Current Pharmaceutical Biotechnology - Volume 11, Issue 7, 2010

The inter-discplinary science of Drug and Lead discovery continues to evolve and it does so by bringing more technologies to the lab. In the last decade we saw the advent of technologies that change the way we approach target biology (the human genome project), build compound collections (combinatorial, automated and contract synthesis), conduct screening (high throughput and high content screens), and ultim Read More

Systems biology focuses on the roles of cellular pathways and networks rather than single biomolecules to describe biological function. A systems view of biology requires technology that can generate and quantitatively analyze, large multi-dimensional data sets from many different sources. New technology has made this approach to drug discovery increasingly feasible. Detailed changes in cellular phenotype can be quantitat Read More

The development of RNA interference (RNAi)-mediated gene inhibition has changed the direction and speed of drug target discovery and validation. RNAi technology has already influenced strategies for the pharmacological treatment of many diseases including cancer, viral diseases, bacterial pathogens, inflammation, diseases of central nervous systems (CNS), and others. This technology provides a better understanding of th Read More

G protein-coupled receptors represent one of the largest families of drug targets. Time and cost may be saved if GPCR modulators are assessed in terms of signaling pathway selectivity, species selectivity, and selectivity against closely-related family members early in the drug discovery process, perhaps even at the stage of high-throughput screening. Examples are given of how these kinds of selectivity have been addre Read More

High throughput screening (HTS) facilitates screening large numbers of compounds against a biochemical target of interest using validated biological or biophysical assays. In recent years, a significant number of drugs in clinical trails originated from HTS campaigns, validating HTS as a bona fide mechanism for hit finding. In the current drug discovery landscape, the pharmaceutical industry is embracing open innovation Read More

Controlling elevated tissue-specific levels of cortisol may provide a novel therapeutic approach for treating metabolic syndrome. This concept has spurred large scale medicinal chemistry efforts in the pharmaceutical industry for the design of 11β-HSD1 inhibitors. High resolution X-ray crystal structures of inhibitors in complex with the enzyme have facilitated the structure-based design of diverse classes of molecules. A summ Read More