Details

Autor(en) / Beteiligte

• Nalawansha, Dhanusha A.
• Crews, Craig M.

Titel

PROTACs: An Emerging Therapeutic Modality in Precision Medicine

Ist Teil von

• Cell chemical biology, 2020-08, Vol.27 (8), p.998-1014

Ort / Verlag

Elsevier Ltd

Erscheinungsjahr

2020

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Targeted protein degradation (TPD) has emerged as an exciting new era in chemical biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets cellular proteins for degradation by co-opting the ubiquitin-proteasome system. Over the last 5 years, numerous studies have expanded our understanding of the unique mode of action and advantages of PROTACs, which has in turn spurred interest in both academia and industry to explore PROTACs as a novel therapeutic strategy. In this review, we first highlight the key advantages of PROTACs and then discuss the spatiotemporal regulation of protein degradation. Next, we explore current chemically tractable E3 ligases focusing on expanding the existing repertoire with novel E3 ligases to uncover the full potential of TPD. Collectively, these studies are guiding the development of the PROTAC technology as it emerges as a new modality in precision medicine. [Display omitted] Nalawansha et al. review the advantages and recent advances of the PROTAC technology focusing on the spatiotemporal regulation of protein degradation, the chemically tractable E3 ligases, as well as covalent and non-covalent PROTACs.