VHL binders and their functionalized analogs
The VHL E3 ligase, a member of the Cullin-RING E3 ubiquitin ligase family, is responsible for the ubiquitination and subsequent proteasomal degradation of specific substrates, including HIF-α. PROTACs, heterobifunctional molecules, exploit this cellular machinery by recruiting target proteins to the E3 ligase, leading to their ubiquitination and degradation. The development of effective PROTACs relies on the availability of high-affinity small-molecule ligands that can bind to E3 ligases with high specificity.
With years of experience in VHL chemistry, our team has a deep understanding of this field. Our chemists continuously innovate, designing and synthesizing novel Building Blocks and exploring creative modifications of key intermediates. Leveraging this expertise, we’ve enumerated a REAL space of over 8 million VHL-targeted compounds, which can be rapidly synthesized within 4 weeks with an impressive 80% success rate. Also, we are offering ready-to-use VHL ligand-linkers conjugate kits – sets with well-balanced linkers and common VHL binders to support your discoveries.
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Examples of in-stock VHL binders
Selected publications
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Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders.
Diehl C., Ciulli A. Chem. Soc. Rev. 2022, 51, 8216. DOI: 10.1039/D2CS00387B
