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Expert Opinion on Drug Discovery

Mauro Giovanni Carta, Pasquale Paribello, Antonio Preti
No abstract text is available yet for this article.
September 17, 2018: Expert Opinion on Drug Discovery
Bence Szilágyi, György G Ferenczy, György M Keserű
Introduction D-amino acid oxidase (DAAO) degrades D-serine, a co-agonist of the NMDA receptor whose dysfunction is involved in the positive, negative and cognitive symptoms of schizophrenia. The inhibition of DAAO appears to be a viable strategy to increase D-serine level and to have therapeutic potential in schizophrenia. However, despite the intensive research in the field, a single clinical study was performed so far to evaluate the efficacy of a DAAO inhibitor, namely benzoate. Areas covered This review describes the efforts to develop DAAO inhibitors and to optimize their in vitro and in vivo effects in preclinical settings...
September 17, 2018: Expert Opinion on Drug Discovery
Heitor G Araújo-Filho, Erik W M Pereira, Adriana Rolim Campos, Lucindo J Quintans-Júnior, Jullyana S S Quintans
Chronic orofacial pain is one of the most common pain conditions experienced by adults. Animal models are often selected as the most useful scientific methodology to explore the pathophysiology of the disorders that cause this disabling pain to facilitate the development of new treatments. The creation of new models or the improvement of existing ones is essential for finding new ways to approach the complex neurobiology of this type of pain. Areas covered: The authors describe and discuss a variety of animal models used in chronic orofacial pain (COFP)...
September 17, 2018: Expert Opinion on Drug Discovery
Fisayo Olotu, Emmanuel Adeniji, Clement Agoni, Imane Bjiji, Shama Khan, Ahmed Elrashedy, Mahmoud Soliman
Over the years, not a single HSP inhibitor has progressed into the post-market phase of drug development despite the success recorded in various pre-clinical and clinical studies. The inability of existing drugs to specifically target oncogenic HSPs has majorly accounted for these setbacks. Recent combinatorial strategies that incorporated computer-aided drug design (CADD) techniques are geared towards the development of highly specific HSP inhibitors with increased activities and minimal toxicities. Areas covered: In this review, strategic therapeutic approaches that have recently aided the development of selective HSP inhibitors were highlighted...
September 12, 2018: Expert Opinion on Drug Discovery
Paula Blanco, Fernando Sanz-García, Sara Hernando-Amado, José Luis Martínez, Manuel Alcalde-Rico
One of the possibilities for reducing the emergence and spread of antibiotic resistance is the use of anti-resistance compounds capable of resensitizing resistant microorganisms to current antimicrobials. For this purpose, multidrug efflux pumps, whose inhibition may increase bacterial susceptibility to several antibiotics, including macrolides to which Gram-negatives are considered intrinsically resistant, have emerged as suitable targets. Areas covered: In the current review, the authors discuss different mechanisms that can be exploited for inhibiting multidrug efflux pumps and describe the properties and the potential therapeutic value of already studied efflux pumps inhibitors...
September 10, 2018: Expert Opinion on Drug Discovery
Joseph V Pergolizzi, Jo Ann LeQuang, Robert Taylor, Michael H Ossipov, Daniel Colucci, Robert B Raffa
The recent dramatic increase in intentional and unintentional deaths attributed to opioids has refocused attention on the therapeutic ratio (risk-benefit ratio) of opioid analgesics. Almost all traditional opioid analgesics produce their effects (therapeutic and adverse) via the activation of μ-opioid receptor (MOR) pathways. It is therefore important to examine the question of whether this natural endogenous pathway can still be activated, but with greater safety. Areas covered: Other comprehensive reviews have focused on pharmacokinetic (e...
September 3, 2018: Expert Opinion on Drug Discovery
Mathew Renwick, Elias Mossialos
No abstract text is available yet for this article.
