Characterization of Agouti-Related Protein Binding to Melanocortin Receptors

摘要: Agouti-related protein (AGRP) is a naturally occurring antagonist of melanocortin action that thought to play an important role in the hypothalamic control feeding behavior. The exact mechanism AGRP and Agouti has been difficult examine, part because difficulties producing homogeneous forms these molecules can be used for direct binding assays. In this report we describe application chemical synthesis construction two novel variants. Examination biological activity variants demonstrates truncated variant, human AGRP(87–132), 46-amino acid variant based on carboxyl-terminal cysteine-rich domain AGRP, equipotent 111-amino mouse [Leu127Pro]AGRP (mature minus its signal sequence), ability dose dependently inhibitα -MSH-generated cAMP generation at cloned receptors. Furthermore, deletion amino-terminal portion full-length did n...