Peptides and cyclopeptides
NMR spectroscopy helps solving the structure of peptides and cyclopeptides as well, our selected molecules are potential drug candidates.
NGR peptides that recognize CD13 receptors in tumor neovasculature are of high interest, in particular due to their potential applications in drug targeting. We analysed the structure of novel thioether bond-linked cyclic NGR peptides. A significant correlation was found between chemostability and structural measures, such as NHGly−COAsn-sc distances. The sidechain orientation of Asn is a key determining factor; as chemostability increases once the position is turned away from HNGly.
The direct antitumor activity of sea lamprey (Petromyzon marinus) gonadotropin-releasing hormone III (IGnRH-III) was described on several tumor cells. In order to find a correlation between the biological and structural features of modified IGnRH-III compounds, the conformation of lGnRH-III and its dimer derivatives was determined by ECD, VCD, FT-IR and 1H NMR spectroscopy.
Gábor Mező , András Perczel , Michael Przybylski , Magdolna Kovács , Orsolya Csuka , Borbála Vincze , Marian Boldizsár , Bence Kapuvári , Andrea Bodor , Elemér Vass , Zsuzsa Majer , Viktor Farkas , Annamária Jakab , Marilena Manea , András Czajlik , Ferenc Hudecz
Structure, enzymatic stability and antitumor activity of sea lamprey GnRH-III and its dimer derivatives
Peptides 28(4): 806-820 (2007) Kivonat
Kata N. Enyedi , András Czajlik , Krisztina Knapp , András Láng , Zsuzsa Majer , Eszter Lajkó , László Kőhidai , András Perczel , Gábor Mező
Development of cyclic NGR-peptides with thioether linkage: structure and dynamics determining deamidation and bioactivity
J. Med. Chem. 58(4):1806-1817. | DOI: 10.1021/jm501630j | PMID: 25646854 (2015) Kivonat