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Expert Opinion on Drug Discovery

Wenjing Lu, Roland J Pieters
Protein-carbohydrate interactions play a very important role in many biological processes. A single interaction between a protein and a carbohydrate is usually weak, but multivalent ligands can compensate for this deficiency by binding multiple binding sites to one biological entity simultaneously. Over the past few years, numerous efforts have been made for the design and synthesis of carbohydrate-based multivalent ligands thereby serving as potent inhibitors for pathogens such as the influenza A virus. Areas covered: In this review, the authors cover a variety of multivalent systems from small to large molecules which showed a potent inhibitory effect against several pathogens...
February 5, 2019: Expert Opinion on Drug Discovery
Anas Najjar, Rafik Karaman
Ample efforts have been carried out to improve the efficacy of a variety of drugs. The prodrugs approach was found to be a safe haven for providing medications with improved pharmacokinetic and pharmacodynamic properties. Areas covered: Herein, several selected successful prodrugs are reported and categorized. These include prodrugs for the treatment of the cardiovascular system, the central nervous system, the gastrointestinal tract, ophthalmology, the immune system, and oncology. In addition, some successful antiviral, antibacterial, antifungal, antiprotozoal, and several other miscellaneous prodrugs are documented...
February 4, 2019: Expert Opinion on Drug Discovery
Dirk M Hermann, Aurel Popa-Wagner, Christoph Kleinschnitz, Thorsten R Doeppner
Representing the leading cause of long-term disability, ischemic stroke urgently needs further research and drug development. This review summarizes current animal models of ischemic stroke that can be used for drug discovery. Areas covered: Several reproducible models of permanent and transient focal cerebral ischemia have been established in a variety of animal species including rats and mice, in which a brain-supplying artery, often the middle cerebral artery, is occluded by mechanical devices including sutures, clips and hooks, pharmacological agents or delivery of blot clots...
February 4, 2019: Expert Opinion on Drug Discovery
Vinaya Vijayan, Andrew D Rouillard, Deepak K Rajpal, Pankaj Agarwal
No abstract text is available yet for this article.
January 30, 2019: Expert Opinion on Drug Discovery
Michele Zanoni, Sara Pignatta, Chiara Arienti, Massimiliano Bonafè, Anna Tesei
Despite the increasing financial outlay on cancer research and drug discovery, many advanced cancers remain incurable. One possible strategy for increasing the approval rate of new anticancer drugs for use in clinical practice could be represented by three-dimensional (3D) tumor models on which to perform in vitro drug screening. There is a general consensus among the scientific community that 3D tumor models more closely recapitulate the complexity of tumor tissue architecture and biology than bi-dimensional cell cultures...
January 28, 2019: Expert Opinion on Drug Discovery
Emanuela Berrino, Claudiu T Supuran
In all living species, pH regulation is a tightly controlled process, with a plethora of proteins involved in its regulation. These include sodium-proton exchangers, carbonic anhydrases, anion exchangers, bicarbonate transporters/cotransporters, H+ -ATPases, and monocarboxylate transporters. All of them play crucial roles in acid-base balancing, both in eukaryotic as well as in prokaryotic organisms, making them interesting drug targets for the management of pathological events (in)directly involved in pH regulation...
January 25, 2019: Expert Opinion on Drug Discovery
Sina Azizi Machekposhti, Saeid Mohaved, Roger J Narayan
Inkjet-dispensing printing is a promising additive manufacturing method for pharmaceutical applications such as drug discovery. The unique advantages of this technology, including low cost, programmability, high resolution, high throughput, high speed, and biocompatibility, may reduce the financial resources needed to discover new drug candidates. Sophisticated and miniaturized assays have been developed to accomplish drug discovery and drug screening using modern inkjet dispensing printers. Areas covered: This paper reviews recent advancements in the field of inkjet printer technology for drug discovery...
January 24, 2019: Expert Opinion on Drug Discovery
Fabio Broccatelli, Marcel Hop, Matthew Wright
The PK optimization of drug candidates is one of the most resource-intensive tasks in pharmaceutical research and development. With the increasing availability of in silico, in vitro and mechanistic in vivo ADME models, drug discovery scientists have progressively learned to recognize common SAR patterns and engineer data-driven strategies to accelerate the resolution of ADME issues in lead optimization. Many of these strategies gravitate toward the concept of drug-likeness, which defines a number of optimal holistic physicochemical parameters (such as lipophilicity) that idealized oral drugs possess...
January 24, 2019: Expert Opinion on Drug Discovery
Katerina Papanikolopoulou, Amrit Mudher, Efthimios Skoulakis
Drosophila melanogaster offers a powerful expedient and economical system with facile genetics. Because of the high sequence and functional conservation with human disease-associated genes, it has been cardinal in deciphering disease mechanisms at the genetic and molecular level. Drosophila are amenable to and respond well to pharmaceutical treatment which coupled to their genetic tractability has led to discovery, repositioning, and validation of a number of compounds. Areas covered: This review summarizes the generation of fly models of human diseases, their advantages and use in elucidation of human disease mechanisms...
January 21, 2019: Expert Opinion on Drug Discovery
Savita Bisht, Georg Feldmann
Despite the introduction of novel therapeutic regimens for advanced stages of pancreatic cancer, long-term survival and overall outcome for patients are still very poor. Suitable small animal models are a prerequisite for better understanding of underlying pathophysiology and for translational studies designed to uncover novel therapeutic targets and to evaluate therapy regimens on a preclinical level. Areas covered: Genetically engineered mouse models as well as syngenic and xenotransplantation models are summarized and critically discussed with respect to their value for pancreatic cancer translational research...
January 18, 2019: Expert Opinion on Drug Discovery
Simona Lattanzi, Pasquale Striano
No abstract text is available yet for this article.
