Design and application of light-activated probes for cellular signaling

Multiple reports have described the presence of functional G protein-coupled receptors (GPCRs) in the perinuclear/nuclear membranes of many cell types where they are able to modulate nuclear Ca(2+) influx, transcription initiation, and gene expression. Because GPCRs represent "some of the most promising targets for drug development" a better understanding of their roles, not only at the cell membrane but also at the nuclear level, in healthy and disease states, will certainly generate new avenues for therapeutic intervention. The photo-triggered release of biologically active compounds has been regarded as one of the most effective methods for inducing an in vitro-controlled biochemical or physiological response. Here, we describe various methodologies and alternatives related to the conception of inert biologically active peptides through the incorporation of photo-triggered groups at key positions of the native peptide sequence.