Shield-1

Shield-1 is a protein stabilizing ligand that prevents the proteosomal degradation of proteins fused to FK-506 binding protein 1A (FKBP12) containing a leucine-to-proline substitution at position 106 (FKBP12^L106P).¹ It displays specific binding for the destabilizing domain FKBP12^L106P and does not interfere with other measured cell processes. Shield-1 inhibits decreases in fluorescence in NIH3T3 cells stably expressing YFP-FKBP12^L106P in a concentration-dependent manner. It increases secretion of IL-2-FKBP12^L106P in HCT116 cells stably expressing IL-2-FKBP12^L106P when used at a concentration of 1 µM.² In vivo, shield-1 (5 and 10 mg/kg every two days) reduces tumor volume in a mouse xenograft model using HCT116 cells stably expressing IL-2-FKBP12^L106P.

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1. Banaszynski, L.A., Chen, L.-c., Maynard-Smith, L.A., et al. A rapid, reversible, and tunable method to regulate protein function in living cells using synthetic small molecules. Cell 126(5), 995-1004 (2006).

2. Banaszynski, L.A., Sellmyer, M.A., Contag, C.H., et al. Chemical control of protein stability and function in living mice. Nat. Med. 14(10), 1123-1127 (2008).