1,357 results match your criteria Expert Opinion on Drug Discovery[Journal]


Exploitation of the Ugi-Joullié reaction in drug discovery and development.

Expert Opin Drug Discov 2019 Apr 19:1-14. Epub 2019 Apr 19.

a Dipartimento di Chimica , Università degli Studi di Milano , Milano , Italy.

Introduction: Multicomponent reactions are paramount in drug discovery for their ability to achieve high levels of diversity within the chemical space, generating complex structures from simple building blocks. Among them, the isocyanide-based Ugi-Joulliè reaction is particularly suited for the rapid synthesis of peptidomimetics and nitrogen-containing compounds. Areas covered: The latest achievements in drug discovery and synthetic chemistry regarding the application of the Ugi-Joulliè reaction in the field of natural compounds, peptidomimetics and small molecules, are reported in this article. Read More

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http://dx.doi.org/10.1080/17460441.2019.1604676DOI Listing

Developing animal models of Zika virus infection for novel drug discovery.

Expert Opin Drug Discov 2019 Apr 16:1-13. Epub 2019 Apr 16.

a Department of Microbiology, Institute of Biomedical Sciences , University of São Paulo , São Paulo , Brazil.

Introduction: Just before the Brazilian outbreak, Zika virus was related to a mild infection, causing fever and skin rash. Congenital Zika Syndrome was first described in Brazil, causing microcephaly and malformations in newborns. Three years after the outbreak, the mechanisms of Zika pathogenesis are still not completely elucidated. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1597050DOI Listing
April 2019
2 Reads

Have marine natural product drug discovery efforts been productive and how can we improve their efficiency?

Authors:
Florbela Pereira

Expert Opin Drug Discov 2019 Apr 15:1-6. Epub 2019 Apr 15.

a LAQV and REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia , Universidade Nova de Lisboa , Caparica , Portugal.

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http://dx.doi.org/10.1080/17460441.2019.1604675DOI Listing

Drugs that target aging: how do we discover them?

Authors:
A Myers G J Lithgow

Expert Opin Drug Discov 2019 Apr 11:1-8. Epub 2019 Apr 11.

a Buck Institute for Research on Aging , Novato , CA , USA.

Introduction: Biology of aging is focused on elucidating the biochemical and genetic pathways that contribute to cellular damage accumulation over time. Thirty years of research are beginning to bear fruit as the first pharmacological interventions based on biology of aging go through clinical trials. Evolutionary theories of aging suggest that naturally selected traits believed to impart fitness in young organisms may be damaging in later life. Read More

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http://dx.doi.org/10.1080/17460441.2019.1597049DOI Listing
April 2019
2 Reads

The discovery and development of inhaled therapeutics for migraine.

Expert Opin Drug Discov 2019 Mar 29:1-9. Epub 2019 Mar 29.

a Headache Group, Department of Basic and Clinical Neuroscience , King's College London , London , UK.

Introduction: Migraine is a disabling primary headache disorder that requires effective treatments. Inhalation is currently being explored for the delivery of drugs for migraine. Pulmonary-route delivery of drugs shows potential advantages for its use as a treatment, particularly compared the oral route. Read More

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http://dx.doi.org/10.1080/17460441.2019.1598373DOI Listing
March 2019
1 Read

How can we develop better antispasmodics for irritable bowel syndrome?

Expert Opin Drug Discov 2019 Mar 28:1-14. Epub 2019 Mar 28.

d Department of Toxicology and Pharmacology, Faculty of Pharmacy , Tehran University of Medical Sciences , Tehran , Iran.

Introduction: Irritable bowel syndrome (IBS) is a prevalent gastrointestinal (GI) disease. Antispasmodics are a heterogeneous group of drugs that tackle IBS-associated altered bowel habit and abdominal pain. However, some studies have shown their failure to exhibit benefit over placebo. Read More

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http://dx.doi.org/10.1080/17460441.2019.1593369DOI Listing
March 2019
2 Reads

GABA(A) receptor-targeted drug development -New perspectives in perioperative anesthesia.

