Exogenous N-terminal fragments of galanin, which are agonists of the GalR2 receptor, have therapeutic potential in experimental cardiac pathology. This implies the need to study their proteolytic stability in biological environments. The aim of this work was to evaluate the proteolytic degradation of galanin G1 (GWTLNSAGYLLGPHAIDNHRSFSDKHGLT-NH₂), its natural and modified fragments G2 and G3 (WTLNSAGYLLGPHA-OH and WTLNSAGYLLGPβAH-OH, respectively) in human plasma. The peptides were obtained by solid-phase synthesis using the Fmoc methodology, purified by HPLC; their structure was confirmed by MALDI-TOF mass spectrometry and ¹H-NMR spectroscopy. The kinetics of galanins G1–G3 degradation in blood plasma was studied by ¹H-NMR spectroscopy based on changes in the intensity of Trp2 signals at 310 K. The results indicate a higher proteolytic stability of the G3 peptide compared to the natural G2 fragment and full-length galanin G1. They indicate the potential of using modified peptide agonists of GalR2 receptors to protect vital organs in pathophysiological conditions.
Download PDF:
Keywords: galanin, N-terminal fragments of galanin, 1H NMR, human plasma
Citation:
Avdeev D.V., Selyutina O.Yu., Sidorova M.V., Pisarenko O.I. (2025) The study of biodegradation of galanin and its N-terminal fragments in a model system in vitro. Biomeditsinskaya Khimiya, 71(1), 71-76.
Avdeev D.V. et al. The study of biodegradation of galanin and its N-terminal fragments in a model system in vitro // Biomeditsinskaya Khimiya. - 2025. - V. 71. -N 1. - P. 71-76.
Avdeev D.V. et al., "The study of biodegradation of galanin and its N-terminal fragments in a model system in vitro." Biomeditsinskaya Khimiya 71.1 (2025): 71-76.
Avdeev, D. V., Selyutina, O. Yu., Sidorova, M. V., Pisarenko, O. I. (2025). The study of biodegradation of galanin and its N-terminal fragments in a model system in vitro. Biomeditsinskaya Khimiya, 71(1), 71-76.
References
Lang R., Gundlach A.L., Holmes F.E., Hobson S.A., Wynick D., Hökfelt T., Kofler B. (2015) Physiology, signaling, and pharmacology of galanin peptides and receptors: three decades of emerging diversity. Pharmacol. Rev., 67(1), 118–175. CrossRef Scholar google search
Pisarenko O.I., Studneva I.M., Veselova O.M. (2021) Modified N-terminal fragments of galanin: cardioprotective properties and mechanisms of action. Biochemistry (Moscow), 86(10), 1502–1512. CrossRef Scholar google search
Serebryakova L., Veselova O., Studneva I., Dobrokhotov I., Palkeeva M., Avdeev D., Molokoedov A., Ovchinnikov M., Sidorova M., Pisarenko O. (2022) Exogenous GalR2-specific peptide agonist as a tool for treating myocardial ischemia/reperfusion injury. Fundam. Clin. Pharmacol., 37(6), 1109–1118. CrossRef Scholar google search
Pisarenko O., Timotin A., Sidorova M., Studneva I., Shulzhenko V., Palkeeva M., Serebryakova L., Molokoedov A., Veselova O., Cinato M., Boal F., Tronc