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BDA-366 suppresses lung cancer tumor growth by selectively targeting the BH4 domain of Bcl-2 and Bcl-2-dependent Bax activation. (a) The chemical structure of BDA-366 is shown. (b) BDA-366 binds Bcl-2 selectively as illustrated by the competition fluorescence polarization assay. (c) BDA-366 can induce Bcl-2-dependent Bax activation rather than activate Bax directly. (d) BDA-366 strongly synergizes with RAD001 in vivo. Reproduced, with permission, from [50].
