Recent progress in synthetic and biological studies of GPI anchors and GPI-anchored proteins

•Great progress has been made in revealing GPI and GPI-anchored protein biosynthesis.•Progress in GPI and GPI-anchored protein synthesis has made their access practical.•Synthetic GPIs and GPI-anchored proteins have facilitated the study of GPI biology. Covalent attachment of glycosylphosphatidylinositols (GPIs) to the protein C-terminus is one of the most common posttranslational modifications in eukaryotic cells. In addition to anchoring surface proteins to the cell membrane, GPIs also have many other important biological functions, determined by their unique structure and property. This account has reviewed the recent progress made in disclosing GPI and GPI-anchored protein biosynthesis, in the chemical and chemoenzymatic synthesis of GPIs and GPI-anchored proteins, and in understanding the conformation, organization, and distribution of GPIs in the lipid membrane.