Light-cleavable rapamycin dimer as an optical trigger for protein dimerizationElectronic supplementary information (ESI) available: Molecular dynamics simulations, synthetic and biological protocols. See DOI: 10.1039/c4cc09442e

Rapamycin-induced protein heterodimerization of FKBP12 and FRB is one of the most commonly employed switches to conditionally control biological processes. We developed an optically activated rapamycin dimer that does not induce FKBP12-FRB dimerization until exposed to light, and applied it to control kinase, protease, and recombinase function. Protein heterodimerization of FKBP12 and FRB can be optically controlled with a photocleavable rapamycin dimer.