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Expert Opinion on Drug Discovery

Emanuela Berrino, Claudiu T Supuran
Microwave (MW)-assisted synthesis of biologically active compounds has received a lot of attention in the last decades due to the advantages that such a technique offers compared to traditional heating procedures. Areas covered: The authors provide a focused review on the recent applications of this technique for drug design purposes. MW syntheses have been used for designing libraries of compounds, in combinatorial and multicomponent approaches, for lead optimization, as well as for forcing reactions which do not occur or occur in low yields using traditional methods...
July 16, 2018: Expert Opinion on Drug Discovery
George Lambrinidis, Anna Tsantili-Kakoulidou
The complexity in the drug discovery pipeline, in combination with the exponential growth of experimental and computational data, the technological achievements, and the access to large data sets, has led to a continuous evolution and transformation of quantitative structure-activity relationships (QSAR) to compete with the challenges of multi-objective drug discovery. Areas covered: After a short overview of the multiple objectives involved in drug discovery, this review focuses on definition of the drug-like space and the construction of local and/or global models, platforms and workflows for step-by-step single-objective optimization (SOO) of the different and often conflicting processes...
July 12, 2018: Expert Opinion on Drug Discovery
Carlos F M Silva, Vasco F Batista, Diana C G A Pinto, Artur M S Silva
No abstract text is available yet for this article.
July 9, 2018: Expert Opinion on Drug Discovery
Donna A Volpe, Hisham Qosa
Given that membrane efflux transporters can influence a drug's pharmacokinetics, efficacy and safety, identifying potential substrates and inhibitors of these transporters is a critical element in the drug discovery and development process. Additionally, it is important to predict the inhibition potential of new drugs to avoid clinically significant drug interactions. The goal of preclinical studies is to characterize a new drug as a substrate or inhibitor of efflux transporters. Areas Covered: This article reviews preclinical systems that are routinely utilized to determine whether a new drug is substrate or inhibitor of efflux transporters including in silico models, in vitro membrane and cell assays, and animal models...
June 26, 2018: Expert Opinion on Drug Discovery
Olapeju Bolarinwa, Jianfeng Cai
The development of multidrug-resistant strains of bacteria resulting from prolonged treatment with conventional antibiotics has necessitated the need for continuous research for better antibiotic strategies. One of these alternatives is evolutionary antimicrobial peptides also known as host-defense peptides (HDPs). HDPs are an integral part of the innate defense system in multicellular eukaryotes. Although HDPs can largely circumvent the persistent problem of antibiotic resistance due to their bacteriolytic membrane mechanism, they have some drawbacks including a low activity profile and protease instability...
June 22, 2018: Expert Opinion on Drug Discovery
Aditya Kiran Gatta, Raghu Chandrashekhar Hariharapura, Nayanabhirama Udupa, Meka Sreenivasa Reddy, Venkata Rao Josyula
RNA interference has become a tool of choice in the development of drugs in various therapeutic areas of Post Transcriptional Gene Silencing (PTGS). The critical element in developing successful RNAi therapeutics lies in designing small interfering RNA (siRNA) using an efficient algorithm satisfying the designing criteria. Further, translation of siRNA from bench-side to bedside needs an efficient delivery system and/or chemical modification. Areas covered: This review emphasizes the importance of dicer, the criteria for efficient siRNA design, the currently available algorithms and strategies to overcome off-target effects, immune stimulatory effects and endosomal trap...
June 14, 2018: Expert Opinion on Drug Discovery
Gary A Gintant, Christopher H George
Despite a burgeoning knowledge of the intricacies and mechanisms responsible for human disease, technological advances in medicinal chemistry, and more efficient assays used for drug screening, it remains difficult to discover novel and effective pharmacologic therapies. Areas covered: By reference to the primary literature and concepts emerging from academic and industrial drug screening landscapes, the authors propose that this disconnect arises from the inability to scale and integrate responses from simpler model systems to outcomes from more complex and human-based biological systems...
June 6, 2018: Expert Opinion on Drug Discovery
D Merlotti, M Materozzi, T Picchioni, S Bianciardi, M Alessandri, R Nuti, L Gennari
Osteoporosis is a growing health and health-economic problem due to the increased proportion of elderly people in the population. Basic and clinical advances in research over the past two decades have led to the development of different compounds with antiresorptive or anabolic activity on bone that improved substantially the management of patients with osteoporosis over calcitonin or estrogen replacement. New compounds are in preclinical and clinical development. Areas covered: In this review, the authors review the approaches for the preclinical and clinical development of antiresorptive and anabolic agents for osteoporosis, particularly focusing on the recent advances in technology and in the understanding of skeletal biology, together with their implications on novel osteoporosis drug discovery...
June 5, 2018: Expert Opinion on Drug Discovery
Yaxi Li, Tianfu Wu
Systemic lupus erythematosus (SLE) is a complex autoimmune disease with a high risk of morbidity and mortality; however, there is no cure and the current medications are far from optimal in addressing efficacy and safety concerns. Over the past decade, various emerging technologies have been used in the search for novel drug targets of SLE which have resulted in numerous promising data. However, the systematic review and careful digestion of this information have been lacking. Areas covered: In this review, the authors summarize promising biomarkers and drug targets which have been identified via various multiplexing and high-throughput proteomic strategies...