September 1, 2018: Expert Opinion on Drug Discovery
Anthony Travis, Olga Chernova, Vladislav Chernov, Rustam Aminov
No abstract text is available yet for this article.
August 29, 2018: Expert Opinion on Drug Discovery
Ashok Vaidya, Anuradha Roy, Rathnam Chaguturu
No abstract text is available yet for this article.
August 27, 2018: Expert Opinion on Drug Discovery
Ewout J N Groen
No abstract text is available yet for this article.
August 27, 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
Alessandro Sinigaglia, Silvia Riccetti, Marta Trevisan, Luisa Barzon
After the WHO declared Zika virus (ZIKV) as a public health emergency of international concern, intense research for the development of vaccines and drugs has been undertaken, leading to the development of several candidates. Areas covered: This review discusses the developments achieved so far by computational methods in the discovery of candidate compounds targeting ZIKV proteins, i.e. the envelope and capsid structural proteins, the NS3 helicase/protease, and the NS5 methyltransferase/RNA-dependent RNA polymerase...
September 2018: Expert Opinion on Drug Discovery
Dinesh Aggarwal, Nikita Arumalla, Hannah Jethwa, Sonya Abraham
Psoriatic disease is a relatively new term which encompasses psoriatic arthritis, psoriasis, and associated comorbidities. In this heterogeneous condition, the study of biomarkers is necessary to direct best therapy. Resulting in significant disability and socioeconomic burden, recent recommendations stress the need for tight control in psoriatic disease. Areas covered: The authors outline recent advances in the understanding of psoriatic disease pathogenesis which has highlighted multiple biomarkers that have been pursued as drug targets with varying degrees of success...
September 2018: Expert Opinion on Drug Discovery
Xin-Yu Zhang, Adnan A Elfarra
6-Mercaptopurine (6-MP) and 6-thioguanine (6-TG), two anticancer drugs, have high systemic toxicity due to a lack of target specificity. Therefore, increasing target selectivity should improve drug safety. Areas covered: The authors examined the hypothesis that new prodrug designs based upon mechanisms of kidney-selective toxicity of trichloroethylene would reduce systemic toxicity and improve selectivity to kidney and tumor cells. Two approaches specifically were investigated. The first approach was based upon bioactivation of trichloroethylene-cysteine S-conjugate by renal cysteine S-conjugate β-lyases...
September 2018: Expert Opinion on Drug Discovery
Ilya Blokhin, Olga Khorkova, Jane Hsiao, Claes Wahlestedt
The central dogma of molecular biology, which states that the only role of long RNA transcripts is to convey information from gene to protein, was brought into question in recent years due to discovery of the extensive presence and complex roles of long noncoding RNAs (lncRNAs). Furthermore, lncRNAs were found to be involved in pathogenesis of multiple diseases and thus represent a new class of therapeutic targets. Translational efforts in the lncRNA field have been augmented by progress in optimizing the chemistry and delivery platforms of lncRNA-targeting modalities, including oligonucleotide-based drugs and CRISPR-Cas9...
September 2018: Expert Opinion on Drug Discovery
Romain Yvinec, Pascale Crépieux, Eric Reiter, Anne Poupon, Frédérique Clément
Pituitary gonadotropins play an essential and pivotal role in the control of human and animal reproduction within the hypothalamic-pituitary-gonadal (HPG) axis. The computational modeling of pituitary gonadotropin signaling encompasses phenomena of different natures such as the dynamic encoding of gonadotropin secretion, and the intracellular cascades triggered by gonadotropin binding to their cognate receptors, resulting in a variety of biological outcomes. Areas covered: The authors provide an overview of the historical and ongoing issues in modeling and data analysis related to gonadotropin secretion in the field of both physiology and neuroendocrinology...
September 2018: Expert Opinion on Drug Discovery
Theodora Katsila, Minos-Timotheos Matsoukas
No abstract text is available yet for this article.
September 2018: 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...
September 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...
September 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.
September 2018: Expert Opinion on Drug Discovery
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