The Effects of a Novel Series of KTTKS Analogues on Cytotoxicity and Proteolytic Activity
| Autor: | Paulina Uścinowicz, Ilona Zaręba, Urszula Tałałaj, Bruzgo I, Agnieszka Markowska, Arkadiusz Surażyński |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2019 |
| Předmět: |
Arginine
Cell Survival Plasmin Lysine Pharmaceutical Science Peptide Article Analytical Chemistry lcsh:QD241-441 Inhibitory Concentration 50 030207 dermatology & venereal diseases 03 medical and health sciences 0302 clinical medicine Thrombin lcsh:Organic chemistry palmitoyl pentapeptide Drug Discovery medicine cosmetic peptides Physical and Theoretical Chemistry Cells Cultured 030304 developmental biology chemistry.chemical_classification 0303 health sciences plasmin inhibitors collagen biosynthesis Organic Chemistry Kallikrein Fibroblasts Trypsin In vitro chemistry Biochemistry Chemistry (miscellaneous) Proteolysis cytotoxity Molecular Medicine Collagen Peptides KTTKS Oligopeptides medicine.drug |
| Zdroj: | Molecules Volume 24 Issue 20 Molecules, Vol 24, Iss 20, p 3698 (2019) |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules24203698 |
| Popis: | KTTKS is a matrikine that originates from the proteolytic hydrolysis of collagen. This peptide stimulates ECM production and types I and III collagen expression in vitro. A more stable form of KTTKS is pal-KTTKS, known as Matrixyl® or palmitoyl pentapeptide-3. A series of novel pentapeptides, analogues of KTTKS with the general formula X-KTTKS-OH(NH2), where X = acetyl, lipoyl, palmitoyl residues, was designed and synthesized. Their effect on amidolytic activity of urokinase, thrombin, trypsin, plasmin, t-PA, and kallikrein were tested. Cytotoxic tests on fibroblasts, as well as collagen and DNA biosynthesis tests for selected peptides, were also carried out. The test results showed that the most active plasmin inhibitors were palmitoyl peptides, whether in acid or amide form. No biological effects of lysine modification to arginine in the synthesized peptides were found. None of the synthesized peptides was not cytotoxic on fibroblasts, and three of them showed cell growth. These three compounds showed no concentration-activity relationship in the collagen and DNA biosynthesis assays. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
| Nepřihlášeným uživatelům se plný text nezobrazuje | K zobrazení výsledku je třeba se přihlásit. |