The PROTACtable genome

Autor: Lykourgos-Panagiotis Zalmas, Andrew Hercules, Melanie Schneider, Ian Dunham, David Ochoa, Andrew B. Benowitz, Markus A. Queisser, Sven Ruf, Veerabahu Shanmugasundaram, Andrew R. Leach, Kris Brown, Pamela Thomas, Gerhard Hessler, Chris J Radoux, Michael M. Hann
Rok vydání: 2021
Předmět:
Zdroj: Nature Reviews Drug Discovery. 20:789-797
ISSN: 1474-1784
1474-1776
Popis: 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.
Databáze: OpenAIRE
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