Protein degraders enter the clinic—a new approach to cancer therapy

D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …

Advances in covalent drug discovery

L Boike, NJ Henning, DK Nomura - Nature Reviews Drug Discovery, 2022 - nature.com
Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

[HTML][HTML] Expanding PROTACtable genome universe of E3 ligases

Y Liu, J Yang, T Wang, M Luo, Y Chen, C Chen… - Nature …, 2023 - nature.com
Proteolysis-targeting chimera (PROTAC) and other targeted protein degradation (TPD)
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …

Rational chemical design of molecular glue degraders

ES Toriki, JW Papatzimas, K Nishikawa… - ACS central …, 2023 - ACS Publications
Targeted protein degradation with molecular glue degraders has arisen as a powerful
therapeutic modality for eliminating classically undruggable disease-causing proteins …

Molecular glues: the adhesive connecting targeted protein degradation to the clinic

JM Sasso, R Tenchov, DS Wang, LS Johnson… - Biochemistry, 2022 - ACS Publications
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …

Small-molecule discovery through DNA-encoded libraries

AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …

A CRISPR activation screen identifies FBXO22 supporting targeted protein degradation

AA Basu, C Zhang, IA Riha, A Magassa… - Nature Chemical …, 2024 - nature.com
Targeted protein degradation (TPD) represents a potent chemical biology paradigm that
leverages the cellular degradation machinery to pharmacologically eliminate specific …

The rise of degrader drugs

M Teng, NS Gray - Cell Chemical Biology, 2023 - cell.com
The cancer genomics revolution has served up a plethora of promising and challenging
targets for the drug discovery community. The field of targeted protein degradation (TPD) …

[HTML][HTML] Chemoproteomics-enabled discovery of a covalent molecular glue degrader targeting NF-κB

EA King, Y Cho, NS Hsu, D Dovala, JM McKenna… - Cell chemical …, 2023 - cell.com
Targeted protein degradation has arisen as a powerful therapeutic modality for degrading
disease targets. While proteolysis-targeting chimera (PROTAC) design is more modular, the …

Targeted protein degradation: current and emerging approaches for E3 ligase deconvolution

Y Xiao, Y Yuan, Y Liu, Z Lin, G Zheng… - Journal of Medicinal …, 2024 - ACS Publications
Targeted protein degradation (TPD), including the use of proteolysis-targeting chimeras
(PROTACs) and molecular glue degraders (MGDs) to degrade proteins, is an emerging …