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The PROTACtable genome.

Authors :
Schneider M
Radoux CJ
Hercules A
Ochoa D
Dunham I
Zalmas LP
Hessler G
Ruf S
Shanmugasundaram V
Hann MM
Thomas PJ
Queisser MA
Benowitz AB
Brown K
Leach AR
Source :
Nature reviews. Drug discovery [Nat Rev Drug Discov] 2021 Oct; Vol. 20 (10), pp. 789-797. Date of Electronic Publication: 2021 Jul 20.
Publication Year :
2021

Abstract

Proteolysis-targeting chimeras (PROTACs) are an emerging drug modality that may offer new opportunities to circumvent some of the limitations associated with traditional small-molecule therapeutics. By analogy with the concept of the 'druggable genome', the question arises as to which potential drug targets might PROTAC-mediated protein degradation be most applicable. Here, we present a systematic approach to the assessment of the PROTAC tractability (PROTACtability) of protein targets using a series of criteria based on data and information from a diverse range of relevant publicly available resources. Our approach could support decision-making on whether or not a particular target may be amenable to modulation using a PROTAC. Using our approach, we identified 1,067 proteins of the human proteome that have not yet been described in the literature as PROTAC targets that offer potential opportunities for future PROTAC-based efforts.<br /> (© 2021. Springer Nature Limited.)

Details

Language :
English
ISSN :
1474-1784
Volume :
20
Issue :
10
Database :
MEDLINE
Journal :
Nature reviews. Drug discovery
Publication Type :
Academic Journal
Accession number :
34285415
Full Text :
https://doi.org/10.1038/s41573-021-00245-x