Expert Opin Drug Discov 2019 Mar 26:1-17. Epub 2019 Mar 26.

c University Hospital rechts der Isar , Department of Anesthesiology , München , Germany.

Introduction: Perioperative anesthesia delivers pre-, intra-, and postoperative care to meet the needs of patients undergoing diagnostic and surgical procedures. Major challenges are patients at the extremes of age and individuals with a pre-existing disease burden. Frequent problems are the development of chronic pain and cognitive dysfunction upon surgery. Read More

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http://dx.doi.org/10.1080/17460441.2019.1599356DOI Listing
March 2019
1 Read

Are academic drug discovery efforts receiving more recognition with declining industry efficiency?

Expert Opin Drug Discov 2019 Mar 25:1-3. Epub 2019 Mar 25.

b Faculty of Medicine , National Heart & Lung Institute, Imperial College , London , UK.

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http://dx.doi.org/10.1080/17460441.2019.1596080DOI Listing
March 2019
5 Reads

Discovery of natural products with metal-binding properties as promising antibacterial agents.

Expert Opin Drug Discov 2019 Mar 25:1-14. Epub 2019 Mar 25.

c Organic Chemistry Laboratory , University of Bayreuth , Bayreuth , Germany.

Introduction: More than 50% of the clinically established antibiotics are either genuine natural products or derivatives thereof, featuring a mode of action decisively depending on their metal affinity and suitability as metal complex ligands. As their structural diversity and harvest from renewable sources is well-nigh inexhaustible, any future quest for affordable new antibiotics will have to concentrate on natural drugs with obvious metal ligating properties. Areas covered: The authors provide an overview of the promising developments in the field of antibiotic natural products with metal-binding properties with a specific focus on metal binders such as polyphenols, quinones, 3-acyltetramic and -tetronic acids. Read More

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http://dx.doi.org/10.1080/17460441.2019.1593367DOI Listing
March 2019
5 Reads

The impact of decreasing biodiversity on novel drug discovery: is there a serious cause for concern?

Authors:
David J Newman

Expert Opin Drug Discov 2019 Mar 22:1-5. Epub 2019 Mar 22.

a Newman Consulting LLC , Wayne , PA , USA.

Introduction: The aim of this perspective is to discuss the current and potential situation concerning the loss of biodiversity and its current and potential effects upon the search for novel bioactive agents from natural sources, be they from marine, microbial or terrestrial environments. Areas covered: Herein, the author covers terrestrial plants, marine organisms (but not vertebrates), and unicellular microbes from both terrestrial and marine sources. The emphasis is on the unknown effects of biodiversity perturbation and/or loss of microbes that are now realized to underlie the production of a significant number of natural products, whether they were first found in plants or marine invertebrates. Read More

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http://dx.doi.org/10.1080/17460441.2019.1593370DOI Listing

Animal models for Niemann-Pick type C: implications for drug discovery & development.

Expert Opin Drug Discov 2019 May 19;14(5):499-509. Epub 2019 Mar 19.

a Orphazyme A/S , Copenhagen , Denmark.

Introduction: Niemann-Pick type C (NPC) is a neurovisceral, progressively detrimental lysosomal storage disease with very limited therapeutic options and no approved treatment available in the US. Despite its rarity, NPC has seen increased drug developmental efforts over the past decade, culminating in the completion of two potential registration trials in 2018. Areas covered: This review highlights the many available animal models that have been developed in the field and briefly covers classical and new cell technologies. Read More

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http://dx.doi.org/10.1080/17460441.2019.1588882DOI Listing
May 2019
1 Read

A new wave of innovation in Semantic web tools for drug discovery.

Expert Opin Drug Discov 2019 May 19;14(5):433-444. Epub 2019 Mar 19.

a Department of Chemistry , Highfield Campus, University of Southampton , Southampton , UK.

