Chemical biology strategies for directly perturbing protein homeostasis including the degradation tag (dTAG) system provide temporal advantages over genetic approaches and improved selectivity over small molecule inhibitors. We describe dTAG-1, an exclusively selective VHL-recruiting dTAG molecule, to rapidly degrade FKBP12-tagged proteins. dTAG-1 overcomes a limitation of previously reported CRBN-recruiting dTAG molecules to degrade recalcitrant oncogenes, supports combination degrader studies and facilitates investigations of protein function in cells and mice.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7501296PMC
http://dx.doi.org/10.1038/s41467-020-18377-wDOI Listing

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