Second generation of peptide products

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The major disadvantage of peptide preparations, low stability at non-invasive methods of administration, limits the use of these class compounds in medical practice.

Among the standard ways of increasing the enzymatic stability of peptide molecules are the introduction of elements with rigid structure, which are resistant to proteolytic degradation.

To overcome these complications, we have developed the original chemical platform based on cyclic branched 2,5-piperazine-dion derivatives (2,5-diketopiperazines) to create orally available biologically active ones peptidomimetics. The platform includes a diketopiperazine scaffold with “built-in” functionally active peptide fragments covalently attached via linkers.

The first generation of the hemoregulatory peptides – Thymogen, Stemokin, and Thymodepressin have created opportunities for the breakthrough in peptide drug development.

The combined hemo-and immunoregulatory data Thymogen and Thymodepressin have created the background for expansion of our platform technology of exploration of DKP peptidomimetics of all LL-analogs of L-Glu–L-Trp-OH and DD-analogs of D- Glu(D-Trp-OH)-OH.

calculation 2

Calculation of the spatial structures of linear and cyclopeptide (Stvologen)

The enantiomeric molecule pairs (Thymogen and Thymodepressin) acted in opposite directions at both ways of application, similarly to dipeptides at systemic application.

The results provide a novel example of such an unusual phenomenon as reciprocal bioactivity of enantiomeric chemical preparations initially demonstrated on linear stereo-isomers of Thymogen and Thymodepressin. It is the first example of such peptide behavior.