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Amide-to-ester substitution allows fine-tuning of the cyclopeptide conformational ensemble

Abstract:

(Figure Presented) Without affecting the overall 3D structure, amide-to-ester backbone substitution (or ester scan) exerts a pronounced influence on the conformational equilibrium of the RCD cyclopeptide cilengitide and its derivatives (see figure; RGD = Arg-GlyAsp). The appropriate substitution, which stabilized the receptor-complementary conformations, improved the biological activity of this integrin antagonist. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.

Año de publicación:

2010

Keywords:

  • Bioorganic chemistry
  • Molecular dynamicsNMR spectroscopy
  • Depsipeptides
  • Conformation analysis

Fuente:

scopusscopus

Tipo de documento:

Article

Estado:

Acceso restringido

Áreas de conocimiento:

  • Bioquímica
  • Proteína

Áreas temáticas:

    Contribuidores:

    Adan J.Adan J.
    Ruíz-Rodríguez J.Ruíz-Rodríguez J.
    Alberício F.Alberício F.
    Mitjans F.Mitjans F.
    Cupido T.Cupido T.
    Jan SpenglerJan Spengler
    Piulats J.Piulats J.