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. 2012 Jan 6;7(1):e30484. doi: 10.1371/journal.pone.0030484

Figure 6. Structurally divergent acidic and non-acidic γ-secretase modulators compete binding of the photo-probe AR243 to the N-terminal fragment of PSEN1.

Figure 6

Competition experiments were performed under cell-free conditions with membrane preparations from N2a-ANPP cells. Membranes were co-incubated with 0.5 µM of the photo-probe AR243 and 100 µM of acidic or non-acidic GSM competitor compounds. (A) The acidic GSM JNJ-40418677 abolished binding of the photo-probe to PSEN1-NTF. (B) Three non-acidic GSMs competed binding of the photo-probe to variable degrees. Compound 1 reduced binding of the photo-probe as effectively as the acidic compound JNJ-40418677. Compound 2 and E-2012 only partially competed binding of the photo-probe to PSEN1-NTF. Input represents 0.02% of the total membrane material.