Antibody–PROTAC conjugates enable HER2-dependent targeted protein degradation of BRD4

M Maneiro, N Forte, MM Shchepinova… - ACS chemical …, 2020 - ACS Publications
Targeting protein degradation with Proteolysis-Targeting Chimeras (PROTACs) is an area of
great current interest in drug discovery. Nevertheless, although the high effectiveness of …

Antibody-mediated delivery of chimeric BRD4 degraders. Part 2: improvement of in vitro antiproliferation activity and in vivo antitumor efficacy

PS Dragovich, TH Pillow, RA Blake… - Journal of Medicinal …, 2021 - ACS Publications
Heterobifunctional compounds that direct the ubiquitination of intracellular proteins in a
targeted manner via co-opted ubiquitin ligases have enormous potential to transform the …

Antibody-mediated delivery of chimeric BRD4 degraders. Part 1: exploration of antibody linker, payload loading, and payload molecular properties

PS Dragovich, TH Pillow, RA Blake… - Journal of Medicinal …, 2021 - ACS Publications
The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and
related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin …

[HTML][HTML] Targeted degradation via direct 26S proteasome recruitment

C Bashore, S Prakash, MC Johnson… - Nature Chemical …, 2023 - nature.com
Engineered destruction of target proteins by recruitment to the cell's degradation machinery
has emerged as a promising strategy in drug discovery. The majority of molecules that …

Protein degradation by in-cell self-assembly of proteolysis targeting chimeras

H Lebraud, DJ Wright, CN Johnson… - ACS central …, 2016 - ACS Publications
Selective degradation of proteins by proteolysis targeting chimeras (PROTACs) offers a
promising potential alternative to protein inhibition for therapeutic intervention. Current …

[HTML][HTML] Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation

MJ Bond, CM Crews - RSC chemical biology, 2021 - pubs.rsc.org
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …

Iterative design and optimization of initially inactive proteolysis targeting chimeras (PROTACs) identify VZ185 as a potent, fast, and selective von Hippel–Lindau (VHL) …

V Zoppi, SJ Hughes, C Maniaci, A Testa… - Journal of medicinal …, 2018 - ACS Publications
Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently
degrade a target protein within cells can be a lengthy and unpredictable process, and it …

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 …

Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets

Y Xiong, Y Zhong, H Yim, X Yang, KS Park… - Journal of the …, 2022 - ACS Publications
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed for …

Acquired resistance to BET-PROTACs (proteolysis-targeting chimeras) caused by genomic alterations in core components of E3 ligase complexes

L Zhang, B Riley-Gillis, P Vijay, Y Shen - Molecular cancer therapeutics, 2019 - AACR
Proteolysis-targeting chimeras (PROTAC) are bifunctional molecules that hijack
endogenous E3 ubiquitin ligases to induce ubiquitination and subsequent degradation of …