Introduction: The use of semantic web technologies to aid drug discovery has gained momentum over recent years. Researchers in this domain have realized that semantic web technologies are key to dealing with the high levels of data for drug discovery. These technologies enable us to represent the data in a formal, structured, interoperable and comparable way, and to tease out undiscovered links between drug data (be it identifying new drug-targets or relevant compounds, or links between specific drugs and diseases). Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1586880DOI Listing
May 2019
4 Reads

Omics of antimicrobials and antimicrobial resistance.

Expert Opin Drug Discov 2019 May 19;14(5):455-468. Epub 2019 Mar 19.

b Institute of Fundamental Medicine and Biology , Kazan (Volga region) Federal University , Kazan , Russian Federation.

Introduction: The development of new antimicrobials has become an urgent priority because of a global challenge emerging from the rise of antimicrobial resistant pathogens. Areas covered: In this review, the authors discuss the opportunities offered by modern omics approaches to address the challenge and the use of this approach in antimicrobial development. Specifically, the authors focus on the role of omics technologies and bioinformatics for the revelation of the effects of antimicrobials in a variety of microbial cellular processes, as well as the identification of potential cellular targets, the mechanisms of antimicrobial resistance, and the development of new antimicrobials. Read More

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http://dx.doi.org/10.1080/17460441.2019.1588880DOI Listing

Duality of activity cliffs in drug discovery.

Authors:
Jürgen Bajorath

Expert Opin Drug Discov 2019 Mar 18:1-4. Epub 2019 Mar 18.

a Department of Life Science Informatics, B-IT, LIMES Program Unit Chemical Biology and Medicinal Chemistry , Rheinische Friedrich-Wilhelms-Universität , Bonn , Germany.

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http://dx.doi.org/10.1080/17460441.2019.1593371DOI Listing

The problem of racemization in drug discovery and tools to predict it.

Expert Opin Drug Discov 2019 Mar 18:1-13. Epub 2019 Mar 18.

a Physical Organic Chemistry Centre , School of Chemistry, Cardiff University , Cardiff , UK.

Introduction: Racemization has long been an ignored risk in drug development, probably because of a lack of convenient access to good tools for its detection and an absence of methods to predict racemization risk. As a result, the potential effects of racemization have been systematically underestimated. Areas covered: Herein, the potential effects of racemization are discussed through a review of drugs for which activity and side effects for both enantiomers are known. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1588881DOI Listing
March 2019
2 Reads

Is one-shot learning a viable option in drug discovery?

Authors:
Igor I Baskin

Expert Opin Drug Discov 2019 Mar 18:1-3. Epub 2019 Mar 18.

a Faculty of Physics , M.V. Lomonosov Moscow State University , Moscow , Russia.

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1593368DOI Listing
March 2019
3 Reads

Are animal models a necessity for acute radiation syndrome drug discovery?

Expert Opin Drug Discov 2019 Mar 14:1-5. Epub 2019 Mar 14.

a Department Radiation Oncology , University of California at Los Angeles , Los Angeles , CA , USA.

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http://dx.doi.org/10.1080/17460441.2019.1591364DOI Listing
March 2019
3 Reads

The discovery and development of topical medicines for wound healing.

Expert Opin Drug Discov 2019 May 14;14(5):485-497. Epub 2019 Mar 14.

a Department of Medical Cell Biology , Uppsala University , Uppsala , Sweden.

Introduction: Chronic, nonhealing skin wounds claim >3% of the health-care budget in industrialized countries, and the incidence is rising. Currently, two parallel trends influence innovations within the field of wound healing: the need to reduce spread of antibiotic resistance and the emerging use of health economy and value-based models. Areas covered: This review focuses on the discovery of drug candidates and development of treatments aiming to enhance wound healing in the heterogeneous group of patients with nonhealing wounds. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1588879DOI Listing
May 2019
9 Reads

Modeling heart failure in animal models for novel drug discovery and development.

