AP1867

AP1867 (FK506-binding protein) is a synthetic FKBP12 F36V-directed ligand attached to 320 substituted tetrahydrooxazepines (THOXs) . AP1867 (FK506-binding protein) was synthesized via combined liquid- and solid-phase methods employing sequential Mitsunobu displacements followed by ruthenium-mediated olefin metathesis to close seven-membered rings; the resin-bound THOX ligands were coupled to AP1867 in parallel, yielding candidate heterodimerizers that demonstrated membrane permeability and bioactivity in human fibrosarcoma cells, facilitating the study of targeted protein interactions and intracellular modulation.