abstract |
The present invention provides a method of increasing in vivo half-life and stability of drugs by forming in vivo conjugation between disulfanyl group of modified bioactive substances and serum protein, especially free thiol group (Cys34) of serum albumin, i.e., 'new stable disulfide (S-S) covalent bond'. The invention provides efficient in vitro analysis methods capable of showing that the designed disulfanyl group is conjugated with serum protein in qualitative and quantitative ways. The invention provides a method of suitably designing bioactive substances on molecular level so that the bioactive substances and blood proteins can be efficiently in vivo conjugated via a disulfide covalent bond. The invention provides specific pharmacological treatment effects and treatment methods using the modified bioactive substances. |