Schlagwort-Archiv: Molecular Grafting

New publication on the design of cyclic peptide BBB shuttles.

An interdisciplinary team reported on the design of natural peptide derived cyclic BBB shuttles. In ‚Design of sunflower trypsin inhibitor 1 derived probes targeting the LDLR and evaluation of their brain delivery‘ , published in the Journal of Biom. & Pharmacotherapy (IF 7.5), we show that natural peptide are scaffolds for design of novel BBB shuttle probes using computational prediction-informed peptide molecular grafting. The sunflower trypsin inhibitor-1 scaffold was used as prototype and probes generated that incorporated reported BBB shuttle sequences of different size, conformation and amino acid composition. The probe L2-peptide 22 was selected for in vitro characterization and was applied in a rat CNS transprot model.

The full citation: Schwarz P., Dieringer J. Jadhav BK., Lucana M., Ginosyan A., Oller-Salvia B., Gruber CW., Loryan I.,* and Hellinger R.,* Design of sunflower trypsin inhibitor 1 derived probes targeting the LDLR and evaluation of their brain delivery, 2026 Biomed. and Pharmacoth., 202:119756; https://doi.org/10.1016/j.biopha.2026.119756

Research Publication

Our latest study ‚Engineering Peptide Modulators for T-Cell Migration by Structural Scaffold Matching‚ is online! Enjoy reading our article in the #Journal of Medicinal Chemistry.

An international consortium led by the PeptAIDes research team identified the peptide inhibitor of transendothelial T-cell migration (Pepitem) as a prototypic peptide with migration inhibition activity (read more about this topic in a comprehensive review article: Peptide modulators of cell migration: Overview, applications and future development). Using pepitem as a starting point and by developing the powerful structural scaffold matching approach, we generated the stabilized highly active probe VhTI-pep and showed its potency to reduce transendothelial migration of activated T-lymphocytes.

#structural scaffold matching, #pepitem, #transendothelial T-cell migration, #peptide drug design, #natural peptide drug development, #Medical University of Vienna

Link: Gattringer et al.

Peptide modulators of cell migration: Overview, applications and future development

Jasmin Gattringer, Christian W. Gruber and Roland Hellinger published a review article in Drug Discovery Today on peptide cell migration inhibitors.

The article is available here.

Gattringer J, Gruber CW, Hellinger R. Peptide modulators of cell migration: Overview, applications and future development. Drug Discov Today. 2023 Mar 13:103554. doi: 10.1016/j.drudis.2023.103554. PMID: 36921670.