Fig. 1.

Small-molecule screening to identify inhibitors of the GIV–Gαi interaction. (A) Diagram depicting the rationale for targeting the GIV–Gαi interaction with small molecules. (B) Scheme of the full screening campaign. (C) Confirmation of hit compounds that inhibit the GIV–Gαi interaction in two orthogonal biochemical assays, FP and AS. (D) Triage of compounds based on unfavorable chemical properties and availability of quality controlled molecules. (E) Test of 69 IGGi compounds (100 μM) on MDA-MB-231 cell migration and viability. Red, <30% reduction; blue, >30% reduction. Mean ± SEM (N = 4). (F) Comparison of the effect of IGGi compounds (100 μM) on the viability of three breast cell lines, MDA-MB-231, MCF-7, and MCF-10A (mean of N = 3).