2. Academic Validation
  3. Design, synthesis, and in vitro activity of peptidomimetic inhibitors of myeloid differentiation factor 88

Design, synthesis, and in vitro activity of peptidomimetic inhibitors of myeloid differentiation factor 88

  • J Med Chem. 2008 Mar 13;51(5):1189-202. doi: 10.1021/jm070723u.
Nicola Fantò 1,  Grazia Gallo,  Andrea Ciacci,  Mauro Semproni,  Davide Vignola,  Marco Quaglia,  Valentina Bombardi,  Domenico Mastroianni,  M Pia Zibella,  Giancarlo Basile,  Marica Sassano,  Vito Ruggiero,  Rita De Santis,  Paolo Carminati
Affiliations

Affiliation

  • 1 Sigma-Tau Industrie, Pomezia, Italy. nicola.fanto@sigma-tau.it
PMID: 18275134 DOI: 10.1021/jm070723u
Abstract

We describe the design and synthesis of a peptidomimetic library derived from the heptapeptide Ac-RDVLPGT-NH 2, belonging to the Toll/IL-1 receptor (TIR) domain of the adaptor protein MyD88 and effective in inhibiting its homodimerization. The ability of the peptidomimetics to inhibit protein-protein interaction was assessed by yeast 2-hybrid assay and further validated in a mammalian cell system by evaluating the inhibition of NF-kappaB activation, a transcription factor downstream of MyD88 signaling pathway that allows production of essential effector molecules for immune and inflammatory responses.

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