Use of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway.

Using this assay, we could show that compounds FMP-503533, FMP-214534, FMP-401319 and to a slightly lesser extend FMP-214219 significantly inhibited translocation and processing of CRF 1 R-pPL (p < 0.0001) whereas compound FMP-208236 only had a minor effect on translocation inhibition, although with borderline significance (18% reduced translocation; p = 0.0467) ( Fig 5A , the red arrow indicates the SPcNC fragment, i.e. the translocated CRF 1 R-pPL without signal peptide).

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