2022年1月5日 · VHL-based PRTOACs have been developed for the treatment of diseases that are difficult to be dealt with by conventional methods, such as radiotherapy, chemotherapy, …

2022年10月10日 · Here, we optimise VHL-based PROTACs to obtain quantifiable oral bioavailability in addition to in vivo efficacy. We also outline structure guided and hypothesis …

2024年12月18日 · Herein we describe a series of nine VHL PROTACs that vary in the structure of their linkers, but have identical POI and VHL ligands, to obtain insight into how the linker may …

2023年9月12日 · PROTACs have expanded as a therapeutic strategy to open new avenues for unmet medical needs. Leveraging our expertise, we undertook a series of in vitro experiments …

2024年2月5日 · The scientific community has shown considerable interest in proteolysis-targeting chimeras (PROTACs) in the last decade, indicating their remarkable p…

2024年3月13日 · After validating VHL engagement by VHL-SF2 both on isolated protein and in intact cells, we synthesized a BRD4-targeted PROTAC, BRD-SF2, incorporating VHL-SF2 and …

2019年1月10日 · Here, we generate isoform-selective PROTACs for the p38 MAPK family using a single warhead (foretinib) and recruited E3 ligase (von Hippel-Lindau). Based on their distinct …

2017年10月10日 · We describe Homo-PROTACs as an approach to dimerize an E3 ligase to trigger its suicide-type chemical knockdown inside cells. We provide proof-of-concept of Homo …

2024年2月5日 · Here, we review the discovery of VHL ligands, the types of linkers employed to develop VHL-based PROTACs, and their subsequent modulation to design advanced non …

2022年1月5日 · We will provide a comprehensive update on the latest research progress in VHL-based PRTOACs area. We also provide our own perspective on the future prospects and …