January 11, 2019: Expert Opinion on Drug Discovery
Ana Artero-Castro, Stepan Popelka, Pavla Jendelova, Jan Motlik, Taras Ardan, Francisco Javier Rodriguez Jimenez, Slaven Erceg
Combinatory strategies using pharmacology and stem cell therapy have emerged due to their potential in the treatment of retinal pigment epithelium (RPE) cell related diseases, and a variety of different stem cell sources have been evaluated both in animal models and in humans. RPE cells derived from human embryonic stem cells (hESCs) and human induced pluripotent cells (hiPSCs) are already in clinical trials, holding great promise for the treatment of age-related macular disease (AMD) and hereditary RPE-related retinal dystrophies...
January 8, 2019: Expert Opinion on Drug Discovery
Woo-Jin Shin, Baik L Seong
The emergence of drug-resistant influenza virus strains highlights the need for new antiviral therapeutics to combat future pandemic outbreaks as well as continuing seasonal cycles of influenza. Areas covered: This review summarizes the mechanisms of current FDA-approved anti-influenza drugs and patterns of resistance to those drugs. It also discusses potential novel targets for broad-spectrum antiviral drugs and recent progress in novel drug design to overcome drug resistance in influenza. Expert opinion: Using the available structural information about drug-binding pockets, research is currently underway to identify molecular interactions that can be exploited to generate new antiviral drugs...
December 26, 2018: Expert Opinion on Drug Discovery
Andrea K Pomerantz, Farid Sari-Sarraf, Kerri J Grove, Liliana Pedro, Patrick J Rudewicz, John W Fathman, Thomas Krucker
Single-cell imaging-based assays are an area of active and growing investment in drug discovery and development. This approach offers researchers the capability to interrogate rare subpopulations of cells with minimal sample consumption and multiplexed readouts. Recent technological advances in the optical interrogation and manipulation of single cells have substantially increased the throughput and sensitivity of these assays. Areas covered: In this review, the authors focus on three classes of single-cell imaging-based analyses: single-cell microscopy combined with microfluidics, mass spectrometric imaging for subcellular compound localization, and imaging mass cytometry (IMC)...
December 24, 2018: Expert Opinion on Drug Discovery
S A Usanov, A V Kliuchenovich, N V Strushkevich
Cushing's syndrome (CS) is a metabolic disorder caused by chronic hypercortisolism. CS is associated with cardiovascular, metabolic, skeletal and psychological dysfunctions and can be fatal if left untreated. The first-line treatment for all forms of CS is a surgery. However, medical therapy has to be chosen if surgical resection is not an option or is deemed ineffective. Currently available therapeutics are either not selective and have side effects or are only available as an injection (pasireotide). Areas covered: The authors discuss the recent drug developments for the medical treatment of CS through two validated molecular targets...
December 20, 2018: Expert Opinion on Drug Discovery
Jasmin C Haderspeck, Johanna Chuchuy, Stefan Kustermann, Stefan Liebau, Peter Loskill
Disorders of the eye that lead to visual impairment are affecting millions of people worldwide. Nevertheless, for many of these disorders, there are still no effective treatment options available due to the lack of in vitro model systems that emulate the physiological in vivo structure and function of human eyes. Microphysiological organ-on-a-chip (OoC) technology represents a novel and powerful approach to overcome the limitations of conventional model systems and lead to a paradigm shift in ophthalmic research...
December 8, 2018: Expert Opinion on Drug Discovery
Aline Silva de Miranda, Amanda Silva de Miranda, Antônio Lúcio Teixeira
Lamotrigine (LTG) is a well-established anticonvulsant that is also approved for the prevention of mood relapses in bipolar disorder. However, the mechanisms underlying LTG mood stabilizing effects remain unclear. Areas covered: Herein, the pre-clinical evidence concerning LTG's' mode of action in depression and mania is reviewed. Bottlenecks and future perspectives for this expanding and promising field are also discussed. Pre-clinical studies have indicated that neurotransmitter systems, especially serotoninergic, noradrenergic and glutamatergic, as well as non-neurotransmitter pathways such as inflammation and oxidative processes might play a role in LTG's antidepressant effects...
December 7, 2018: Expert Opinion on Drug Discovery
Zhi-Gang Sun, Yong-An Yang, Zhi-Gang Zhang, Hai-Liang Zhu
c-Met kinase plays an important part in the regulation of cell growth, invasion and anti-apoptosis. This enzyme is also an important target in cancer treatment. Through structural optimization and structure-activity studies of drugs currently on the market and those still in clinical trials, a great number of novel c-Met kinase inhibitors have been developed. This review focuses on recent developments in research regarding novel c-Met inhibitor synthesis, optimization, and structure-activity relationship (SAR) studies...
December 5, 2018: Expert Opinion on Drug Discovery
Anuradha Roy
No abstract text is available yet for this article.
December 4, 2018: Expert Opinion on Drug Discovery
Vinicius Gonçalves Maltarollo, Thales Kronenberger, Gabriel Zarzana Espinoza, Patricia Rufino Oliveira, Kathia Maria Honorio
Novel drug discovery remains an enormous challenge, with various computer-aided drug design (CADD) approaches having been widely employed for this purpose. CADD, specifically the commonly used support vector machines (SVMs), can employ machine learning techniques. SVMs and their variations offer numerous drug discovery applications, which range from the classification of substances (as active or inactive) to the construction of regression models and the ranking/virtual screening of databased compounds. Areas covered: Herein, the authors consider some of the applications of SVMs in medicinal chemistry, illustrating their main advantages and disadvantages, as well as trends in their utilization, via the available published literature...
November 29, 2018: Expert Opinion on Drug Discovery
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