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BH3 Mimetics Off-Target Effects.pdf

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Preview of BH3 Mimetics Off-Target Effects
🔗 Source: nature.com
📊 Size: 1.7 MB
👤 Author: David J. Mallick
⬇️ Downloads: 101

Summary

MIM1, UMI-77, and A-1210477, putative MCL1 inhibitors, were investigated for their mechanisms of action. MIM1 and UMI-77 induced NOXA, sensitizing leukemia cells to ABT-199, while A-1210477 accumulated MCL1 protein without inducing NOXA. However, at higher concentrations, A-1210477 induced a novel, BAX/BAK-independent mechanism of apoptosis, releasing cytochrome c without loss of mitochondrial membrane potential, suggesting off-target effects at commonly used concentrations.

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Description

MIM1, UMI-77, and A-1210477, putative MCL1 inhibitors, were investigated for their mechanisms of action.

Technical Information

  • File Format: PDF
  • File Size: 1.7 MB
  • Pages: 13
  • Language: EN
  • Author: David J. Mallick
  • Total Downloads: 101
  • Last Updated: 1 month ago

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