Apaf-1
Apoptotic protease activating factor-1 (Apaf-1) is a key molecule in the intrinsic or mitochondrial pathway of apoptosis, which oligomerizes in response to cytochrome c release and forms a large complex known as apoptosome. At least six splice isoforms of Apaf-1 has been reported including Apaf-1S, Apaf-1XL, Apaf-1L, Apaf-1M, Apaf-1XS and Apaf-1ALT. Cytosolic cytochrome c binds to Apaf-1 protein, unraveling its closed auto-inhibited conformation. In response to cytochrome c binding and ADP exchange with ATP, Apaf-1 adopts a heptameric quaternary structure and thus recruits inactive procaspase-9 molecules.This mega Dalton complex, known as apoptosome, serves as an activation platform for the initiator procaspase-9 in the intrinsic pathway of apoptosis.Beside its fundamental role in the apoptotic cell death pathways, Apaf-1 has cell-cycle modulatory effect during DNA damage induced by genotoxic stress. Apaf-1 is involved in the DNA damage checkpoint in a phylogenetically conserved fashion and it seems to perform that independently from the activation of apoptotic effectors and Apaf-1 also participates in the centrosomal microtubule nucleation process, and cytoskeleton organization.
References
1.Shakeri R,et al. Biochimie. 2017 Apr;135:111-125.
References
1.Shakeri R,et al. Biochimie. 2017 Apr;135:111-125.
Apoptosis
Apaf-1
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QM31
catalog no : M16717
cas no: 937735-00-7
QM31 (SVT016426, Apaf-1 inhibitor QM31) is a cytoprotective agent that inhibits the formation of the apoptosome (IC50=7.9 uM in vitro). -
Leonurine
catalog no : M13719
cas no: 24697-74-3
Leonurine (SCM-198) is a natural alkaloid that exhibits cardio-and neuronal-protective effects both in vitro and in vivo. -
ZYZ-488
catalog no : M12015
cas no: 1470302-79-4
ZYZ-488 is a novel inhibitor of apoptotic protease activating factor-1 (Apaf-1).