Sep 2026· Handbook of Experimental Pharmacology· 0 citations
Medicine
TL;DR
This review summarizes the development of classical small-molecule E3 ligase ligands and highlights emerging biological recruitment strategies involving antibodies, nanobodies, aptamers, peptides, and engineered proteins that provide greater programmability and selectivity.
The molecular mechanisms, recent advances, and emerging applications of bioPROTAC technology are summarized, the current technical challenges are evaluated, potential strategies to address these limitations are discussed, and future directions that may facilitate its clinical translation are highlighted.
This review summarizes recent advances in chemical protein degradation strategies for neurodegenerative disorders and highlights potential future perspectives of multifunctional PROTACs for therapeutic development.
Pasquale Degennaro, Imane Ghafir El Idrissi, Rosa Purgatorio et al.· Pharmaceuticals· 0 citations
Proteolysis-targeting chimeras (PROTACs) are promising degraders in targeted protein degradation (TPD) systems. Although more than 600 E3 ubiquitin (Ub) ligases exist in the human genome, only a few E3 ligases have been engaged in PROTACs. It is essential to expand the range of available E3 ligase resources to combat d...
Tokiha Masuda-Ozawa, Shusuke Tomoshige, E. Hayakawa et al.· RSC Chemical Biology· 0 citations
Advances establish PROTAC technology as a transformative platform in modern drug discovery while emphasizing the scientific and translational challenges that must be addressed to enable broader clinical application.
Sandip Badadhe, Vikas B. Gawali, Mahesh D. Bhalsing et al.· Discover Chemistry· 0 citations
KLHL12 is identified as a potentially tumor-selective E3 ligase and the development of the first-in-class KLHL12-recruiting PROTACs are reported, which established KLHL12 as a promising tumor‑selective E3 ligase and provided a KLHL12-recruiting PROTAC platform for cancer therapy.
Shicheng Xu, Xian Zhang, Shun-Bo Hu et al.· Angewandte Chemie· 0 citations
Gaining deeper mechanistic insight into the nature of HyT degradation will be essential to further the potential of HyTDs as powerful tools in cancer research and therapeutics.
