The last decade has seen a productive confluence of Biophotonics and Nanotechnology. In particular, photoluminescent nanomaterials, such as fluorescent nanodiamonds (FND), nanorubies and upconversion nanoparticles (UCNP) provide means for imaging biomolecular processes. The exceptional photophysical properties of these nanoparticles push the sensitivity limit to the single biomolecule level. Well-developed surface of these nanoparticles represents a flexible platform, where various surface moieties can be attached, enabling to dock targeting and/or therapeutic biomolecules. These nanoparticle biocomplexes, e.g. FND-(enhanced green fluorescent protein), nanoruby-(opioid receptor ligand), (quantum dot)-somatostatin or UCNP-(mini-antibody) are pieced together to form targeting hybrid nanocomplexes to provide diagnostic capabilities, whereas the attachment of fluorescent proteins generating singlet oxygen (miniSOG) allows treatment of these targeted cellular or biological tissue sites.