Combinatorial chemistry

High Throughput Screening in Academia – Drug discovery initiatives at the University of Kansas By Dr P McDonald, Dr Roy, Byron Taylor, Ashleigh Price, Dr Sittampalam, Dr Scott Weir, Dr Chaguturu Academia has historically been involved in exploring the fundamental aspects of the disease targets and in developing tool molecules to better understand the genetic, […]

Progress in Systems-Based Analysis of Cellular Signalling By Dr Jeffrey A. Radding Drug discovery currently focuses on targeted approaches, relying on validation of the target as a disease driver. However, the underlying biological complexity of disease often frustrates these attempts at therapeutic intervention, resulting in high failure rates due to lack of efficacy. Systems biology […]

Perspectives for ADMET Integration in the Discovery Process By Dr Constance Hofer ADMET (ADME/Tox), is a relatively new symbiotic acronym for the investigation of basic compound behaviour in terms of absorption, distribution, metabolism and excretion, combined with assessments of toxicity. The emergence of ADMET instead of ADME reflects the growing practice of combining in vitro […]

Challenges and opportunities for the greening of separation science in the pharmaceutical industry Dr Christopher J. Welch Opportunities for reducing solvent consumption and waste generation in separation sciences used to support industrial pharmaceutical discovery and development are presented and discussed in this article. Several approaches are considered for ‘greening’ analytical chromatography, where small solvent savings […]

The Power of APTAMERS in the Drug Discovery Process Professor Michael Famulok Methods of combinatorial biochemistry allow the identification of nucleic acid sequences, or aptamers, which can bind their target molecules with high affinity and specificity and are able to efficiently inhibit their biological function. Macugen, the first aptamer-based drug for the treatment of age-related […]

The Deming Approach to Quality In Pharmaceutical Research By John H. Van Drie We explore the relevance to pharmaceutical research of the ideas of W. Edwards Deming, the statistician whose ideas on quality transformed the manufacturing sector of post-war Japan. To enhance productivity in pharmaceutical research, we have tended to look to innovations in science […]

Technology, Bane or Bonanza for the Pharmaceutical industry? By Dr Stephen Naylor, Adam W. Culbertson and Dr Stephen J. Valentine Productivity in the pharmaceutical industry has long held well-documented concerns.   While the adoption of new technologies into the drug discovery and development process has often been seen as a panacea, this article argues that, […]

Lean Thinking for Drug Discovery – Better Productivity for Pharma By Dr Edward W. Petrillo Success in drug discovery controls the success of the pharmaceutical enterprise. The molecular structure of every drug candidate, and the body of knowledge that will guide its use in the treatment of disease, are established during drug discovery in the […]

Medicinal Chemistry: Progress through innovation By Dr Terry Hart Medicinal chemistry is a specialised science that has evolved to encompass a broad range of disciplines concerned with the identification, synthesis and development of drug-like compounds for therapeutic use. It needs a wide range of expertise, developed through years of training, dedication and learning from best […]

Miniaturisation of Assay Development and Screening By Andreas Boettcher and Dr Lorenz M. Mayr In recent years we have seen a strong increase in the number of chemical compounds and molecular targets used for lead discovery by high-throughput screening among most Pharma and Biotech companies. This has caused a strong push towards volume reduction, throughput […]