Some amphiphilic cations block the mitochondrial apoptosis-induced channel, MAC

Sonia Martinez-Caballero, Laurent M. Dejean, Kathleen W. Kinnally

Research output: Contribution to journalArticle

Abstract

The mitochondrial apoptosis-induced channel (MAC) forms in the outer membrane of mitochondria early in apoptosis and this activity is altered by physiological levels of cytochrome c. While cyclosporine A and lidocaine have no effect, dibucaine induces a fast blockade of MAC with an IC50 of 39 μM. In contrast, the IC50 for propranolol and trifluoperazine are 52 and 0.9 μM, respectively, and these drugs likely destabilize the open state of MAC. These agents, and others not yet identified, should be valuable tools in the study of apoptosis. Profiling MAC's pharmacology may generate novel therapeutic regimes for disease.

Original languageEnglish (US)
Pages (from-to)35-38
Number of pages4
JournalFEBS Letters
Volume568
Issue number1-3
DOIs
StatePublished - Jun 18 2004

Fingerprint

Cations
Apoptosis
Inhibitory Concentration 50
Dibucaine
Trifluoperazine
Mitochondria
Lidocaine
Cytochromes c
Propranolol
Cyclosporine
Pharmacology
Membranes
Pharmaceutical Preparations
Therapeutics

Keywords

  • Apoptosis
  • Bax
  • Cytochrome c
  • Ion channel
  • MAC, mitochondrial apoptosis-induced channel
  • Mitochondrial apoptosis-induced channel
  • Patch clamp
  • Pharmacology
  • PTP, permeability transition pore
  • Tim, translocase of the inner membrane

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

Some amphiphilic cations block the mitochondrial apoptosis-induced channel, MAC. / Martinez-Caballero, Sonia; Dejean, Laurent M.; Kinnally, Kathleen W.

In: FEBS Letters, Vol. 568, No. 1-3, 18.06.2004, p. 35-38.

Research output: Contribution to journalArticle

Martinez-Caballero, S, Dejean, LM & Kinnally, KW 2004, 'Some amphiphilic cations block the mitochondrial apoptosis-induced channel, MAC', FEBS Letters, vol. 568, no. 1-3, pp. 35-38. https://doi.org/10.1016/j.febslet.2004.05.006
Martinez-Caballero, Sonia ; Dejean, Laurent M. ; Kinnally, Kathleen W. / Some amphiphilic cations block the mitochondrial apoptosis-induced channel, MAC. In: FEBS Letters. 2004 ; Vol. 568, No. 1-3. pp. 35-38.
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