[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review

RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …

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 …

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 …

Natural product-based proteolysis targeting chimeras (PROTACs)

M Liu, AP Martyn, RJ Quinn - Natural Product Reports, 2022 - pubs.rsc.org
Covering: upto 2022 Natural products have an embedded recognition of protein surfaces.
They possess this property as they are produced by biosynthetic enzymes and are …

Assays and technologies for developing proteolysis targeting chimera degraders

X Liu, X Zhang, D Lv, Y Yuan, G Zheng… - Future Medicinal …, 2020 - Taylor & Francis
Targeted protein degradation by small-molecule degraders represents an emerging mode of
action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules …

Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

Y Zhong, F Chi, H Wu, Y Liu, Z Xie, W Huang… - European journal of …, 2022 - Elsevier
Targeted protein degradation technology has evolved a brand-new therapeutic modality
from an innovative drug discovery perspective. Though the classical PROTACs has …

A platform for the rapid synthesis of proteolysis targeting chimeras (Rapid-TAC) under miniaturized conditions

L Guo, Y Zhou, X Nie, Z Zhang, Z Zhang, C Li… - European journal of …, 2022 - Elsevier
Proteolysis targeting chimera (PROTAC) is one of the most frequently used technologies for
targeted protein degradation. PROTACs are composed of target protein ligand, E3 ligase …

The PROTAC technology in drug development

Y Zou, D Ma, Y Wang - Cell biochemistry and function, 2019 - Wiley Online Library
Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been
developed for inducing the protein degradation by a targeting molecule. This technology …

Targeted protein modification as a paradigm shift in drug discovery

R Amirian, MA Badrbani, Z Izadi, H Samadian… - European Journal of …, 2023 - Elsevier
Abstract Targeted Protein Modification (TPM) is an umbrella term encompassing numerous
tools and approaches that use bifunctional agents to induce a desired modification over the …

Homobivalent, trivalent, and covalent PROTACs: emerging strategies for protein degradation

J Yan, T Li, Z Miao, P Wang, C Sheng… - Journal of medicinal …, 2022 - ACS Publications
Proteolysis-targeting chimeras (PROTACs) is a fast-growing technology providing many
strengths over inhibition of protein activity directly and is attracting increasing interest in new …