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 …

[HTML][HTML] 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 …

Intracellular delivery of glutathione peroxidase degrader induces ferroptosis in vivo

T Luo, Q Zheng, L Shao, T Ma, L Mao… - Angewandte …, 2022 - Wiley Online Library
Ferroptosis is a new form of regulated, non‐apoptotic cell death driven by iron‐dependent
phospholipid peroxidation. Its therapeutic potential is however, greatly limited by the low …

Developing potent LC3-targeting AUTAC tools for protein degradation with selective autophagy

J Pei, X Pan, A Wang, W Shuai, F Bu, P Tang… - Chemical …, 2021 - pubs.rsc.org
Autophagy-based protein degradation is emerging as a promising technology for anti-
diseases and innovative drug discovery. Here, we demonstrate a novel type of autophagy …

[HTML][HTML] Recent advances in PROTACs for drug targeted protein research

T Yao, H Xiao, H Wang, X Xu - International Journal of Molecular …, 2022 - mdpi.com
Proteolysis-targeting chimera (PROTAC) is a heterobifunctional molecule. Typically,
PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and …

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 …

Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione Derivative Inhibits d-Dopachrome Tautomerase Activity and Suppresses the Proliferation of Non-Small Cell Lung Cancer …

Z Xiao, A Osipyan, S Song, D Chen… - Journal of Medicinal …, 2022 - ACS Publications
The homologous cytokines macrophage migration inhibitory factor (MIF) and d-dopachrome
tautomerase (d-DT or MIF2) play key roles in cancers. Molecules binding to the MIF …

Progress of small molecules for targeted protein degradation: PROTACs and other technologies

HY Zhao, M Xin, SQ Zhang - Drug Development Research, 2023 - Wiley Online Library
Recent years have witnessed the rapid development of targeted protein degradation (TPD),
especially proteolysis targeting chimeras. These degraders have manifested many …

Destabilization of macrophage migration inhibitory factor by 4‐IPP reduces NF‐κB/P‐TEFb complex‐mediated c‐Myb transcription to suppress osteosarcoma …

L Zheng, Z Feng, S Tao, J Gao, Y Lin… - Clinical and …, 2022 - Wiley Online Library
Background As an inflammatory factor and oncogenic driver protein, the pleiotropic cytokine
macrophage migration inhibitory factor (MIF) plays a crucial role in the osteosarcoma …

Discovery of selective platelet-derived growth factor receptor-beta (PDGFR-β) bifunctional small-molecule degraders

R Si, N Liu, J Wang, Q Zhang, Y Li, X Pan… - Bioorganic & Medicinal …, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) is a promising strategy for treatment of various
diseases by degrading of disease-related proteins in recent years. Up to now, most …