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 …

PROTAC targeted protein degraders: the past is prologue

M Békés, DR Langley, CM Crews - Nature Reviews Drug Discovery, 2022 - nature.com
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …

Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

CJ Diehl, A Ciulli - Chemical Society Reviews, 2022 - pubs.rsc.org
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

The therapeutic potential of targeting regulated non-apoptotic cell death

K Hadian, BR Stockwell - Nature Reviews Drug Discovery, 2023 - nature.com
Cell death is critical for the development and homeostasis of almost all multicellular
organisms. Moreover, its dysregulation leads to diverse disease states. Historically …

TF-PROTACs enable targeted degradation of transcription factors

J Liu, H Chen, HU Kaniskan, L Xie… - Journal of the …, 2021 - ACS Publications
Transcription factors (TFs) represent a major class of therapeutic targets for the treatment of
human diseases including cancer. Although the biological functions and even crystal …

[PDF][PDF] Targeted protein degradation: A promise for undruggable proteins

KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …

Recent developments in PROTAC‐mediated protein degradation: from bench to clinic

Z Hu, CM Crews - ChemBioChem, 2022 - Wiley Online Library
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …

c-Myc-targeting PROTAC based on a TNA-DNA bivalent binder for combination therapy of triple-negative breast cancer

X Li, Z Zhang, F Gao, Y Ma, D Wei, Z Lu… - Journal of the …, 2023 - ACS Publications
Triple-negative breast cancer (TNBC) is highly aggressive with a poor clinical prognosis and
no targeted therapy. The c-Myc protein is a master transcription factor and a potential …

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 …