Medicinal chemistry

Channelling Drug Discovery – Current trends in ion channel drug discovery research By Dr David Owen and Andrew Silverthorne Ion channels are proteins that span cell membranes thus forming conduits or ‘channels’ through which charged ions such as sodium and potassium can pass across a normally impermeant barrier such as the plasmalemma. By so doing, […]

The genomics revolution is poised to sweep aside the old economics of pharmaceutical R&D. The biotechnology and pharmaceutical industries; and perhaps healthcare delivery in general; are on the brink of transformation, and companies that embrace the revolution in the right way stand to reap enormous benefits. Developing a new drug should become considerably less unpredictable […]

Hit to lead and lead to candidate optimisation using multi-parametric principles By Dr Anthony D. Baxter and Dr Peter M. Lockey As the numbers of potential target proteins become available for pharmaceutical companies of all sizes, the drive towards more cost-effective drug discovery assumes greater significance. It is a truism to state that the biggest […]

Chemogenomics – A gene family approach to parallel drug discovery By Dr Paul R. Caron, Dr Michael D. Mullican, Dr Robert D. Mashal, Dr Keith P. Wilson, Dr Michael S. Su and Dr Mark A. Murcko Currently available drugs only target around 500 different proteins (4). Recent reports from efforts to sequence the human genome […]

Biologically Relevant Chemistry By Dr Stephen A. Hill A large proportion of R&D expenditure relates to the investigation of compounds which ultimately fail to reach the market as useful medicines. We discuss why early drug discovery – using high throughput, automated in vitro and in silico methods, must become the primary testing ground for novel […]

Pharmaceutical Industry R&D Partnering Strategies By Riccardo Pigliucci Drug Discovery With a sustained rate of more than 250 R&D partnering deals each year many valuable lessons are being learned. Although there is no exact ‘formula for success’ there are many ‘success factors’ that can be utilised to reduce the risk of failure. Research & Development […]

Increasing the chances of lead discovery By Sandra Fox, MBA, Dr Helen Wang, Dr Lynne Sopchak and Dr Richard Khoury For HTS laboratories worldwide, the mission is to supply therapeutic groups in the shortest time possible with high quality hits and leads that will become drug candidates. Mounting pressure to screen more targets against more […]

High Throughput Screening (HTS) – Where next? By Dr Mark Beggs After approximately a decade of maturation and a three orders of magnitude increase in capabilities, High Throughput Screening (HTS) is now an established discipline within pharmaceutical discovery. But opposing stresses exist within the screening world; the resolution of which will significantly affect the path […]

Discovery Research in the Co-Genomic Era – Biology goes industrial By Dr Timothy Wells and Dr Georg Feger The parallel between the search for gold in the last century and drug discovery in the co-genome era is very clear. As with all gold rushes the rewards will go to the most creative entrepreneurs who can […]

High-throughput Crystallisation By Dr Sara Moran and Dr Lance Stewart With structure-based drug design on the increase can the development of high-throughput crystallisation fulfil its promise to revolutionise the drug discovery process? In an era when the development of drugs is hindered by the exorbitant costs of discovery and clinical trials, any method that can […]