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Makale Tam Makale Uluslararası 2016

Development of glycine-alpha-methyl-proline-containing tripeptides with neuroprotective properties

Ivana Cacciatore, Erika Fornasari, Antonio Di Stefano, Lisa Marinelli, Laura Serafina Cerasa, Hasan Türkez, Elanur Aydin, Alessandro Moretto, Alessio Ferrone, Mirko Pesce, Viviana di Giacomo, Marcella Reale, Erica Costantini, Pamela di Giovanni, Lorenza Speranza, Mario Felaco, Antonia Patruno

European journal of medicinal chemistry Cilt 108 · ss. 553–563 · 01.01.2016
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Özet

Herein is described the synthesis of novel glycine-alpha-methyl-proline-containing tripeptides (GP(Me)X tripeptides namely GP(Me)R, GP(Me)K, and GP(Me)H) with the aim of obtaining derivatives highly stable in human plasma and able to counteract neuroinflammatory processes that are distinctive of neurodegenerative pathologies. The syntheses of GP(Me)R, GP(Me)K, and GP(Me)H were all achieved both by introducing the Pro(Me) residue into the Gly-Pro-Arg (GPR) sequence in place of the native Pro in P2 position and replacing the basic amino acid Arg in P3 position by Lys or His.

Anahtar kelimeler

oxidative stress CELLS MECHANISMS ALZHEIMERS-DISEASE cytotoxicity INHIBITOR prodrug neuroinflammation Codrug Memantine alpha-methyl-proline Gly-Pro-Arg Neurodegenerative disease NITRIC-OXIDE PROTECTS

Atıf için künye

Cacciatore, I., Fornasari, E., Di Stefano, A., Marinelli, L., Cerasa, L. S., Türkez, H., Aydin, E., Moretto, A., Ferrone, A., Pesce, M., di Giacomo, V., Reale, M., Costantini, E., di Giovanni, P., Speranza, L., Felaco, M., & Patruno, A. (2016). Development of glycine-alpha-methyl-proline-containing tripeptides with neuroprotective properties. European journal of medicinal chemistry, 108, 553–563. https://doi.org/10.1016/j.ejmech.2015.12.003

BibTeX 
@article{cacciatore2016-245039,
  author = {Cacciatore, Ivana and Fornasari, Erika and Di Stefano, Antonio and Marinelli, Lisa and Cerasa, Laura Serafina and Türkez, Hasan and Aydin, Elanur and Moretto, Alessandro and Ferrone, Alessio and Pesce, Mirko and di Giacomo, Viviana and Reale, Marcella and Costantini, Erica and di Giovanni, Pamela and Speranza, Lorenza and Felaco, Mario and Patruno, Antonia},
  title = {Development of glycine-alpha-methyl-proline-containing tripeptides with neuroprotective properties},
  journal = {European journal of medicinal chemistry},
  year = {2016},
  volume = {108},
  pages = {553--563},
  issn = {0223-5234},
  doi = {10.1016/j.ejmech.2015.12.003},
  url = {https://akademik.atauni.edu.tr/yayinlar/245039-development-of-glycine-alpha-methyl-proline-containing-tripeptides-with}
}