Gold nanoparticles were conjugated with transferrin molecules for targeting, imaging and therapy of breast cancer cells (Hs578T, ATCC). Results show that, the transferrin-transferrin receptor-mediated cellular uptake of gold nanoparticles is six times of that in the absence of this interaction. As a consequence, the laser power effective for photothermal therapy of the cancer cells was reduced to values of two orders of magnitude lower. To demonstrate the efficiency of the conjugated gold nanoparticles in selectively targeting cancer cells, the cellular uptake of the gold nanoparticles by noncancerous cells (3T3, ATCC) was also investigated. The cellular uptake by the normal cells is only one fourth of that by the cancerous cells indicating that the transferrin-transferrin receptor interaction plays an important role in controlling the cellular uptake of the gold nanoparticles.