Article
Conformational Propensity and Biological Studies of Proline Mutated LR Peptides Inhibiting Human Thymidylate Synthase and Ovarian Cancer Cell Growth.
Journal of medicinal chemistry - 23 Aug 2018
Saxena Puneet, Severi Leda, Santucci Matteo, Taddia Laura, Ferrari Stefania, Luciani Rosaria, Marverti Gaetano, Marraccini Chiara, Tondi Donatella, Mor Marco, Scalvini Laura, Vitiello Simone, Losi Lorena, Fonda Sergio, Pacifico Salvatore, Guerrini Remo, D'Arca Domenico, Ponterini Glauco, Costi Maria Paola
Abstract excerpt
LR and [d-Gln4]LR peptides bind the monomer-monomer interface of human thymidylate synthase and inhibit cancer cell growth. Here, proline-mutated LR peptides were synthesized. Molecular dynamics calculations and circular dichroism spectra have provided a consistent picture of the conformational propensities of the [Pro n]-peptides. [Pro3]LR and [Pro4]LR show improved cell growth inhibition and similar...
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