It has been shown that peptide tyrosine tyrosine (PYY) plays a key role in appetite regulation. Release of PYY(3-36), a PYY derived analogue, creates an anorectic effect, which may be of value as a therapeutic in the worldwide struggle with obesity. There are almost 80 million obese adults in the United States alone, and that figure reaches over 1 billion when regarding obese persons worldwide. Research with PYY(3-36) is constantly expanding and the use of vitamin B12 (B12) as an oral delivery agent is also being explored, with its own record of successes. A successful oral delivery of clinically relevant levels of PYY(3-36) via B12 has been established in vivo. Herein we describe the full pharmacodynamic studies through selectivity and agonism of B12-PYY(3-36) with its Y2 receptor in vitro through a calcium-induced calcium response (CICR) assay and 3H-inositol assay. Synthesis of a B12-PYY(3-36) conjugate will be produced from B12coupled to PYY(3-36) through the K4 lysine position using a Sharpless/Huisgen Cu(I)-catalyzed cycloaddition reaction. The results of this study provide a direction for the potential of pharmaceutical development of B12 peptide conjugates. Figure 1. <img src='https://acs-archive-assets2.s3.amazonaws.com/239nm/uploads/7180_figure.jpg' alt='' />

In vitro delivery and pharmacodynamics of the appetite-suppressing peptide PYY(3-36) through the vitamin B12 uptake pathway

246th National Meeting (2013)

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