Showing papers in "Drug Discovery Today in 2008"

TL;DR: Various screening approaches are being developed to improve the ease with which natural products can be used in drug discovery campaigns, and data mining and virtual screening techniques are also being applied to databases of natural products.

TL;DR: This article addresses pharmaceutical cocrystals from the perspective of design (crystal engineering) and presents a series of case studies that demonstrate how they can enhance the solubility, bioavailability, and/or stability of API crystal forms.

TL;DR: This review explores how human ABC transporters modulate the pharmacological effects of various drugs, and how this predictable ADME-TOX modulation can be used during the process of drug discovery and development.

TL;DR: An insight into the various constraints associated with ocular drug delivery is provided, recent findings and applications of various nanoparticulate systems like microemulsions, nanosuspensions, nanoparticles, liposomes, niosomes, dendrimers and cyclodextrins are summarized and how the various upcoming of nanotechnology can be utilized to explore the frontiers of ocularDrug delivery and therapy are depicted.

TL;DR: Adaptation of conventional instrumentation combined with new nanotechnology developments will continue to expand use of zebrafish for drug screening, and full validation will require assessment of a large number of compounds from diverse classes.

TL;DR: The structure/activity relationships (SARs) as mentioned in this paper explicitly incorporate the interplay between enthalpy and entropy and accelerate the optimization process are being developed and gaining popularity in the literature.

TL;DR: The plant-based drug discovery resulted mainly in the development of anticancer and anti-infectious agents and continues to contribute to the new leads in clinical trials as of September 2007.

TL;DR: This review examines the various siRNA modifications available, including every aspect of the RNA structure and siRNA duplex architecture, with a focus on specificity, delivery, and nuclease stability and potency.

TL;DR: The extracellular flux (XF), that is the changes in oxygen and proton concentrations in the media surrounding cells, can simultaneously determine their relative state of aerobic and glycolytic metabolism, respectively, making it an attractive format for studying drug effects in vitro.

TL;DR: The biggest drug delivery challenge is to develop effective methods for posterior segment therapies that would also be applicable for the out-patient use.

TL;DR: An overview of the recent advances in the study of S-SEDDS, especially the related solidification techniques and the development of solid SE dosage forms is given.

TL;DR: The recent advances of microfluidic devices for drug discovery and development are reviewed and their applications in different stages of the process are highlighted, including target selection, lead identification, preclinical tests, clinical trials, chemical synthesis, formulations studies and product management.

TL;DR: DARPins (designed ankyrin repeat proteins) are a novel class of binding molecules with the potential to overcome limitations of monoclonal antibodies, hence allowing novel therapeutic approaches and taken together are a prominent member of the next generation of protein therapeutics.

TL;DR: There is a large armoury of methods that can be used to tackle the appearance and disappearance of polymorphs, and the methods and their successes over the last few years are surveyed.

TL;DR: This manuscript will review the approaches that have been explored to achieve chemical functionalization of drugs or of drug vector systems and endogenous transporters at the blood-brain barrier at the BBB.

TL;DR: An overview of key technologies and latest developments in the area of 3D pharmacophores is given and provides insight into different approaches as implemented by the 3D Pharmacophore modeling packages like Catalyst, MOE, Phase and LigandScout.

TL;DR: The understanding of the role played by Hsp90 in regulating and maintaining the transformed phenotype in cancers and neurodegenerative diseases, as well as recent findings on its roles in fungal and viral infections are discussed.

TL;DR: Interestingly, attrition is approximately 60-70% across a variety of therapeutic areas, including the central nervous system and cardiovascular medicine (where animal models are considered to be more predictive).

TL;DR: As it is demonstrated, molecules are not 'frozen statues' but 'dancing ballerinas', and several of their computable physicochemical properties are conformation-dependent and lead to the concept of property spaces, which appears as a promising descriptor to encode some of the information contained in molecular property spaces.

TL;DR: ACGH increased the ability to detect segmental genomic CNVs in patients with global developmental delay, mental retardation, autism, multiple congenital anomalies and dysmorphism, and is becoming a powerful tool in disease gene discovery and prenatal diagnostics.

TL;DR: This review summarises the recent developments in the field of intra-pocket drug delivery systems and identifies areas where further research may lead to a clinically effective intra- pocket delivery system.

TL;DR: The lessons learned from antisense drug development can help in the development of other oligonucleotide-based therapeutics such as CpG oligon nucleotides, RNAi and miRNA.

TL;DR: Computational tools for predicting toxicity have been exhaustively optimized for early safety-relevant endpoints like genotoxicity and future activities will now be directed to prevent the occurrence of undesired toxicity in patients by making these tools more relevant to human disease.

TL;DR: In the scenario of a continuous request for better drugs in shorter times, medicinal chemists must face the challenging task of preparing new patentable molecules, combining high activity and selectivity, drug-likeness and good pharmacokinetic properties.

TL;DR: Some of the uncertainties introduced during the process of deriving an atomic model from the experimentally observed electron density are highlighted with recent examples from the literature, together with snippets of advice for the medicinal chemist embarking on using X-ray crystal structure information in a drug discovery programme.

TL;DR: This work focuses on the protein epitope mimetic (PEM) approach, where folded 3D structures of peptides and proteins are taken as starting points for the design of synthetic molecules that mimic key epitopes involved in protein-protein and protein-nucleic acid interactions.

TL;DR: The potential of ITC for the characterization of different functionalities carried by nanoparticles as well as their interaction with living systems was outlined and their use for pharmaceutical formulations and drug delivery system characterization was outlined.

TL;DR: This work provides a concise review of a number of new potential anti-tuberculosis drug candidates with novel modes of action, their structure-activity relationships, in vitro and in vivo activity, pharmacokinetics, mechanism of action and combination regimens.

TL;DR: Although the average number of therapeutic candidates entering clinical study per year more than doubled, the US approval success rate was low (8%) during the period, indicating that improvement in the efficiency of the development process for innovative cancer treatments is needed.

TL;DR: This review will outline which fatty acid amides have been isolated from mammalian sources, detail what is known about how these molecules are made and degraded in vivo, and highlight their potential for the development of novel therapeutics.