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. 2019 Oct 3;4(19):e129110. doi: 10.1172/jci.insight.129110

Figure 8. Chemical inhibition of KIAA0317 prevents SOCS2 degradation and inflammation in vitro.

Figure 8

(A) Structural analysis of the KIAA0317 HECT domain revealed a major cavity within the C-terminus of the HECT domain. (B and C) Docking study of the candidate inhibitor BC-1365 with the KIAA0317-HECT domain. (D) BC-1365 competition assay. SOCS2 protein was incubated with KIAA0317-bound resin and a titration of BC-1365 prior to immunoblot analysis. The relative amounts of SOCS2 detected in the PDs was normalized to vehicle and quantified. Data represent mean values ± SEM (n = 3). (E) Immunoblot analysis of MLE cells following exposure to a titration of BC-1365. Data represent mean values ± SEM (n = 4). (F) MLE cells were exposed to a titration of BC-1365 for 18 hours before qPCR analysis. Data represent mean values ± SEM (n = 4). NS: P > 0.05, *P < 0.05, **P < 0.01 compared with vehicle treatment; 1-way ANOVA with Dunnett’s multiple-comparisons test (E and F).