Hydrogen Peroxide‐Inducible PROTACs for Targeted Protein Degradation in Cancer Cells

D Yu, H Fan, Z Zhou, Y Zhang, J Sun, L Wang… - …, 2023 - Wiley Online Library
Proteolysis‐targeting chimeras (PROTACs) provide a powerful technique to degrade
targeted proteins utilizing the cellular ubiquitin‐proteasome system. The major concern is …

Click chemistry in the development of PROTACs

C Yang, R Tripathi, B Wang - RSC Chemical Biology, 2024 - pubs.rsc.org
Proteolysis-targeting chimeras or PROTACs are hetero-bifunctional molecules designed to
mediate the disposal of a target protein via recruitment of the ubiquitination–proteasome …

High-throughput cellular profiling of targeted protein degradation compounds using HiBiT CRISPR cell lines

KM Riching, SD Mahan, M Urh, DL Daniels - JoVE (Journal of Visualized …, 2020 - jove.com
Targeted protein degradation compounds, including molecular glues or proteolysis targeting
chimeras, are an exciting new therapeutic modality in small molecule drug discovery. This …

iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells

H Bouguenina, S Nicolaou, YV Le Bihan, EA Bowling… - Iscience, 2023 - cell.com
To address the limitation associated with degron based systems, we have developed iTAG,
a synthetic tag based on IMiDs/CELMoDs mechanism of action that improves and addresses …

Targeted protein degradation

P Zhou - Current opinion in chemical biology, 2005 - Elsevier
The ubiquitin-proteasome pathway plays a major role in cellular protein destruction and
regulates fundamental cellular processes such as the cell cycle, cell signaling, and …

Specific non-genetic IAP-based protein erasers (SNIPERs) as a potential therapeutic strategy

Z Ma, Y Ji, Y Yu, D Liang - European journal of medicinal chemistry, 2021 - Elsevier
As a newly emerged technology, PROTAC (proteolysis targeting chimera) is a promising
therapeutic strategy for varieties of diseases. Unlike small molecule inhibitors, PROTACs …

Harnessing the E3 ligase KEAP1 for targeted protein degradation

J Wei, F Meng, KS Park, H Yim, J Velez… - Journal of the …, 2021 - ACS Publications
Proteolysis targeting chimeras (PROTACs) represent a new class of promising therapeutic
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …

Targeted protein degradation and drug discovery

M Naito - The Journal of Biochemistry, 2022 - academic.oup.com
Targeted protein degradation attracts attention as a novel modality for drug discovery, as
well as for basic research. Various types of degrader molecules have been developed so …

Development of Protacs to target cancer-promoting proteins for ubiquitination and degradation

KM Sakamoto, KB Kim, R Verma, A Ransick… - Molecular & Cellular …, 2003 - ASBMB
The proteome contains hundreds of proteins that in theory could be excellent therapeutic
targets for the treatment of human diseases. However, many of these proteins are from …

Receptor elimination by E3 ubiquitin ligase recruitment (REULR): a targeted protein degradation toolbox

DH Siepe, LK Picton, KC Garcia - ACS synthetic biology, 2023 - ACS Publications
In recent years, targeted protein degradation (TPD) of plasma membrane proteins by
hijacking the ubiquitin proteasome system (UPS) or the lysosomal pathway has emerged as …