A synthetic FK-506 Binding Protein (FKBP) ligand
FK-506 is a potent immunosuppressant that forms a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T-cell activation. Synthetic ligand of FKBP (SLF) is a cell-permeable analog of FK-506 that binds tightly to FKBP but lacks the ability to inhibit calcineurin. By itself, SLF does not exhibit a significant cellular response. However, homodimers of SLF or heterodimers with another protein ligand, provide a method to promote the dimerization of ligand-specific fusion proteins to induce signaling events within a cellular environment. For example, SLF monomers connected with a 10-atom linker activates Fas signaling via Fas-FKBP fusion proteins with an EC50 of 6 nM.
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