Site Specific Biotinylation of Endothelin-1: Potential Use for Characterization of Endothelin-Receptor Populations,

Determination of sites on Endothelin-1 ET-1 which are preferable for biotinylation was assessed by acetylation of individual amino groups and quantitation of analog potency. Acetylation of both ET-1 amino groups had been reported to result in a 200-fold decrease in contractile activity on guinea pig pulmonary artery ring preparation. Incorporation of more bulky groups, such as biotin, would be expected to reduce further the biological activity of ET-1.