June 4, 2018: Expert Opinion on Drug Discovery
Ecaterina Ileana Dumbrava, Funda Meric-Bernstam, Timothy A Yap
No abstract text is available yet for this article.
May 24, 2018: Expert Opinion on Drug Discovery
Anna Wesołowska, Anna Partyka, Magdalena Jastrzębska-Więsek, Marcin Kołaczkowski
Cariprazine is approved in the United States and Europe for the treatment of manic or mixed episodes associated with bipolar I disorder and for the treatment of schizophrenia in adult patients. It is typically administered orally once a day (a dose range 1.5 - 6 mg/day), does require titration, and may be given with or without food. It has a half-life of 2 - 4 days with an active metabolite that has a terminal half-life of 2 - 3 weeks. Areas covered: This review article focuses on the preclinical discovery of cariprazine providing details regarding its pharmacological, behavioral, and neurochemical mechanisms and its contribution to clinical therapeutic benefits...
May 3, 2018: Expert Opinion on Drug Discovery
(no author information available yet)
No abstract text is available yet for this article.
July 2018: Expert Opinion on Drug Discovery
Keye Du, Jia Liu, Ruth Broering, Xiaoyong Zhang, Dongliang Yang, Ulf Dittmer, Mengji Lu
Toll-like receptor (TLR) ligands remain as promising antiviral drug candidates for the treatment of chronic viral infections. Basic research on the mechanisms of antiviral activity of TLR ligands in preclinical animal models and clinical testing of drug candidates have been carried out in recent years. Areas covered: This review provides an overview of the preclinical and clinical testing of TLR ligands in two major viral infections: hepatitis B virus (HBV) and human immunodeficiency virus (HIV). Recent results have further demonstrated the potent antiviral activity of various TLR ligands ...
July 2018: Expert Opinion on Drug Discovery
Wilian Augusto Cortopassi, Tanos Celmar Costa Franca, Antoniana Ursine Krettli
In spite of significant efforts to reduce malaria deaths, this disease still kills around 445,000 people every year. Overcoming drug resistance is one of the main goals of current malaria research programs. This is challenging, since the biology of Plasmodium is not fully understood, requiring the development of advanced models for data analysis in the search for new antimalarials. Areas covered: In this review the authors introduce the importance of computational models to address the challenges of drug discovery, presenting examples of pioneering systems biology approaches in the search for new antimalarial drugs and their role in the future of drug research programs...
July 2018: Expert Opinion on Drug Discovery
Dani Setiawan, Jeffrey Brender, Yang Zhang
Protein function is determined by protein structure which is in turn determined by the corresponding protein sequence. If the rules that cause a protein to adopt a particular structure are understood, it should be possible to refine or even redefine the function of a protein by working backwards from the desired structure to the sequence. Automated protein design attempts to calculate the effects of mutations computationally with the goal of more radical or complex transformations than are accessible by experimental techniques...
July 2018: Expert Opinion on Drug Discovery
Feng Li, Yongli Wang, Dapeng Li, Yilun Chen, Xuguang Qiao, Rania Fardous, Ashton Lewandowski, Jinbao Liu, Tak-Hang Chan, Q Ping Dou
Increasing evidence has expanded the role of green tea from a traditional beverage to a source of pharmacologically active molecules with diverse health benefits. However, conclusive clinical results are needed to better elucidate the cancer-preventive and therapeutic effects of green tea polyphenols (GTPs). Areas covered: The authors describe GTPs' chemical compositions and metabolic biotransformations, and their recent developments in drug discovery, focusing on their cancer chemopreventive and therapeutic effects...
July 2018: Expert Opinion on Drug Discovery
Sun-Hwa Lee, Kyoungho Suk
Despite the considerable social and economic burden on the healthcare system worldwide due to neurodegenerative diseases, there are currently few disease-altering treatment options for many of these conditions. Therefore, new approaches for both prevention and intervention for neurodegenerative diseases are urgently required. Microglia-mediated neurotoxicity is one of the pathologic hallmarks common to Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis. Current therapeutic approaches to target microglia-mediated neurotoxicity are focused on the identification of glia phenotype modulators (GPMs), which can inhibit the 'classical' pro-inflammatory and neurotoxic phenotypes of microglia...
July 2018: Expert Opinion on Drug Discovery
Erik Gawehn, Jan A Hiss, J B Brown, Gisbert Schneider
No abstract text is available yet for this article.
July 2018: Expert Opinion on Drug Discovery
Martin Vogt
Activity landscapes (ALs) are representations and models of compound data sets annotated with a target-specific activity. In contrast to quantitative structure-activity relationship (QSAR) models, ALs aim at characterizing structure-activity relationships (SARs) on a large-scale level encompassing all active compounds for specific targets. The popularity of AL modeling has grown substantially with the public availability of large activity-annotated compound data sets. AL modeling crucially depends on molecular representations and similarity metrics used to assess structural similarity...
July 2018: Expert Opinion on Drug Discovery
Bernard T Golding, Michael J Waring
No abstract text is available yet for this article.
July 2018: Expert Opinion on Drug Discovery
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