[HTML][HTML] The BH3 α-helical mimic BH3-M6 disrupts Bcl-XL, Bcl-2, and MCL-1 protein-protein interactions with Bax, Bak, Bad, or Bim and induces apoptosis in a Bax …
A critical hallmark of cancer cell survival is evasion of apoptosis. This is commonly due to
overexpression of anti-apoptotic proteins such as Bcl-2, Bcl-X L, and Mcl-1, which bind to the
BH3 α-helical domain of pro-apoptotic proteins such as Bax, Bak, Bad, and Bim, and inhibit
their function. We designed a BH3 α-helical mimetic BH3-M6 that binds to Bcl-X L and Mcl-1
and prevents their binding to fluorescently labeled Bak-or Bim-BH3 peptides in vitro. Using
several approaches, we demonstrate that BH3-M6 is a pan-Bcl-2 antagonist that inhibits the …
overexpression of anti-apoptotic proteins such as Bcl-2, Bcl-X L, and Mcl-1, which bind to the
BH3 α-helical domain of pro-apoptotic proteins such as Bax, Bak, Bad, and Bim, and inhibit
their function. We designed a BH3 α-helical mimetic BH3-M6 that binds to Bcl-X L and Mcl-1
and prevents their binding to fluorescently labeled Bak-or Bim-BH3 peptides in vitro. Using
several approaches, we demonstrate that BH3-M6 is a pan-Bcl-2 antagonist that inhibits the …