Alkenyl - Model UFG202 -Building Blocks for Stapled Peptides

Stapled peptides are formed by incorporating special amino acids with olefinic side chains at the i and i+4 positions (one-loop staple) or at i and i+7 positions (two-loop staple). The hydrocarbon bridge is formed by a ring-closing metathesis reaction catalyzed by benzylidenebis(tricyclohexyl-phosphine)-dichlororuthenium (Grubb’s catalyst).

Stapled peptides are good drug leads due to these features:

• Retain active conformation
• Permeate cell membranes
• Resist proteolysis for longer duration