Targeted protein degradation: from mechanisms to clinic

JM Tsai, RP Nowak, BL Ebert, ES Fischer - Nature Reviews Molecular …, 2024 - nature.com
Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …

[HTML][HTML] Proteomic approaches advancing targeted protein degradation

G Sathe, GP Sapkota - Trends in pharmacological sciences, 2023 - cell.com
Targeted protein degradation (TPD) is an emerging modality for research and therapeutics.
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …

[HTML][HTML] Antiviral PROTACs: opportunity borne with challenge

J Liang, Y Wu, K Lan, C Dong, S Wu, S Li, HB Zhou - Cell Insight, 2023 - Elsevier
Proteolysis targeting chimera (PROTAC) degradation of pathogenic proteins by hijacking of
the ubiquitin-proteasome-system has become a promising strategy in drug design. The …

Progress in RAS‐targeted therapeutic strategies: From small molecule inhibitors to proteolysis targeting chimeras

X Lu, J Jin, Y Wu, X Liu, X Liang, J Lin… - Medicinal Research …, 2024 - Wiley Online Library
As a widely considerable target in chemical biology and pharmacological research, rat
sarcoma (RAS) gene mutations play a critical driving factor in several fatal cancers. Despite …

HiBiT-SpyTag: A Minimal Tag for Covalent Protein Capture and Degrader Development

T Tsang, F Huerta, Y Liu, J Che, RJ Metivier… - ACS Chemical …, 2023 - ACS Publications
The ability to rapidly and selectively modulate cellular protein levels using small molecules
is essential for studying complex biological systems. Degradation tags, such as dTAG, allow …

Structural and functional annotation of solute carrier transporters: implication for drug discovery

V Dvorak, G Superti-Furga - Expert Opinion on Drug Discovery, 2023 - Taylor & Francis
ABSTRACT Introduction Solute carriers (SLCs) represent the largest group of membrane
transporters in the human genome. They play a central role in controlling the …

[HTML][HTML] Cancer-specific delivery of proteolysis-targeting chimeras (PROTACs) and their application to cancer immunotherapy

Y Moon, SI Jeon, MK Shim, K Kim - Pharmaceutics, 2023 - mdpi.com
Proteolysis-targeting chimeras (PROTACs) are rapidly emerging as a potential therapeutic
strategy for cancer therapy by inducing the degradation of tumor-overexpressing oncogenic …

[HTML][HTML] Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders

C Bouvier, R Lawrence, F Cavallo, W Xolalpa… - Cells, 2024 - mdpi.com
Proteolysis-targeting chimeras (PROTACs) describe compounds that bind to and induce
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …

[HTML][HTML] PROTAC-Based Protein Degradation as a Promising Strategy for Targeted Therapy in Sarcomas

C Mancarella, A Morrione, K Scotlandi - International Journal of …, 2023 - mdpi.com
Sarcomas are heterogeneous bone and soft tissue cancers representing the second most
common tumor type in children and adolescents. Histology and genetic profiling discovered …

Ugi reaction-assisted assembly of covalent PROTACs against glutathione peroxidase 4

L Zhu, S Hu, X Yan, Q Zeng, B Zhang, L Jiang… - Bioorganic …, 2023 - Elsevier
Inducing cell ferroptosis by inactivating glutathione peroxidase 4 (GPX4) is a popular cancer
treatment strategy. However, only few GPX4 inhibitors have been developed to date …