Optimization of PROTAC ternary complex using DNA encoded library approach

Q Chen, C Liu, W Wang, X Meng, X Cheng… - ACS Chemical …, 2023 - ACS Publications
The proteolysis targeting chimera (PROTAC) strategy results in the down-regulation of
unwanted protein (s) for disease treatment. In the PROTAC process, a heterobifunctional …

Protac-induced protein degradation in drug discovery: breaking the rules or just making new ones?

I Churcher - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted protein degradation, using bifunctional small molecules (Protacs) to remove
specific proteins from within cells, has emerged as a novel drug discovery strategy with the …

[HTML][HTML] Recent advances in PROTACs for drug targeted protein research

T Yao, H Xiao, H Wang, X Xu - International Journal of Molecular …, 2022 - mdpi.com
Proteolysis-targeting chimera (PROTAC) is a heterobifunctional molecule. Typically,
PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and …

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 …

Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets

Y Xiong, Y Zhong, H Yim, X Yang, KS Park… - Journal of the …, 2022 - ACS Publications
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed for …

Targeted protein degradation directly engaging lysosomes or proteasomes

J Kim, I Byun, H Joh, HJ Kim, MJ Lee - Chemical Society Reviews, 2024 - pubs.rsc.org
Targeted protein degradation (TPD) has been established as a viable alternative to
attenuate the function of a specific protein of interest in both biological and clinical contexts …

Cancer selective target degradation by folate-caged PROTACs

J Liu, H Chen, Y Liu, Y Shen, F Meng… - Journal of the …, 2021 - ACS Publications
PROTACs (proteolysis targeting chimeras) are an emerging class of promising therapeutic
modalities that degrade intracellular protein targets by hijacking the cellular ubiquitin …

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

S Zeng, W Huang, X Zheng, Z Zhang, J Wang… - European journal of …, 2021 - Elsevier
Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …

PROTAC-DB 2.0: an updated database of PROTACs

G Weng, X Cai, D Cao, H Du, C Shen… - Nucleic acids …, 2023 - academic.oup.com
Proteolysis targeting chimeras (PROTACs), which harness the ubiquitin-proteasome system
to selectively induce targeted protein degradation, represent an emerging therapeutic …

Emerging new concepts of degrader technologies

Y Ding, Y Fei, B Lu - Trends in Pharmacological Sciences, 2020 - cell.com
Traditional drug discovery focuses on identifying direct inhibitors of target proteins. This
typically relies on a measurable biochemical readout and accessible binding sites whose …