Constrained Peptides

Come visit our booth at the ABRF 2011 conference where Bio-Synthesis’ peptide chemist
will be giving more information over constrained peptides

Synthetic locked polypeptide

, a method to mimic protein–protein interactions, have been shown to increase activity, potency in vivo cancer cell death and enhance therapeutic properties.

The need for introducing short peptides that regulate important biological process in various types of diseases, have offered great potential as a new class of therapeutic candidates. However, when isolated and introduced into an aqueous solution, peptide helices are highly susceptible to conformational changes. They are easily degraded by proteolysis and have difficulty in intact cell penetration, which often leads to a reduction in biological activity and thus diminishes therapeutic benefit.

This challenge can be overcome by chemically locking the conformational structure of a peptide which in turn mimics the molecular structure that are typically found at the interface of protein-protein interactions. When locked into this stable configuration, constraint peptides are able to penetrate cells efficiently and can exert their effects on intracellular protein targets. The large surface area of the peptides gives them advantages over small molecules in their ability to disrupt specific signaling pathways by inhibiting targeted protein-protein interactions.

Advantages of constrained peptides:

Enhance receptor affinity and efficacy

Increased cell permeability

Decrease proteolysis hence increased bio-activities.

Bio-Synthesis offers a new peptide conformation screening tool called positional cyclization scanning. This technique involve

synthesis of peptides

with constrained structures in the form of lactam bridge or stapling at various position to determine the overall structure conformation of the protein. This process not only

provides peptides

with desirable pharmacokinetic properties but also provides a conceptual approach towards applying peptidomimetics and small molecules for intracellular protein-protein interactions.

Bio-Synthesis' Custom Peptide Department provides you with dedicated project managers who works directly with our expert scientists to deliver your peptide project to specification. Our goal is to provide the highest level of quality and services for your particular needs.

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