PROTACs: A novel strategy for cancer drug discovery and development

X Han, Y Sun - MedComm, 2023 - Wiley Online Library
Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug
discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists …

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 …

Revolutionizing drug targeting strategies: integrating artificial intelligence and structure-based methods in PROTAC development

Danishuddin, MS Jamal, KS Song, KW Lee, JJ Kim… - Pharmaceuticals, 2023 - mdpi.com
PROteolysis TArgeting Chimera (PROTAC) is an emerging technology in chemical biology
and drug discovery. This technique facilitates the complete removal of the target proteins …

Small-molecule PROTACs: novel agents for cancer therapy

Y Wan, C Yan, H Gao, T Liu - Future medicinal chemistry, 2020 - Taylor & Francis
Proteolysis-targeting chimera (PROTAC) is a new technology to selectively degrade target
proteins via ubiquitin-proteasome system. PROTAC molecules (PROTACs) are a class of …

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 …

Discovery of E3 ligase ligands for target protein degradation

J Lee, Y Lee, YM Jung, JH Park, HS Yoo, J Park - Molecules, 2022 - mdpi.com
Target protein degradation has emerged as a promising strategy for the discovery of novel
therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a …

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 …

[HTML][HTML] The impact of E3 ligase choice on PROTAC effectiveness in protein kinase degradation

T Sobierajski, J Małolepsza, M Pichlakb… - Drug Discovery …, 2024 - Elsevier
Proteolysis targeting chimera (PROTACs) provide a novel therapeutic approach that is
revolutionizing drug discovery. The success of PROTACs largely depends on the …

[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 …

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 …