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

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

doi:10.1016/j.ejmech.2015.12.003

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

Atıf İçin Kopyala

Cacciatore I., Fornasari E., Di Stefano A., Marinelli L., Cerasa L. S., Turkez H., ...Daha Fazla

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.108, ss.553-563, 2016 (SCI-Expanded)

Yayın Türü: Makale / Tam Makale
Cilt numarası: 108
Basım Tarihi: 2016
Doi Numarası: 10.1016/j.ejmech.2015.12.003
Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
Sayfa Sayıları: ss.553-563
Anahtar Kelimeler: alpha-methyl-proline, Gly-Pro-Arg, Neurodegenerative disease, Neuroinflammation, NITRIC-OXIDE PROTECTS, ALZHEIMERS-DISEASE, OXIDATIVE STRESS, MEMANTINE, CYTOTOXICITY, MECHANISMS, INHIBITOR, PRODRUG, CODRUG, CELLS
Atatürk Üniversitesi Adresli: Hayır

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.