The earliest reported small molecule-based strategies involved conjugation of naphthalene acylsulfonamide or phosphate ester-based tags to improve in vivo half-lives of peptide anticoagulants.95,96 More recent strategies have mostly focussed on improving the in vivo pharmacokinetic properties of Glucagon like peptide-1 (GLP-1) analogues, such as extendin-4, which are used in the treatment of type 2 diabetes. The gene discussed is GCG; the disease is type 2 diabetes mellitus.