Prestwick Peptidic Macrocycle Library

Prestwick Peptidic Macrocycle Library: A Unique Library of 400 Peptidic Macrocycles

In the past decade, interest into macrocycles strongly increased in medicinal chemistry. More than 100 macrocyclic drugs and clinical candidates are currently marketed or in drug discovery programs.

Prestwick Chemical Libraries in collaboration with GENEPEP include a screening library of 400 high purity short macrocyclic peptides designed with a mix of natural and non-natural amino acids and different types of cyclization (disulfide, lactam, triazole). Macrocyclization can provide a method of improving target potency and modulating selectivity. Macrocycles can become more drug-like than expected based on their physicochemical and pharmacokinetic properties.

Moreover, cyclic peptides in comparison to their linear counterparts combine multiple interesting properties like low toxicity and improved enzymatic stability; they are metabolically more stable, and should have a lower degree of flexibility, with more defined secondary structure conformations that can be adapted to imitate protein interface.

 

Prestwick Peptidic Macrocycle Library: key features

  • A collection of 400 short (5 amino acids), chemically synthesized peptidic macrocycles containing natural and non-natural amino acids
  • Structures with 17 to 20-membered rings
  • Different cyclization motifs (disulfide, lactam, triazole)
  • Mean MW: 570 (see both MW distribution graphs)
  • Constrained, stabilized peptide sequences with exposed side chains
  • Conveniently prepared, ready for multiple screenings

 

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Prestwick Peptidic Macrocycle Library: application

  • Great starting point to identify enzyme inhibitors, agonist or antagonists of GPCRs, …..
  • Ability to attack intracellular targets such as Protein-Protein Interactions, therefore potential use as Protein-Protein Interaction disruptors (inhibitors)
  • Modulators of PPI
  • Chemical probes of protein surfaces

Prestwick Peptidic Macrocycle Library: how Provided?

  • Lyophilized in five 96-well plates.
  • The amount of compound in each well is 0.1 µmol and yields a 1 mM peptidic macrocycle solution when adding 100 µL of solvent
  • Cherry-picking options in lyophilized form
  • Powder form on request, total Library or cherry-picking

 

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