Promising application of gold nanoparticles (GNPs) in biomedical and environmental fields is increasing the likelihood of direct interaction with living systems. The knowledge about GNPs interacting with cells is quite limited and however, is necessary for risk prediction and evaluation of biological effects. Herein, we review recent advances in cellular effects of GNPs including cellular uptake, trafficking, subcellular distribution and cellular responses, and the relationship between physiochemical properties of GNPs and biological effects as well. To uncover these issues, it is quite instructive for safe and sustainable use of GNPs.