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Unexplored therapeutic opportunities in the human genome.


ABSTRACT: A large proportion of biomedical research and the development of therapeutics is focused on a small fraction of the human genome. In a strategic effort to map the knowledge gaps around proteins encoded by the human genome and to promote the exploration of currently understudied, but potentially druggable, proteins, the US National Institutes of Health launched the Illuminating the Druggable Genome (IDG) initiative in 2014. In this article, we discuss how the systematic collection and processing of a wide array of genomic, proteomic, chemical and disease-related resource data by the IDG Knowledge Management Center have enabled the development of evidence-based criteria for tracking the target development level (TDL) of human proteins, which indicates a substantial knowledge deficit for approximately one out of three proteins in the human proteome. We then present spotlights on the TDL categories as well as key drug target classes, including G protein-coupled receptors, protein kinases and ion channels, which illustrate the nature of the unexplored opportunities for biomedical research and therapeutic development.

SUBMITTER: Oprea TI 

PROVIDER: S-EPMC6339563 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature

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Unexplored therapeutic opportunities in the human genome.

Oprea Tudor I TI   Bologa Cristian G CG   Brunak Søren S   Campbell Allen A   Gan Gregory N GN   Gaulton Anna A   Gomez Shawn M SM   Guha Rajarshi R   Hersey Anne A   Holmes Jayme J   Jadhav Ajit A   Jensen Lars Juhl LJ   Johnson Gary L GL   Karlson Anneli A   Leach Andrew R AR   Ma'ayan Avi A   Malovannaya Anna A   Mani Subramani S   Mathias Stephen L SL   McManus Michael T MT   Meehan Terrence F TF   von Mering Christian C   Muthas Daniel D   Nguyen Dac-Trung DT   Overington John P JP   Papadatos George G   Qin Jun J   Reich Christian C   Roth Bryan L BL   Schürer Stephan C SC   Simeonov Anton A   Sklar Larry A LA   Southall Noel N   Tomita Susumu S   Tudose Ilinca I   Ursu Oleg O   Vidovic Dušica D   Waller Anna A   Westergaard David D   Yang Jeremy J JJ   Zahoránszky-Köhalmi Gergely G  

Nature reviews. Drug discovery 20180323 5


A large proportion of biomedical research and the development of therapeutics is focused on a small fraction of the human genome. In a strategic effort to map the knowledge gaps around proteins encoded by the human genome and to promote the exploration of currently understudied, but potentially druggable, proteins, the US National Institutes of Health launched the Illuminating the Druggable Genome (IDG) initiative in 2014. In this article, we discuss how the systematic collection and processing  ...[more]

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