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Selective Killing: How Chemotherapy Harms Cancer Cells More Than Normal Cells

1The Selectivity Problem: Why Preferential Killing Is Possible but Imperfect2Proliferation as the Primary Vulnerability: Cell-Cycle Dependence3Antimetabolites and the S-Phase Trap4Microtubule Poisons and Mitotic Arrest5DNA-Damaging Agents: Alkylators, Crosslinkers, and Topoisomerase Poisons6The DNA-Damage Response and the Decision to Die7Why Selectivity Fails: Normal-Tissue Toxicity and the Limits of the Window8Resistance: How Tumors Escape and What It Reveals About Selectivity9Widening the Window: Clinical Strategies That Exploit Selectivity
The DNA-Damage Response and the Decision to Die

From Mitochondrial Pore to Caspase Execution

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Watch the sequence from left to right. PUMA and NOXA bind the anti-apoptotic proteins BCL-2, BCL-xL, and MCL-1, which were holding BAX and BAK inactive. Once released, BAX and BAK insert into the mitochondrial outer membrane and oligomerize into a pore. Cytochrome c escapes into the cytosol, where it binds APAF-1 and assembles the apoptosome. The apoptosome recruits and activates caspase-9, an initiator caspase, which then cleaves and activates caspase-3 and caspase-7. Those executioner caspases cut the substrates that produce the visible changes of apoptosis — chromatin condensation, DNA fragmentation, and membrane blebbing. The important point is that once the pore forms, the sequence runs forward without further input; that is why BAX and BAK pore formation is treated as the commitment step.
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The apoptotic arm of the p53 response runs through the mitochondria. In a healthy cell, BAX and BAK are held in check by anti-apoptotic BCL-2-family proteins such as BCL-2, BCL-xL, and MCL-1. When p53 transcribes PUMA and NOXA, these BH3-only proteins bind the anti-apoptotic proteins and displace BAX and BAK. Freed BAX and BAK change conformation, insert into the mitochondrial outer membrane, and assemble into pores. The pores release cytochrome c from the intermembrane space into the cytosol.

Once in the cytosol, cytochrome c binds APAF-1 and, in the presence of dATP or ATP, assembles a heptameric wheel called the apoptosome. The apoptosome recruits procaspase-9 and activates it. Caspase-9 is an initiator caspase; it cleaves and activates the executioner caspases, caspase-3 and caspase-7. These executioner caspases cut a defined set of substrates — nuclear lamins, the inhibitor of CAD (ICAD), and poly(ADP-ribose) polymerase among them — producing the biochemical and morphological changes of apoptosis: chromatin condensation, DNA fragmentation, membrane blebbing, and packaging of the cell into apoptotic bodies that are cleared without inflammation.

The sequence is ordered and irreversible once the mitochondrial pore forms. That is why the BAX/BAK step is often described as the commitment point: upstream signals can be reversed, but once cytochrome c is released, caspase activation proceeds to completion.

References

  1. [1]The BCL-2 protein family: opposing activities that mediate cell deathpubmed.ncbi.nlm.nih.gov
  2. [2]Apoptosis: a review of programmed cell deathpubmed.ncbi.nlm.nih.gov
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