Structural basis of PROTAC cooperative recognition for selective protein degradation
Inducing macromolecular interactions with small molecules to activate cellular signaling is a
challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that …
challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that …
SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate
MJ Roy, S Winkler, SJ Hughes, C Whitworth… - ACS chemical …, 2019 - ACS Publications
Bifunctional degrader molecules, known as proteolysis-targeting chimeras (PROTACs),
function by recruiting a target to an E3 ligase, forming a target/PROTAC/ligase ternary …
function by recruiting a target to an E3 ligase, forming a target/PROTAC/ligase ternary …
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 …
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
S Imaide, KM Riching, N Makukhin, V Vetma… - Nature chemical …, 2021 - nature.com
Bivalent proteolysis-targeting chimeras (PROTACs) drive protein degradation by
simultaneously binding a target protein and an E3 ligase and forming a productive ternary …
simultaneously binding a target protein and an E3 ligase and forming a productive ternary …
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
Abstract PROteolysis-TArgeting Chimeras (PROTACs) are hetero-bifunctional molecules
that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted …
that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted …
Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation
RP Wurz, H Rui, K Dellamaggiore… - Nature …, 2023 - nature.com
Targeted protein degradation via “hijacking” of the ubiquitin-proteasome system using
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
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 …
Targeted protein degradation via intramolecular bivalent glues
O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida… - Nature, 2024 - nature.com
Targeted protein degradation is a pharmacological modality that is based on the induced
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …
PROTAC-mediated crosstalk between E3 ligases
C Steinebach, H Kehm, S Lindner, LP Vu… - Chemical …, 2019 - pubs.rsc.org
Small-molecule heterobifunctional degraders can effectively control protein levels and are
useful research tools. We assembled proteolysis targeting chimeras (PROTACs) from a …
useful research tools. We assembled proteolysis targeting chimeras (PROTACs) from a …
[HTML][HTML] Bivalent ligands for protein degradation in drug discovery
M Scheepstra, KFW Hekking, L van Hijfte… - Computational and …, 2019 - Elsevier
Targeting the “undruggable” proteome remains one of the big challenges in drug discovery.
Recent innovations in the field of targeted protein degradation and manipulation of the …
Recent innovations in the field of targeted protein degradation and manipulation of the …