Genes & development
Combinatorial use of VHL and KEAP1 PROTACs reveals unexpected synergy and hook effect relief.
Sehbanul Islam, Haihong Jin, Dong Liu, Dan Lu, Yunkai Zhang, Eric Christenson, Renxu Chang, Joel Austin, Anneliese Faustino, Thomas Beer, Hsin-Yao Tang, Lan Huang, James R Tonra, Luca Busino
Published: 202510.1101/gad.352916.125
Abstract
Proteolysis-targeting chimeras (PROTACs) are bifunctional molecules bridging a protein with an E3 ubiquitin ligase, promoting its ubiquitylation and degradation. However, PROTACs are not without limitations, including suboptimal target degradation an…
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