Expert Opin Drug Discov 2019 Apr 12;14(4):355-363. Epub 2019 Mar 12.

a Department of Physiology and Cell Biology , The Ohio State University Wexner Medical Center , Columbus, OH, USA.

Introduction: When investigating drugs that treat heart diseases, it is critical when choosing an animal model for the said model to produce data that is translatable to the human patient population, while keeping in mind the principles of reduction, refinement, and replacement of the animal model in the research. Areas covered: In this review, the authors focus on mammalian models developed to study the impact of drug treatments on human heart failure. Furthermore, the authors address human patient variability and animal model invariability as well as the considerations that need to be made regarding choice of species. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1582636DOI Listing
April 2019
4 Reads

Binding site comparisons for target-centered drug discovery.

Authors:
Janez Konc

Expert Opin Drug Discov 2019 May 11;14(5):445-454. Epub 2019 Mar 11.

a Theory Department , National Institute of Chemistry , Ljubljana , Slovenia.

Introduction: The success of binding site comparisons in drug discovery is based on the recognized fact that many different proteins have similar binding sites. Indeed, binding site comparisons have found many uses in drug development and have the potential to dramatically cut the cost and shorten the time necessary for the development of new drugs. Areas covered: The authors review recent methods for comparing protein binding sites and their use in drug repurposing and polypharmacology. Read More

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http://dx.doi.org/10.1080/17460441.2019.1588883DOI Listing

Broad-spectrum coronavirus antiviral drug discovery.

Expert Opin Drug Discov 2019 Apr 8;14(4):397-412. Epub 2019 Mar 8.

a Division of Molecular and Translational Sciences , United States Army Medical Research Institute of Infectious Diseases , Fort Detrick , MD , USA.

Introduction: The highly pathogenic coronaviruses severe acute respiratory syndrome coronavirus (SARS-CoV) and Middle East respiratory syndrome coronavirus (MERS-CoV) are lethal zoonotic viruses that have emerged into human populations these past 15 years. These coronaviruses are associated with novel respiratory syndromes that spread from person-to-person via close contact, resulting in high morbidity and mortality caused by the progression to Acute Respiratory Distress Syndrome (ARDS). Areas covered: The risks of re-emergence of SARS-CoV from bat reservoir hosts, the persistence of MERS-CoV circulation, and the potential for future emergence of novel coronaviruses indicate antiviral drug discovery will require activity against multiple coronaviruses. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1581171DOI Listing
April 2019
5 Reads

Screening drugs for myocardial disease in vivo with zebrafish: an expert update.

Expert Opin Drug Discov 2019 Apr 6;14(4):343-353. Epub 2019 Mar 6.

c Cardiovascular Medicine , Brigham and Women's Hospital, Harvard Medical School , Boston , MA , USA.

Introduction: Our understanding of the complexity of cardiovascular disease pathophysiology remains very incomplete and has hampered cardiovascular drug development over recent decades. The prevalence of cardiovascular diseases and their increasing global burden call for novel strategies to address disease biology and drug discovery. Areas covered: This review describes the recent history of cardiovascular drug discovery using in vivo phenotype-based screening in zebrafish. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1577815DOI Listing
April 2019
6 Reads

Using miniature brain implants in rodents for novel drug discovery.

Authors:
Ben Waldau

Expert Opin Drug Discov 2019 Apr 4;14(4):379-386. Epub 2019 Mar 4.

a Department of Neurological Surgery , University of California, Davis Medical Center , Sacramento , CA , USA.

Introduction: There continues to be a need to create an artificial human blood-brain barrier for pharmacological testing and modeling of diseases. Our group has recently vascularized human brain organoids with human iPSC-derived endothelial cells. Other groups have achieved brain organoid perfusion after vascularization with murine endothelial cells. Read More

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http://dx.doi.org/10.1080/17460441.2019.1577816DOI Listing
April 2019
4 Reads

Exciting advances in GPCR-based drugs discovery for treating metabolic disease and future perspectives.

