In　this　review,　various　strategies　for　artificial　regulation　of　receptor　clustering　on　cell　surface　are　introduced,　which　are　realized　either　by　physical-stimulations　or　biological　macromolecules.　The　former　one　is　induced　by　stimuli-responsive　nanomaterials　under　physical　stimulation,　such　as　light,　magnetic　field,　and　heat.　And　the　later　one　is　achieved　by　utilizing　the　self-assembly　of　biomolecules　including　protein,　peptide　or　nucleic　acids,　thus　inducing　artificial　regulation　of　their　targeting　receptor.　We　aim　to　systematically　introduce　advances　in　this　area　and　provide　insights　into　the　existing　challenges　and　future　perspectives.　©　2020,　Higher　Education　Press.　All　right　reserved.