Showing papers in "Drug Discovery Today in 2016"

TL;DR: In recent years, the declining focus on natural products has impacted the pipeline of NMEs from specific classes, and this trend is likely to continue without specific investment in the pursuit of natural products.

TL;DR: Advances in tissue engineering and microfabrication technologies have enabled rapid growth in the areas of in vitro organoid development as well as organoid-on-a-chip platforms and their applications, which have the potential to dramatically impact biomedical applications in the area of drug development, drug and toxicology screening, disease modeling, and the emerging area of personalized precision medicine.

TL;DR: Assessment of SMKI properties, target selectivity and mechanism of function, and therapeutic indications of these approved inhibitors showed that >30% of approved SMKIs have a molecule weight exceeding 500 and all have a total ring count of between three and five.

TL;DR: Metal-organic frameworks are porous, hybrid materials comprising metal ions linked by organic binding ligands that can act as a reservoir of metal ions, providing their gradual release and resulting in a sustained antibacterial action analogous to that proposed for metal/metal oxide nanoparticles but different to that of antibiotics.

TL;DR: How Nbs are being explored as therapeutics in many fields of medicine, including oncology, inflammatory, infectious and neurological diseases, and imaging, is discussed and their potential for use in the diagnosis and monitoring of diseases is highlighted.

TL;DR: Generally, injectable hydrogel-based drug delivery systems are found to be more efficacious than the conventional systemic chemotherapy in terms of cancer treatment.

TL;DR: Drug combinations of two or more compounds with different mechanisms of action are an alternative approach to increase the success rate of drug repositioning.

TL;DR: The physical chemical properties of various cyclodextrins are discussed, including the effects of substitutions on these properties, as well as the regulatory status of their use, commercial products containing cyclodeXTrins, toxicological considerations, and the forces involved in complex formation.

TL;DR: This Keynote review presents the bioprinting technology and covers a first-time comprehensive overview of its application areas from tissue engineering and regenerative medicine to pharmaceutics and cancer research.

TL;DR: The molecular mechanisms underlying the neuroprotective effects of GLP-1 analogues in the laboratory and their potential therapeutic utility with particular relevance to PD and PD dementia (PDD) are reviewed.

TL;DR: This review introduces cubosomes focusing on their structure, preparation methods, mechanism of release and potential routes of administration.

TL;DR: The cellular mechanisms underlying the rapid antidepressant actions of ketamine and related agents are discussed, as well as novel, selective glutamatergic receptor targets that are safer and have fewer side effects.

TL;DR: A brief explanation of descriptors and the selection approaches most commonly used in QSAR experiments is provided, and some studies have also demonstrated the positive influence of features selection for any drug development model.

TL;DR: This paper provides the largest, revised drug reference list annotated and ranked by the risk for developing hepatotoxicity in humans (DILIrank) by complementing the previously used drug-labeling information together with existing evidence of clinical causality assessments.

TL;DR: The role of 14-3-3 proteins in normal and disease states is summarized, with a focus on 14- 3-3γ and ɛ.

TL;DR: Light is shed on the developments of drug-drug co-crystals and future perspectives for exploring new therapeutic hybrids deploying drug- drug, drug-nutraceuticals and drug-inorganic salt combinations with improved pharmaceutical and biopharmaceutical performance are highlighted.

TL;DR: The latest developments and challenges in glycosylation analysis and control in the context of bioprocessing monoclonal antibodies are reviewed.

TL;DR: This review will focus on recent research of SODs in cellular regulation, with emphasis on their roles in cancer biology and therapy.

TL;DR: Analysis of the structures of 20 macrocyclic compounds that are approved oral drugs suggests that good solubility requires a topological polar surface area (TPSA) of ≥0.2×molecular weight (MW), and that some degree of chameleonic behavior is required for most high MW oral drugs.

TL;DR: A comprehensive overview of various computational approaches that enable the prediction and analysis of in vitro and in vivo drug-response phenotypes and outline their potential for drug discovery is provided.

TL;DR: The current state-of-the-art in the field of compound combination modelling is reviewed to support the development of approaches that, as it hope, will finally lead to an integration of chemical with systems-level biological information for predicting the effect of chemical mixtures.

TL;DR: The development of drugs targeting the PD-1/PD-L1 pathway is reviewed, including the monoclonal antibodies approved or in clinical trials, peptides and patented small molecules developed against this pathway, which has the potential to treat cancer as well as chronic virological diseases.

TL;DR: This short review discusses the most important technologies currently available for characterizing the direct and indirect target space of bioactive compounds following phenotypic screening and presents a comprehensive strategy employing complementary approaches to balance individual technology strengths and weaknesses.

TL;DR: The rapid assembly and in situ screening of focused combinatorial fragment libraries using CuAAC click chemistry is a highly robust and efficient strategy for establishing SAR and for discovering bioactive molecules.

TL;DR: In this paper, recent developments on in situ gelling systems for nasal delivery are presented, highlighting the mechanisms that govern their formation.

TL;DR: This work focuses on the solubilization of drugs by complexation, and discusses the determination and significance of binding constants for cyclodextrin complexes, and the determination of complexation efficiency and factors that influence it.

TL;DR: This review focuses on known non-oncological drugs with new therapeutic applications in oncology, explaining the rationale behind this approach and providing practical evidence, and highlighting opportunities for repurposing compounds as cancer therapeutics.

TL;DR: DNA-encoded chemical libraries have emerged as a powerful tool for hit identification in the pharmaceutical industry and in academia and can be easily produced within a few weeks by routine procedures.

TL;DR: Four key trends are identified that help to understand the change in strategic focus, realignment of R&D footprint, the shift from primary care toward specialty drugs and biologics and the growth of emerging markets as major revenue drivers for big pharma.

TL;DR: This review presents an overview of the immune-related obstacles that limit mRNA advance for non-immunotherapy-related applications.