Design, synthesis, and in vitro activity of peptidomimetic inhibitors of myeloid differentiation factor 88.
نویسندگان
چکیده
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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ورودعنوان ژورنال:
- Journal of medicinal chemistry
دوره 51 5 شماره
صفحات -
تاریخ انتشار 2008