Here, we combined selective subcellular and receptor-mediated drug delivery strategies with the view of improving the potency and the selectivity of a series of proapoptotic peptides towards mammalian cells (Figure ). Cyanine dyes 1 and 2 (Figure ) and folate were chemically conjugated to the N-terminus of three proapoptotic peptides (3-5) to yield conjugates 6-15 (Table ).