The druggable genome

@article{Hopkins2002TheDG,
  title={The druggable genome},
  author={Andrew L. Hopkins and Colin R. Groom},
  journal={Nature Reviews Drug Discovery},
  year={2002},
  volume={1},
  pages={727-730}
}
An assessment of the number of molecular targets that represent an opportunity for therapeutic intervention is crucial to the development of post-genomic research strategies within the pharmaceutical industry. Now that we know the size of the human genome, it is interesting to consider just how many molecular targets this opportunity represents. We start from the position that we understand the properties that are required for a good drug, and therefore must be able to understand what makes a… 
View on Nature
cs.gmu.edu
2,894 Citations
Highly Influential Citations
81
Background Citations
1,013
Methods Citations
71
Results Citations
11

2,894 Citations

3.01 – Genomics
The path to oncology drug target validation: an industry perspective.
TLDR
This chapter provides an overview on target identification and validation approaches to interrogate the functional and therapeutic relevance of a candidate cancer drug target as an essential step towards justifying the subsequent investment in drug discovery efforts.
Chapter 16 – Pharmacological Space
Genetic-Driven Druggable Target Identification and Validation.
Modeling drug action in the mouse with knockouts and RNA interference
Discovery: Use of Systems Biology for Identifying Targets
TLDR
It is emphasized that a combination of reductionist (mechanism- based) and holistic (hypothesis-based) tools in the drug screening process may increase the efficiency of overall Drug Discovery.
Putting small molecules in the lead
TLDR
The 58th Ernst Schering Foundation Workshop on “Chemical Genomics: Small Molecule Probes to Study Cellular Function,” held April 6–8, 2005, in Berlin, Germany, captured recent chemical genomics advances and highlighted the power of a tight integration of chemistry and biology.
Exploitation of silicon medicinal chemistry in drug discovery
TLDR
The application of organosilicon medicinal chemistry in the context of privileged structures to aid drug design and development is one such innovative approach that is reviewed in this paper.
Genomic-scale prioritization of drug targets: the TDR Targets database
TLDR
The development of the TDR Targets database is discussed, which encompasses extensive genetic, biochemical and pharmacological data related to tropical disease pathogens, as well as computationally predicted druggability for potential targets and compound desirability information, and aims to facilitate the identification and prioritization of candidate drug targets for pathogens.
Opportunities to minimise risk in drug discovery and development
  • D. Swinney
  • Biology
    Expert opinion on drug discovery
  • 2006
The last decade has seen great advances in defining the molecular components of physiological pathways with the sequencing of the human genome and advances in protein structure analysis. However,…
...
...

References

SHOWING 1-10 OF 17 REFERENCES
In vivo drug target discovery: identifying the best targets from the genome.
Drug discovery: a historical perspective.
TLDR
The biotech industry is establishing itself as the discovery arm of the pharmaceutical industry, and in bridging the gap between academia and large pharmaceutical companies, the biotech firms have been effective instruments of technology transfer.
Initial sequencing and analysis of the human genome
TLDR
The results of an international collaboration to produce and make freely available a draft sequence of the human genome are reported and an initial analysis is presented, describing some of the insights that can be gleaned from the sequence.
What If There Are Only 30,000 Human Genes?
The complete assembly of the entire human genome sequence by Venter et al. confirms recent estimates that the total number of human protein coding genes might be less than 30,000--a mere one-third…
A functional genomics strategy that uses metabolome data to reveal the phenotype of silent mutations
TLDR
It is demonstrated how the intracellular concentrations of metabolites can reveal phenotypes for proteins active in metabolic regulation, and this approach to functional analysis, using comparative metabolomics, is called FANCY—an abbreviation for functional analysis by co-responses in yeast.
The end of the beginning for genomic medicine
TLDR
The human genome sequence yields several surprises for researchers seeking to exploit genomic data in drug discovery, and this work highlights the importance of understanding the lay of the land for drug discovery.
Metabolite profiling for plant functional genomics
TLDR
The use of metabolite profiling is described as a new tool for a comparative display of gene function and has the potential not only to provide deeper insight into complex regulatory processes but also to determine phenotype directly.
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings.
Effect of Slow Growth on Metabolism of Escherichia coli, as Revealed by Global Metabolite Pool (“Metabolome”) Analysis
TLDR
The results indicate that total metabolite pool ("metabolome") analysis offers a means of revealing novel aspects of cellular metabolism and global regulation.
The InterPro database, an integrated documentation resource for protein families, domains and functional sites
TLDR
InterPro is an integrated documentation resource for protein families, domains and functional sites, which amalgamates the efforts of the PROSITE, PRINTS, Pfam and ProDom database projects.
...
...