Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules
抄録
<jats:title>Abstract</jats:title><jats:p>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<jats:sup>V</jats:sup>-1, an exclusively selective VHL-recruiting dTAG molecule, to rapidly degrade FKBP12<jats:sup>F36V</jats:sup>-tagged proteins. dTAG<jats:sup>V</jats:sup>-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.</jats:p>
収録刊行物
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- Nature Communications
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Nature Communications 11 (1), 4687-, 2020-09-18
Springer Science and Business Media LLC