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: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy

J Gao, B Hou, Q Zhu, L Yang, X Jiang, Z Zou… - Nature …, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) has been exploited to degrade
putative protein targets. However, the antitumor performance of PROTACs is impaired by …

Smart nano‐PROTACs reprogram tumor microenvironment for activatable photo‐metabolic cancer immunotherapy

C Zhang, S He, Z Zeng, P Cheng… - Angewandte Chemie …, 2022 - Wiley Online Library
Protease inhibitors can modulate intratumoral metabolic processes to reprogram the
immunosuppressive tumor microenvironment (TME), which however suffer from the limited …

Bioorthogonal PROTAC prodrugs enabled by on-target activation

M Chang, F Gao, D Pontigon, G Gnawali… - Journal of the …, 2023 - ACS Publications
Although proteolysis targeting chimeras (PROTACs) have become promising therapeutic
modalities, important concerns exist about the potential toxicity of the approach owing to …

Radiotherapy-triggered proteolysis targeting chimera prodrug activation in tumors

C Yang, Y Yang, Y Li, Q Ni, J Li - Journal of the American …, 2022 - ACS Publications
Proteolysis targeting chimera (PROTAC) is an emerging protein degradation strategy, which
shows excellent advantages in targeting those so-called “undruggable” proteins. However …

Self-assembled nano-PROTAC enables near-infrared photodynamic proteolysis for cancer therapy

W Wang, C Zhu, B Zhang, Y Feng… - Journal of the American …, 2023 - ACS Publications
Confining the protein degradation activity of proteolysis-targeting chimera (PROTAC) to
cancer lesions ensures precision treatment. However, it still remains challenging to precisely …

Aptamer-based targeted protein degradation

Y Liu, X Qian, C Ran, L Li, T Fu, D Su, S Xie, W Tan - ACS nano, 2023 - ACS Publications
The selective removal of misfolded, aggregated, or aberrantly overexpressed protein plays
an essential role in maintaining protein-dominated biological processes. In parallel, the …

A bibliometric analysis of PROTAC from 2001 to 2021

D Li, D Yu, Y Li, R Yang - European journal of medicinal chemistry, 2022 - Elsevier
Proteolysis targeting chimera (PROTAC) technology, one of the targeted protein degradation
technologies, has drawn marked attention from researchers of both academia and industry …

Proteolysis-targeting chimera (PROTAC) delivery system: advancing protein degraders towards clinical translation

Y Chen, I Tandon, W Heelan, Y Wang… - Chemical Society …, 2022 - pubs.rsc.org
Proteolysis Targeting Chimeras (PROTACs), an emerging therapeutic entity designed to
degrade target proteins by hijacking the ubiquitin–proteasome system, have the potential to …