Proteomic approaches advancing targeted protein degradation

Gajanan Sathe (Lead / Corresponding author), Gopal P. Sapkota (Lead / Corresponding author)

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)
13 Downloads (Pure)

Abstract

Targeted protein degradation (TPD) is an emerging modality for research and therapeutics. Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways. Proteolysis-targeting chimeras (PROTACs) and molecular glue (MG) degraders (MGDs) represent the most advanced TPD approaches, with some already used in clinical settings. Despite these advances, TPD still faces many challenges, pertaining to both the development of effective, selective, and tissue-penetrant degraders and understanding their mode of action. In this review, we focus on progress made in addressing these challenges. In particular, we discuss the utility and application of recent proteomic approaches as indispensable tools to enable insights into degrader development, including target engagement, degradation selectivity, efficacy, safety, and mode of action.

Original languageEnglish
Pages (from-to)786-801
Number of pages16
JournalTrends in Pharmacological Sciences
Volume44
Issue number11
Early online date29 Sept 2023
DOIs
Publication statusPublished - Nov 2023

Keywords

  • Targeted protein degradation
  • PROTAC
  • Molecular glue
  • Proteomics
  • Chemoproteomics
  • chemoproteomics
  • proteomics
  • targeted protein degradation
  • molecular glue

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology

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