[HTML][HTML] 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 …
[HTML][HTML] 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 …
Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders
Targeted protein degradation is a novel pharmacology established by drugs that recruit
target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target …
target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target …
Hydrogen-bond donors in drug design
PW Kenny - Journal of Medicinal Chemistry, 2022 - ACS Publications
Hydrogen-bond donors are seen to cause more problems for drug designers than hydrogen-
bond acceptors. Most of the polarity in drug-like compounds comes from hydrogen-bond …
bond acceptors. Most of the polarity in drug-like compounds comes from hydrogen-bond …
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 …
Degrader-antibody conjugates
PS Dragovich - Chemical Society Reviews, 2022 - pubs.rsc.org
Degrader-antibody conjugates (DACs) are novel entities that combine a proteolysis
targeting chimera (PROTAC) payload with a monoclonal antibody via some type of chemical …
targeting chimera (PROTAC) payload with a monoclonal antibody via some type of chemical …
Linker-dependent folding rationalizes PROTAC cell permeability
V Poongavanam, Y Atilaw, S Siegel… - Journal of Medicinal …, 2022 - ACS Publications
Proteolysis-targeting chimeras (PROTACs) must be cell permeable to reach their target
proteins. This is challenging as the bivalent structure of PROTACs puts them in chemical …
proteins. This is challenging as the bivalent structure of PROTACs puts them in chemical …
A bibliometric analysis of PROTAC from 2001 to 2021
D Li, D Yu, Y Li, R Yang - European journal of medicinal chemistry, 2022 - Elsevier
Proteolysis targeting chimera (PROTAC) technology, one of the targeted protein degradation
technologies, has drawn marked attention from researchers of both academia and industry …
technologies, has drawn marked attention from researchers of both academia and industry …
Advancing strategies for proteolysis-targeting chimera design
M Li, Y Zhi, B Liu, Q Yao - Journal of medicinal chemistry, 2023 - ACS Publications
Proteolysis-targeting chimeras (PROTACs) have shown great therapeutic potential by
degrading various disease-causing proteins, particularly those related to tumors. Therefore …
degrading various disease-causing proteins, particularly those related to tumors. Therefore …