Today, nanomaterials have been considered as highly promising functional materials for various applications, impacting virtually all the fields of science and technologies. Functional nanoparticles (NPs), as one of the most important nanomaterials, are playing significantly important roles in some emerging research topics, such as biomedicine and biosensing. Among numerous NPs, gold NPs (AuNPs) with diverse shapes, such as rods, shells, and cages, have attracted increasing attention due to their unique properties of biocompatibility, absorption/scattering, and facile conjugation with a large variety of biomolecules. Recent advances in synthetic chemistry render the fabrication of AuNPs with precise control over physicochemical and optical properties, which are highly desired for specific clinical or biological applications, leading to remarkable achievements in the research field of biology and medicine. In this article, we briefly summarize the preparation of the AuNPs and their most recent advances in biology and medicine.