Opportunities and challenges of protein-based targeted protein degradation

L Dassama, F Shen - Chemical Science, 2023 - pubs.rsc.org
In the 20 years since the first report of a proteolysis targeting chimeric (PROTAC) molecule,
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …

Advancement of targeted protein degradation strategies as therapeutics for undruggable disease targets

MP Kannan, S Sreeraman, CS Somala… - Future Medicinal …, 2023 - Future Science
Targeted protein degradation (TPD) aids in developing novel bifunctional small-molecule
degraders and eliminates proteins of interest. The TPD approach shows promising results in …

Repurposing an endogenous degradation domain for antibody-mediated disposal of cell-surface proteins

J Schmitt, E Poole, I Groves, DJ Owen, SC Graham… - EMBO …, 2024 - embopress.org
The exquisite specificity of antibodies can be harnessed to effect targeted degradation of
membrane proteins. Here, we demonstrate targeted protein removal utilising a protein …

Transferrin Receptor Targeting Chimeras (TransTACs) for Membrane Protein Degradation

D Zhang, J Duque-Jimenez, G Brixi, F Facchinetti… - BioRxiv, 2023 - biorxiv.org
Cancer cells require high levels of iron for rapid proliferation, leading to a significant
upregulation of the iron carrier protein Transferrin Receptor (TfR) on their cell surface …

[HTML][HTML] Targeted protein degradation: A promising approach for cancer treatment

MZI Khan, A Nazli, I Naz, D Khan, I Haq… - Journal of Pharmaceutical …, 2023 - Elsevier
Targeted protein degradation (TPD) is a promising approach that has the ability to address
disease-causing proteins. Compared to traditional inhibition, proteolysis targeting chimera …

Redirecting the specificity of tripartite motif containing-21 scaffolds using a novel discovery and design approach

D VanDyke, L Xu, PR Sargunas, RN Gilbreth… - Journal of Biological …, 2023 - ASBMB
Hijacking the ubiquitin proteasome system to elicit targeted protein degradation (TPD) has
emerged as a promising therapeutic strategy to target and destroy intracellular proteins at …

Discovery of SOCS7 as a versatile E3 ligase for protein-based degraders

A Cornebois, M Sorbara, M Cristol, E Vigne… - Iscience, 2024 - cell.com
Targeted protein degradation (TPD) strategy harnesses the ubiquitin-proteasome system
(UPS) to degrade a protein of interest (POI) by bringing it into proximity with an E3 ubiquitin …

Genetically-encoded degraders as versatile modulators of intracellular therapeutic targets

C Dai, J Wang, L Tu, Z Pan, J Yang, S Zhou… - Current Opinion in …, 2023 - Elsevier
Targeted protein degradation (TPD) is an emerging therapeutic approach that has attracted
significant interest. The traditional TPD degraders rely on small molecules that can only …

TAC‐tics for Leveraging Proximity Biology in Drug Discovery

DA Nalawansha, K Mangano, W den Besten… - …, 2024 - Wiley Online Library
Chemically induced proximity (CIP) refers to co‐opting naturally occurring biological
pathways using synthetic molecules to recruit neosubstrates that are not normally …