Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications

Q Li, L Zhou, S Qin, Z Huang, B Li, R Liu… - European Journal of …, 2023 - Elsevier
The success of inhibitor-based therapeutics is largely constrained by the acquisition of
therapeutic resistance, which is partially driven by the undruggable proteome. The …

PROTACs: current trends in protein degradation by proteolysis-targeting chimeras

J Madan, VK Ahuja, K Dua, S Samajdar… - BioDrugs, 2022 - Springer
In the recent past, proteolysis-targeting chimera (PROTAC) technology has received
enormous attention for its ability to overcome the limitations of protein inhibitors and its …

[HTML][HTML] PROteolysis TArgeting Chimeras (PROTACs)—past, present and future

M Pettersson, CM Crews - Drug Discovery Today: Technologies, 2019 - Elsevier
The majority of currently used therapeutics are small molecule-based and utilize occupancy-
driven pharmacology as the mode of action (MOA), in which the protein function is …

Proteolysis-targeting chimeras for targeting protein for degradation

J Qi, G Zhang - Future Medicinal Chemistry, 2019 - Taylor & Francis
Proteolysis-targeting chimeras (PROTACs) are an emerging tool for therapeutic intervention
by reducing or eliminating disease-causing proteins. PROTACs are bifunctional molecules …

PROTACS: a technology with a gold rush-like atmosphere

YW Wang, L Lan, M Wang, JY Zhang, YH Gao… - European Journal of …, 2023 - Elsevier
Abnormally expressed or malfunctioning proteins may affect or even damage cells, leading
to the onset of diseases. Proteolysis targeting chimera (PROTAC) technology has been …

PROTACs: past, present and future

K Li, CM Crews - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …

PROTACs to address the challenges facing small molecule inhibitors

P Martín-Acosta, X Xiao - European journal of medicinal chemistry, 2021 - Elsevier
Small molecule inhibitors of proteins represent important medicines and critical chemical
tools to investigate the biology of the target proteins. Advances in various-omics …

[引用][C] Proteolysis targeting chimera (PROTAC): a paradigm-shifting approach in small molecule drug discovery

P Wang, J Zhou - Current topics in medicinal chemistry, 2018 - ingentaconnect.com
Great success has been achieved in small molecule drug discovery programs, making
extraordinary contributions for human health, especially in targeted therapy. Taking …

From classic medicinal chemistry to state‐of‐the‐art interdisciplinary medicine: Recent advances in proteolysis‐targeting chimeras technology

X Zhao, Y Chen, H Su, L Zhang - Interdisciplinary Medicine, 2023 - Wiley Online Library
Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD)
technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells. A …

Targeted protein degradation: expanding the toolbox

M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …