Compound class:
Synthetic organic
Comment: YT47R is an experimental PROTAC that targets FKBP12 (via a SLF ligand moiety) to the E3 ligase substrate binding component DCAF1 (via a selective ligand that binds to reactive cysteine C1113 in DCAF1's WD40 repeat domain) [1]. This mediates selective degradation of the FKBP12 protein in in vitro models, and confirms DCAF1 as a novel and targetable E3 ligase component for targeted protein degradation applications.
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References |
1. Tao Y, Remillard D, Vinogradova EV, Yokoyama M, Banchenko S, Schwefel D, Melillo B, Schreiber SL, Zhang X, Cravatt BF. (2022)
Targeted Protein Degradation by Electrophilic PROTACs that Stereoselectively and Site-Specifically Engage DCAF1. J Am Chem Soc, 144 (40): 18688-18699. [PMID:36170674] |