Study summary · research use only
Chemical Platform for the Preparation of Synthetic Orally Active Peptidomimetics with Hemoregulating Activity
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
In this mouse study (also using ex vivo irradiated bone marrow cells), researchers describe a chemical platform based on branched piperazine-2,5-dione derivatives (2,5-diketopiperazines) for preparing orally available peptidomimetics, with a diketopiperazine scaffold carrying covalently attached peptide fragments via linkers. The concept was applied to two hemostimulatory drugs, the dipeptide thymogen (GluTrp) and the tripeptide stemokin (IleGluTrp), and a series of derivatives was prepared. Of five synthesized analogues, three showed high hemostimulatory activity in intact mice and in ex vivo irradiated bone marrow cells, according to the abstract. The authors discuss prospects for further development of this approach.
Abstract
A novel chemical platform based on branched piperazine-2,5-dione derivatives (2,5-diketopiperazines) for creating orally available biologically active peptidomimetics has been developed. The platform includes a diketopiperazine scaffold with "built-in" functionally active peptide fragments covalently attached via linkers. The concept was applied to two hemostimulatory drugs, the dipeptide thymogen (GluTrp) and the tripeptide stemokin (IleGluTrp). Preparation of a series of respective derivatives is described. Of the five synthesized analogues, three demonstrated high hemostimulatory activity in vivo on intact mice and on ex vivo irradiated bone marrow cells. Prospects of further development of the concept are discussed.
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