needed to develop novel compounds with specific properties. Areas covered: This article presents an overview on the structural modifications of NPs in drug development...
December 22, 2016: Expert Opinion on Drug Discovery
Maria Teresa Donato, Maria José Gómez-Lechón, Laia Tolosa
The need for alternatives to animal experimentation and traditional testing methods has been widely discussed in recent years. This has led scientists and regulatory authorities to investigate alternative methods for toxicity testing. High-content screening (HCS) has emerged as a powerful tool in predictive toxicology since it permits molecular, cellular and tissue-based toxicity assessments. HCS allows automated image acquisition and analysis, and provides information on multiple properties of individual cells loaded simultaneously with fluorescent dyes, which is used for drug safety evaluations...
December 21, 2016: Expert Opinion on Drug Discovery
Richard Arkwright, Tri Minh Pham, Jeffrey A Zonder, Q Ping Dou
Mantle cell lymphoma (MCL) is an incurable, often aggressive B-cell malignancy. Bortezomib (BTZ), the 20S proteasome inhibitor was originally developed and approved for treatment of relapsed refractory multiple myeloma, and subsequently approved for treatment of MCL. BTZ's single-agent activity induces clinical responses in approximately one-third of relapsed MCL patients. BTZ-containing combination therapies have further improved the quality and duration of clinical responses compared to standard chemotherapies in previously untreated MCL patients...
December 20, 2016: Expert Opinion on Drug Discovery
Claire M Ouimet, Cara I D'amico, Robert T Kennedy
Many screening platforms are prone to assay interferences that can be avoided by directly measuring the target or enzymatic product. Capillary electrophoresis (CE) and microchip electrophoresis (MCE) have been applied in a variety of formats to drug discovery. CE provides direct detection of the product allowing for the identification of some forms of assay interference. The high efficiency, rapid separations, and low volume requirements make CE amenable to drug discovery. Areas covered: This article describes advances in capillary electrophoresis throughput, sample introduction, and target assays as they pertain to drug discovery and screening...
December 9, 2016: Expert Opinion on Drug Discovery
Bradley C Doak, Jan Kihlberg
No abstract text is available yet for this article.
December 8, 2016: Expert Opinion on Drug Discovery
Yukinori Nagakura
Chronic pain is a major healthcare issue owing to its high prevalence, significant physical and emotional burden on the patients, and huge financial burden on the society. The efficacy of currently available medications is unsatisfactory owing to their limited effect size and the low responder rate (less than 50%). Thus, there is a large unmet need for innovative therapies for chronic pain. Areas covered: In this review, the author points out the need for fundamental reforms in pain research. For the last several decades, drug discovery research has extensively focused on designing new therapies using animal models of chronic pain...
January 2017: Expert Opinion on Drug Discovery
Kam Lun Hon, Vivian W Y Lee
The drug development industry is restructuring worldwide in terms of the research and development process. As with pharmaceuticals in the west, China faces major challenges for drug discovery and development. Areas covered: In this review, the authors discuss anti-cancer, anti-allergy, anti-infectious, and proprietary Chinese Medicines (pCM) for various chronic diseases (such as the allergic diseases: eczema, asthma and allergic rhinitis), which remain the contemporary therapeutic strategies that are being explored and developed...
January 2017: Expert Opinion on Drug Discovery
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