Expert Opin Drug Discov 2019 May 1;14(5):421-431. Epub 2019 Mar 1.

d Neurotransmission et signalisation laboratoire , Inserm UMR-S 839 , Paris , France.

Introduction: Current pharmacological therapies that target single receptors have limited efficacy for the treatment of diabetes and obesity. Novel approaches with hybrid peptides that activate more than one receptor at once to generate beneficial effects through synergistic effects have shown promising results. Several unimolecular dual and tri-agonists, mainly associated with GPCR like GLP-1/GCG/GIP receptors, have shown exceptional efficacy in preclinical models, and are currently being evaluated in clinical trials to investigate their safety and beneficial effects in humans. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1583642DOI Listing
May 2019
8 Reads

Liquid chromatography coupled to mass spectrometry for metabolite profiling in the field of drug discovery.

Expert Opin Drug Discov 2019 May 27;14(5):469-483. Epub 2019 Feb 27.

a Department of Chemical Engineering and Analytical Chemistry , University of Barcelona , Barcelona , Spain.

Introduction: The identification and characterization of the metabolites during the early stages of discovery and development of new drug candidates are essential to establish the metabolic clearance as well as the potential pharmacological and/or toxicological effects. Hence, feasible methods of analysis, preferably rapid and simple, are required to satisfy the increasing demand of metabolite profiling studies. Areas covered: This paper reviews the topic of metabolite profiling in drug discovery based on liquid chromatography, with especial emphasis on chromatographic modes and detectors. Read More

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http://dx.doi.org/10.1080/17460441.2019.1582638DOI Listing
May 2019
1 Read

Are we seeing a resurgence in the use of natural products for new drug discovery?

Expert Opin Drug Discov 2019 May 27;14(5):417-420. Epub 2019 Feb 27.

b Barbara Ann Karmanos Cancer Institute, Departments of Oncology, Pharmacology and Pathology , Wayne State University School of Medicine , Detroit , MI , USA.

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http://dx.doi.org/10.1080/17460441.2019.1582639DOI Listing
May 2019
3 Reads
3.467 Impact Factor

DataWarrior: an evaluation of the open-source drug discovery tool.

Expert Opin Drug Discov 2019 Apr 26;14(4):335-341. Epub 2019 Feb 26.

a Department of Pharmacy, School of Chemistry , National Autonomous University of Mexico , Mexico City , Mexico.

Introduction: DataWarrior is open and interactive software for data analysis and visualization that integrates well-established and novel chemoinformatics algorithms in a single environment. Since its public release in 2014, DataWarrior has been used by research groups in universities, government, and industry. Areas covered: Herein, the authors discuss, in a critical manner, the tools and distinct technical features of DataWarrior and analyze the areas of opportunity. Read More

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http://dx.doi.org/10.1080/17460441.2019.1581170DOI Listing
April 2019
1 Read

A bright future for fragment-based drug discovery: what does it hold?

Expert Opin Drug Discov 2019 May 22;14(5):413-416. Epub 2019 Feb 22.

a Laboratoire d'innovation thérapeutique , UMR7200 CNRS Université de Strasbourg , Illkirch , France.

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http://dx.doi.org/10.1080/17460441.2019.1583643DOI Listing
May 2019
1 Read

How to utilize academic research efforts in cancer drug discovery.

Authors:
Gervais Bérubé

Expert Opin Drug Discov 2019 Apr 20;14(4):331-334. Epub 2019 Feb 20.

a Département de Chimie, Biochimie et Physique , Université du Québec à Trois-Rivières , Trois-Rivières , QC , Canada.

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http://dx.doi.org/10.1080/17460441.2019.1582637DOI Listing
April 2019
7 Reads

Why have transgenic rodent models failed to successfully mimic Alzheimer's disease. How can we develop effective drugs without them?

