In this review, the authors' works published within the past 5 years devoted to the development of bifunctional hybrid nanostructures based on the targeting polypeptides and nanoparticles of various origin (quantum dots, nanogold, nanodiamonds, upconversion nanoparticles, magnetic and polymer nanoparticles) as modules that ensure visualization and various damaging effects on cancer cells are surveyed and the prospects of their application in theranostics and precision medicine have been contemplated.