188Re (T1/2=16.9h) is an ideal and attractive therapeutic radionuclide (Eβmax=2.11MeV) with emission of γ (Eγ=155keV) suitable for imaging. This paper reviews the methods and progresses in researches on 188Re labeling biomolecules. It is encouraging that 188Re-labeled radiopharmaceuticals have prospective applications in cancer therapy.