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Illuminating the Druggable Genome Program Highlights

Investigators in the IDG Consortium have Mapped Out the Targets of Every FDA Approved Drug

The vast majority of drugs approved by the FDA act through binding to and changing the activity of protein targets. These targets could be human proteins or proteins from pathogens that infect humans. One measure of the remaining opportunities available for new drug discovery is the number of proteins that have not yet been targeted by a drug. To this end, the Knowledge Management Center of the IDG Program compiled all the information about which proteins are targeted by all the US FDA approved drugs. Through this effort, they were able to show that 1,414 approved drugs act through targeting 667 human and 189 pathogen proteins. By examining trends in the proteins being targeted by new drugs, the authors were able to determine which types of proteins have been the most successful targets for new medications for particular classes of diseases.  This data can also be used to understand which human proteins have not yet been targeted by drug development efforts, thus cataloging the unexplored space from which new drugs can be designed in the future.


A comprehensive map of molecular drug targets. Santos R1, Ursu O, Gaulton A, Bento AP, Donadi RS, Bologa CG, Karlsson A, Al-Lazikani B, Hersey A, Oprea TI, Overington JP. Nat Rev Drug Discov. 2017 Jan; 16(1):19-34.

Publications from IDG Investigators: Exploring the Druggable Genome

A recent paper published in Nature by IDG grantees Brian Shoichet and Bryan Roth, suggests combining physical and structure-based screening as a broadly useful method for ligand discovery of understudied and orphan GPCRs.

A recent article in Science Translational Medicine from  IDG investigator Joel T. Dudley, demonstrates the usefulness of applying the precision medicine approach to characterize the complexity of Type 2 diabetes using high-dimensional electronic medical records and genotype data from over 11,000 patients.

An article published in Nature Structural and Molecular Biology describes PRESTO-Tango; a screening assay developed by Dr. Bryan L. Roth and colleagues at the University of North Carolina, Chapel Hill. PRESTO-Tango allows for the simultaneous investigation of every nonolfactory G protein-coupled receptor in the human genome. The methods and reagents developed are freely available to the scientific community.

Dr. Gary Johnson at the University of North Carolina, Chapel Hill published a paper in Cell Reports that used a global approach to study the effects of adaptation of the kinome (the full complement of human protein kinases) and its role in drug resistance during cancer treatment.

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