Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules

Behnam Nabet (), Fleur M. Ferguson, Bo Kyung A. Seong, Miljan Kuljanin, Alan L. Leggett, Mikaela L. Mohardt, Amanda Robichaud, Amy S. Conway, Dennis L. Buckley, Joseph D. Mancias, James E. Bradner, Kimberly Stegmaier and Nathanael S. Gray ()
Additional contact information
Behnam Nabet: Dana-Farber Cancer Institute
Fleur M. Ferguson: Dana-Farber Cancer Institute
Bo Kyung A. Seong: Dana-Farber Cancer Institute
Miljan Kuljanin: Dana-Farber Cancer Institute
Alan L. Leggett: Dana-Farber Cancer Institute
Mikaela L. Mohardt: Dana-Farber Cancer Institute
Amanda Robichaud: Dana-Farber Cancer Institute
Amy S. Conway: Dana-Farber Cancer Institute
Dennis L. Buckley: Dana-Farber Cancer Institute
Joseph D. Mancias: Dana-Farber Cancer Institute
James E. Bradner: Dana-Farber Cancer Institute
Kimberly Stegmaier: Dana-Farber Cancer Institute
Nathanael S. Gray: Dana-Farber Cancer Institute

Nature Communications, 2020, vol. 11, issue 1, 1-8

Abstract: Abstract 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 dTAGV-1, an exclusively selective VHL-recruiting dTAG molecule, to rapidly degrade FKBP12F36V-tagged proteins. dTAGV-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.

Date: 2020
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DOI: 10.1038/s41467-020-18377-w

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