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 …
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 …
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 …
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 …
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 …
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
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …
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) …
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 …
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 …
heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of …
Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed 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
Proteolysis-targeting chimeras (PROTAC) are bifunctional molecules that hijack
endogenous E3 ubiquitin ligases to induce ubiquitination and subsequent degradation of …
endogenous E3 ubiquitin ligases to induce ubiquitination and subsequent degradation of …