Proteolysis-targeting chimeras (PROTACs) in cancer therapy
X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …
proteasome system that recruits substrates such as the hypoxia inducible factor for …
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 …
Recent developments in PROTAC‐mediated protein degradation: from bench to clinic
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
Human protein tyrosine phosphatase 1B (PTP1B): from structure to clinical inhibitor perspectives
R Liu, C Mathieu, J Berthelet, W Zhang… - International Journal of …, 2022 - mdpi.com
Phosphorylation is an essential process in biological events and is considered critical for
biological functions. In tissues, protein phosphorylation mainly occurs on tyrosine (Tyr) …
biological functions. In tissues, protein phosphorylation mainly occurs on tyrosine (Tyr) …
PROTAC degraders as chemical probes for studying target biology and target validation
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …
emerged as new promising pharmacological modalities and the first PROTAC drug …
Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity
VG Klein, AG Bond, C Craigon… - Journal of medicinal …, 2021 - ACS Publications
Criteria for predicting the druglike properties of “beyond Rule of 5” Proteolysis Targeting
Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often …
Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often …
From conception to development: investigating PROTACs features for improved cell permeability and successful protein degradation
C Cecchini, S Pannilunghi, S Tardy… - Frontiers in …, 2021 - frontiersin.org
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional degraders that
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
Solution conformations shed light on PROTAC cell permeability
Y Atilaw, V Poongavanam… - ACS Medicinal …, 2020 - ACS Publications
Proteolysis targeting chimeras (PROTACs) induce intracellular degradation of target
proteins. Their bifunctional structure puts degraders in a chemical space where ADME …
proteins. Their bifunctional structure puts degraders in a chemical space where ADME …