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

…, G Gallo, A Ciacci, M Semproni, D Vignola…

Index: Fanto, Nicola; Gallo, Grazia; Ciacci, Andrea; Semproni, Mauro; Vignola, Davide; Quaglia, Marco; Bombardi, Valentina; Mastroianni, Domenico; Zibella, M. Pia; Basile, Giancarlo; Sassano, Marica; Ruggiero, Vito; De Santis, Rita; Carminati, Paolo Journal of Medicinal Chemistry, 2008 , vol. 51, # 5 p. 1189 - 1202

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Citation Number: 22

Abstract

We describe the design and synthesis of a peptidomimetic library derived from the heptapeptide Ac-RDVLPGT-NH2, 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-κB ...