Tailoring Peptide Sequences for their Translation into Small Molecules

4 Tailoring Peptide Sequences for their Translation into Small Molecules 

Peptides to be transformed into small molecules should be as small and as rigid as possible. There is no rule to say which molecular weight leads to a successful 

Peptides are typically highly flexible, but should be as rigid as possible for the transformation process, for two reasons (1) the binding-free energy of a peptide 

Additionally, secondary structure mimetics can be used to introduce constraints that may either have local or global effects. The secondary structure of a peptide is dominated by energetically favoured torsion angels ( ), cp and co, together with 

The introduction of conformational constraints should influence the backbone conformation without compromising any crucial side chain interaction with the receptor. 

---