A “click chemistry platform” for the rapid synthesis of bispecific molecules for inducing protein degradation
RP Wurz, K Dellamaggiore, H Dou… - Journal of medicinal …, 2018 - ACS Publications
Proteolysis targeting chimeras (PROTACs) are bispecific molecules containing a target
protein binder and an ubiquitin ligase binder connected by a linker. By recruiting an …
protein binder and an ubiquitin ligase binder connected by a linker. By recruiting an …
[HTML][HTML] Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs
Abstract The von Hippel-Lindau (VHL) and cereblon (CRBN) proteins are substrate
recognition subunits of two ubiquitously expressed and biologically important Cullin RING …
recognition subunits of two ubiquitously expressed and biologically important Cullin RING …
Impact of target warhead and linkage vector on inducing protein degradation: comparison of bromodomain and extra-terminal (BET) degraders derived from …
KH Chan, M Zengerle, A Testa… - Journal of medicinal …, 2018 - ACS Publications
The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule
approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 …
approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 …
Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead
RP Nowak, L Ragosta, F Huerta, H Liu… - RSC Chemical …, 2023 - pubs.rsc.org
Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras
(PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described …
(PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described …
Lessons in PROTAC design from selective degradation with a promiscuous warhead
Inhibiting protein function selectively is a major goal of modern drug discovery. Here, we
report a previously understudied benefit of small molecule proteolysis-targeting chimeras …
report a previously understudied benefit of small molecule proteolysis-targeting chimeras …
Reversible assembly of proteolysis targeting chimeras
PROteolysis TArgeting Chimeras (PROTACs) are of significant current interest for the
development of probe molecules and drug leads. However, they suffer from certain …
development of probe molecules and drug leads. However, they suffer from certain …
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 …
E3 ligase ligands for PROTACs: how they were found and how to discover new ones
T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …
a new modality of chemical tools and potential therapeutics to understand and treat human …
Harnessing the E3 ligase KEAP1 for targeted protein degradation
Proteolysis targeting chimeras (PROTACs) represent a new class of promising therapeutic
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …
Modular PROTAC design for the degradation of oncogenic BCR‐ABL
AC Lai, M Toure, D Hellerschmied… - Angewandte Chemie …, 2016 - Wiley Online Library
Abstract Proteolysis Targeting Chimera (PROTAC) technology is a rapidly emerging
alternative therapeutic strategy with the potential to address many of the challenges …
alternative therapeutic strategy with the potential to address many of the challenges …