Poster Presentation 10th Australian Peptide Conference 2013

Heteroatom-contained Peptide Side-chain Formation Method Development (#195)

Qingzhou Zhang 1 , Zigang Li 1
  1. Peking University Shenzhen Graduate School, Xili Town, China

Peptides as drug candidates have the prior of biocompatibility (compare with small molecular) and easy manual synthesis (compare with protein), while peptide also have the shortcomings of short half-life, conformation flexible, poor cell permeability. To conquer these many peptide modification methods were developed. Side-chain cyclization developed in the past several decades was wildly used now days and have been proved can neutralize these shortcomings. While till now only a few methods such as RCM was wildly used for the side-chain formation. For variable side-chain modifications new facile side-chain formation methods were needed. Our group has developed several methods which can easily insert heteroatom on most of the position of a hydrocarbon side-chain. And we have proved through serum and mouse digestion that this kind of side-chain on short peptide can highly enhance peptide’s stability and CD result show this method also have some efficacy in peptides alpha-helix conformation stabilization.