Combinatorial chemistry

The search for validated biomarkers in the face of biosystems complexity By Professor Ian Humphery-Smith and Will Dracup As the pharmaceutical industry is all too well aware, the genomics and postgenomic sciences have delivered an excessive number of drug targets few of which have been well validated. Indeed, apart from a few rare exceptions, genomics […]

COX-2 Inhibitor Toxicity – Warning shot over pharma’s bow By Dr Mark Schena and Dr William Greene Human beings are complex gene machines that rely on the intricate interplay of ~25,000 genes to impart biological function. Genomic function is affected by genetic variability and environmental factors, giving rise to considerable functional heterogeneity in the human […]

Systems biology, information, disease and drug discovery By Professor Stephen Naylor Pharmaceutical companies are confronted with an urgent need to increase their lead compound and clinical candidate portfolios and to satisfy market demands for continued innovation and revenue growth. The lack of improved productivity and limited drug pipeline growth is well described and documented. This […]

Leveraging the ion channel platform for lead generation in atrial fibrillation By Professor Andreas Busch Competition in the pharmaceutical industry requires a reduction in research and development project cycle times and, accordingly, an increase in productivity and efficiency. Pharmaceutical companies also are faced with the challenge of translating massive amounts of new genomic data into […]

GENE EXPRESSION as a toxicological screening tool By Dr Bruce Seligmann The use of microarray data in drug development and requirements for FDA audit and approval. Toxicological safety testing of compounds has not yet advanced to the point where measurement of gene expression is being incorporated in the internal decision process of most companies, much […]

The impact of early ADME profiling on drug discovery and development strategy By Dr Jianling Wang and Dr Laszlo Urban The increased costs in the discovery and development of new drugs, due in part to the high attrition rate of drug candidates in development, has led to a new strategy to introduce early, parallel evaluation […]

Applications of liquid chromatography mass spectrometry By Dr David Kwok Applications of liquid chromatography mass spectrometry in accelerating the pace of lead-drug candidate selection and pre-clinical development. This review discusses how the application and benefits of using LC/MS and LC/MS/MS assays in conjunction with in vivo and in vitro study designs can generate significant advantages […]

Structural Genomics drives demand for high throughput protein purification By Karsten Fjarstedt The rapid growth in proteomic and structural and functional genomic research is driving demand for purified proteins that far exceeds the industry’s ability to scale-up conventional protein production technologies. This demand has sparked innovation in protein separation and purification technologies. We discuss how […]

Failure rates in drug discovery and development: will we ever get any better? By William Bains Drug discovery is an expensive, slow and risky business. An analysis which takes into account projects which neither succeed nor fail suggests that it costs more than $1 billion to launch a technically successful drug, and takes 12.5 years. […]

The Current Bioinformatics Analytical Software Landscape By Charles Chang With the vast amount of biochemical data generated from experiments conducted by research laboratories around the globe, there is strong demand for software to analyse and manage the data effectively. Analytical software can be utilised to analyse virtually every single experiment, ranging from gene sequence analysis […]

Virtual Screening – Finding needles in a haystack on a shoestring By Dr David E. Clark, Neil V. Harris, Alan G. Roach and Dr Anthony D. Baxter In recent years, virtual screening (VS) has become an accepted approach to hit-finding alongside biochemical high-throughput screening (HTS). Large pharmaceutical companies are typically in the fortunate position of […]

Opportunities for the pharmaceutical industry: key biotransformation technologies of the future By Praveen Kaul, Anirban Banerjee and Professor UC Banerjee Biotransformation is a broad and growing field of biotechnology and encompasses both enzymatic and microbial biocatalysis. Progress has been made in research on the key drivers of biotransformations, including the isolation, screening and characterisation of […]

SCAVENGER strategies in organic synthesis – Part Two By Professor Peter Wipf and Dr Claire M. Coleman Part 1 of this article discussed the fundamental principles of the use of scavenging techniques in combinatorial and organic synthesis. Part one of scavenger strategies is linked here. In this article, more recent developments are introduced that illustrate […]

Making the Most of Drug Discovery Data By Dr Nick Davies and Dr Tim Peakman Discovery scientists in most pharmaceutical companies are struggling with incompatible legacy systems, a growing volume of data and the imminent advent of a product model that will demand much more of them. Data-driven drug discovery (4D) is a methodology for […]

Gene Expression: Analysis and Drug R&D By Dr Ralph Sinibaldi It is clear that gene expression profiling systems have a role to play in many facets of drug discovery and development, but several questions remain. We take a look at the use of DNA microarray for gene expression or expression profiling and how DNA chips […]

SCAVENGER strategies in organic synthesis – Part One By Professor Peter Wipf and Dr Claire M. Coleman Over the past 20 years combinatorial chemistry has proved to be an important tool for the generation of large numbers of compounds required for drug discovery programmes. This two-part article covers the history and current developments of scavenger […]