Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

X Zhang, VM Crowley, TG Wucherpfennig… - Nature chemical …, 2019 - nature.com
Ligand-dependent protein degradation has emerged as a compelling strategy to
pharmacologically control the protein content of cells. So far, however, only a limited number …

Chemical specification of E3 ubiquitin ligase engagement by cysteine-reactive chemistry

RC Sarott, I You, YD Li, ST Toenjes… - Journal of the …, 2023 - ACS Publications
Targeted protein degradation relies on small molecules that induce new protein–protein
interactions between targets and the cellular protein degradation machinery. Most of these …

DCAF11 supports targeted protein degradation by electrophilic proteolysis-targeting chimeras

X Zhang, LM Luukkonen, CL Eissler… - Journal of the …, 2021 - ACS Publications
Ligand-induced protein degradation has emerged as a compelling approach to promote the
targeted elimination of proteins from cells by directing these proteins to the ubiquitin …

Targeted Protein Degradation through Recruitment of the CUL4 Complex Adaptor Protein DDB1

M Meyers, S Cismoski, A Panidapu… - ACS chemical …, 2024 - ACS Publications
Targeted protein degradation has arisen as a powerful therapeutic modality for eliminating
proteins. Thus far, most heterobifunctional proteolysis targeting chimeras (PROTACs) have …

E3-specific degrader discovery by dynamic tracing of substrate receptor abundance

A Hanzl, E Barone, S Bauer, H Yue… - Journal of the …, 2023 - ACS Publications
Targeted protein degradation (TPD) is a new pharmacology based on small-molecule
degraders that induce proximity between a protein of interest (POI) and an E3 ubiquitin …

Targeted protein degradation through E2 recruitment

N Forte, D Dovala, MJ Hesse, JM McKenna… - ACS chemical …, 2023 - ACS Publications
Targeted protein degradation (TPD) with proteolysis targeting chimeras (PROTACs),
heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of …

Targeted protein degradation by electrophilic PROTACs that stereoselectively and site-specifically engage DCAF1

Y Tao, D Remillard, EV Vinogradova… - Journal of the …, 2022 - ACS Publications
Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …

[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 …

cIAP1-based degraders induce degradation via branched ubiquitin architectures

Y Akizuki, M Morita, Y Mori, A Kaiho-Soma… - Nature Chemical …, 2023 - nature.com
Targeted protein degradation through chemical hijacking of E3 ubiquitin ligases is an
emerging concept in precision medicine. The ubiquitin code is a critical determinant of the …

Rational discovery of molecular glue degraders via scalable chemical profiling

C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka… - Nature chemical …, 2020 - nature.com
Targeted protein degradation is a new therapeutic modality based on drugs that destabilize
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …