Photoactivatable Prolyl Hydroxylase 2 Inhibitors for Stabilizing the Hypoxia-Inducible Factor with Light

HIF prolyl hydroxylase 2 (PHD2) inhibitors
represent a novel approach for treating HIF-related diseases. This
study reports the first application of photoremovable protecting group
to the photoactivatable inhibitor (7) of PHD2. It allows
the inhibitory activity for PHD2 to be controlled by light irradiation,
subsequently stabilizing HIF and promoting expression of the target
gene. Light activation to stabilize HIF offers promising potentials
for the tissue-specific therapies for HIF-related disease by light
irradiation onto target tissues.