Expert Opin Drug Discov 2019 Apr 18;14(4):327-330. Epub 2019 Feb 18.

b CiberNed: Centro de Investigación en Red, enfermedades Neurodegenerativas , Instituto de Salud Carlos III , Madrid , Spain.

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http://dx.doi.org/10.1080/17460441.2019.1581169DOI Listing

Recent developments in biological aspects of chalcones: the odyssey continues.

Expert Opin Drug Discov 2019 Mar;14(3):249-288

a Department of Chemistry , Guru Nanak Dev University , Amritsar , India.

Introduction: Chalcones are attractive to synthetic chemists because they are easy to prepare, have a large number of replaceable hydrogens, thereby having significant biological potential. Chalcones and their derivatives (carbocyclic as well as heterocyclic) exhibit a range of biological properties including anticancer, antimalarial, antioxidant, anti-inflammatory and anti-tubercular activities. Their promising biological profile, along with their ease of synthetic manipulations, have triggered the design and development of new chalcone derivatives as well as their conjugates with active pharmacophores affording therapeutic templates targeting various diseases. Read More

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http://dx.doi.org/10.1080/17460441.2019.1573812DOI Listing

Carbohydrate-protein interactions and multivalency: implications for the inhibition of influenza A virus infections.

Expert Opin Drug Discov 2019 Apr 5;14(4):387-395. Epub 2019 Feb 5.

a Department of Chemical Biology & Drug Discovery , Utrecht Institute for Pharmaceutical Sciences, Utrecht University , Utrecht , The Netherlands.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1573813DOI Listing

Successes, failures, and future prospects of prodrugs and their clinical impact.

Expert Opin Drug Discov 2019 Mar 4;14(3):199-220. Epub 2019 Feb 4.

a Department of Bioorganic & Pharmaceutical Chemistry, Faculty of Pharmacy , Al-Quds University , Jerusalem , Palestine.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1567487DOI Listing
March 2019
6 Reads
3.467 Impact Factor

Animal models of ischemic stroke and their impact on drug discovery.

Expert Opin Drug Discov 2019 Mar 4;14(3):315-326. Epub 2019 Feb 4.

c Department of Neurology , University Medicine Göttingen , Göttingen , Germany.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1573984DOI Listing
March 2019
8 Reads

Could advances in representation learning in Artificial Intelligence provide the new paradigm for data integration in drug discovery?

Expert Opin Drug Discov 2019 Mar 30;14(3):191-194. Epub 2019 Jan 30.

a Computational Biology , GlaxoSmithKline R&D , Collegeville , PA , USA.

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http://dx.doi.org/10.1080/17460441.2019.1573811DOI Listing
March 2019
10 Reads

Anticancer drug discovery using multicellular tumor spheroid models.

Expert Opin Drug Discov 2019 Mar 28;14(3):289-301. Epub 2019 Jan 28.

a Biosciences Laboratory , Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (IRST) IRCCS , Meldola , Italy.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1570129DOI Listing
March 2019
5 Reads

Novel approaches for designing drugs that interfere with pH regulation.

Expert Opin Drug Discov 2019 Mar 25;14(3):231-248. Epub 2019 Jan 25.

a NEUROFARBA Department, Sezione di Scienze Farmaceutiche , University of Florence , Sesto Fiorentino (Florence) , Italy.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1567488DOI Listing
March 2019
6 Reads

Inkjet dispensing technologies: recent advances for novel drug discovery.

Expert Opin Drug Discov 2019 Feb 24;14(2):101-113. Epub 2019 Jan 24.

b Joint Department of Biomedical Engineering , University of North Carolina and North Carolina State University , Raleigh , NC , USA.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1567489DOI Listing
February 2019
2 Reads

Strategies to optimize drug half-life in lead candidate identification.

