PROTAC targeted protein degraders: the past is prologue
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 …
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 …
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
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 …
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 …
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 …
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 …
environment within the cell. However, when natural proteostasis mechanisms are …
Recent developments in PROTAC‐mediated protein degradation: from bench to clinic
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
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 …
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
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed for …
degrading disease-causing proteins. While many PROTACs have been developed for …