Current Pharmaceutical Design - Volume 8, Issue 13, 2002

The current increase in the number of microbes resistant to antibacterial or antifungal agents represents a potential crisis in human and veterinary medicine. Some believe that we are entering a postantibiotic era where most antibiotics no longer will be efficacious. Therefore, it is important that new antibiotics be developed. However, because of the potential for cross-resistance, new targets for the discovery of antibiotics are ne Read More

Whole chromosome sequence of prokaryotes has provided the availability of multiple bacterial pathogen sequence data and it has become a widely used tool in the drug discovery process. However the sequence data in itself is merely a starting point for drug discovery of novel antibacterial targets and, eventually, drugs. In order to leverage this large amount of data it is necessary to match an understanding of Read More

The process of prokaryotic drug discovery has been a model of success for over fifty years, yet the number of exploited bacterial targets is a mere fraction, less than 0.1% of the potential targets (based on total number of bacterial genes identified by gene sequence projects). To better understand the potential for drug intervention, multiple paradigms have been established in the pharmaceutical industry, all with some s Read More

The use of genomics tools to discover new genes, to decipher pathways or to assign a function to a gene is just beginning to have an impact. Genomics approaches have been applied to both antibacterial and antifungal target discovery in order to identify a new generation of antibiotics. This review discusses genomics approaches for antifungal drug discovery, focusing on the areas of gene discovery, target validation, an Read More

In large part, antimicrobial drug discovery is driven by the breadth and quality of both potential drug targets and available chemical libraries to screen. Traditionally, targets have been few in number and have been limited to those with known function, from which biochemical assays could be implemented into drug screens. Iterations of this same basic approach, applied to a few biochemically-defined targets have identifie Read More

Structural Genomics stands out among the emerging fields of proteomics since it influences the drug discovery process at so many points. Recent developments in protein expression technologies, x-ray crystallography and NMR spectroscopy provide the essential elements for high-throughput structure determination platforms. Bioinformatics methods to interrogate the resulting data will provide comprehensive, genome-wide d Read More

Despite considerable progress in the analysis of microbial genomes, the number of validated targets suitable for the development of drugs acting on agents causing infectious diseases remains modest. The diversity of new chemical entities specific for such targets has almost not increased over the last years, while resistance to antiinfectious drugs has, in contrast, become a real threat in certain surroundings. New strategie Read More