Expert Opin Drug Discov 2019 Mar 24;14(3):221-230. Epub 2019 Jan 24.

a Department of Drug Metabolism and Pharmacokinetics , Genentech , South San Francisco , CA , USA.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1569625DOI Listing
March 2019
3 Reads

An assessment of the translational relevance of Drosophila in drug discovery.

Expert Opin Drug Discov 2019 Mar 21;14(3):303-313. Epub 2019 Jan 21.

a Division of Neuroscience , Biomedical Sciences Research Centre "Alexander Fleming" , Vari , Greece.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1569624DOI Listing
March 2019
2 Reads

Animal models for modeling pancreatic cancer and novel drug discovery.

Expert Opin Drug Discov 2019 Feb 18;14(2):127-142. Epub 2019 Jan 18.

a Department of Internal Medicine 3 , University Hospital of Bonn , Bonn , Germany.

Introduction: 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. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1566319DOI Listing
February 2019
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The impact of perampanel and targeting AMPA transmission on anti-seizure drug discovery.

Expert Opin Drug Discov 2019 Mar 11;14(3):195-197. Epub 2019 Jan 11.

b Pediatric Neurology and Muscular Diseases Unit, Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health , University of Genoa, "G. Gaslini" Institute , Genova , Italy.

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http://dx.doi.org/10.1080/17460441.2019.1566318DOI Listing
March 2019
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The identification of small molecules that stimulate retinal pigment epithelial cells: potential novel therapeutic options for treating retinopathies.

Expert Opin Drug Discov 2019 Feb 8;14(2):169-177. Epub 2019 Jan 8.

a Stem Cell Therapies in Neurodegenerative Diseases Lab , Research Center "Principe Felipe" , Valencia , Spain.

Introduction: 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. Highly efficient protocol for RPE generations have been developed, but they are still time-consuming and laborious. Read More

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http://dx.doi.org/10.1080/17460441.2019.1559148DOI Listing
February 2019
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Novel antiviral drug discovery strategies to tackle drug-resistant mutants of influenza virus strains.

Expert Opin Drug Discov 2019 Feb 26;14(2):153-168. Epub 2018 Dec 26.

b Department of Biotechnology , College of Life Science and Biotechnology, Yonsei University , Seoul , South Korea.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1560261DOI Listing
February 2019
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Enabling drug discovery and development through single-cell imaging.

Expert Opin Drug Discov 2019 Feb 24;14(2):115-125. Epub 2018 Dec 24.

d Alliance Management and Partnering , Novartis Institutes for BioMedical Research Inc ., Emeryville , CA , USA.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1559147DOI Listing
February 2019
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Drug design strategies for Cushing's syndrome.

Expert Opin Drug Discov 2019 Feb 20;14(2):143-151. Epub 2018 Dec 20.

a Institute of Bioorganic Chemistry of the National Academy of Science of Belarus , Minsk , Republic of Belarus.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1559146DOI Listing
February 2019
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Lamotrigine as a mood stabilizer: insights from the pre-clinical evidence.

Expert Opin Drug Discov 2019 Feb 7;14(2):179-190. Epub 2018 Dec 7.

a Laboratório Interdisciplinar de Investigação Médica, Faculdade de Medicina , Universidade Federal de Minas Gerais , Belo Horizonte , Brazil.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1553951DOI Listing
February 2019
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Organ-on-a-chip technologies that can transform ophthalmic drug discovery and disease modeling.

Expert Opin Drug Discov 2019 Jan 8;14(1):47-57. Epub 2018 Dec 8.

b Department of Women's Health, Research Institute for Women's Health , Eberhard Karls University Tübingen , Tübingen , Germany.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1551873DOI Listing
January 2019
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Optimization techniques for novel c-Met kinase inhibitors.

Expert Opin Drug Discov 2019 Jan 5;14(1):59-69. Epub 2018 Dec 5.

b State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences , Nanjing University , Nanjing , China.

Introduction: 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. Read More

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http://dx.doi.org/10.1080/17460441.2019.1551355DOI Listing
January 2019
2 Reads