The discovery of a novel inhibitor of apoptotic protease activating factor-1 (Apaf-1) for ischemic heart: synthesis, activity and target identification

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The discovery of a novel inhibitor of apoptotic protease activating factor-1 (Apaf-1) for ischemic heart: synthesis, activity and target identification

Apaf-1 is a central component in the apoptosis regulatory network for the treatment of apoptosis related diseases. Excessive Apaf-1 activity induced by myocardial ischemia causes cell injury. No drug targeted to Apaf-1 for treating myocardial ischemia has been reported to the best of our knowledge. In the present work, we synthesized a novel compound, ZYZ-488, which exhibited significant cardio...

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Apoptotic protease-activating factor 1 (Apaf-1) as a liable gene for spontaneous mutations in vitro

The apoptotic protease-activating factor 1 (Apaf-1) receives the death signal in the intrinsic ormitochondrial pathway of apoptosis. Upon the releasing of cytochrome c from theintermembrane space of mitochondria and binding to Apaf-1 molecules, a heptamericapoptosome complex is formed and triggers the downstream cascade of caspases. Here, for thefirst time we present spontaneous mutations and r...

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APAF 1 ( Apoptotic protease activating factor 1 )

Five isoforms of APAF1 cDNA have been identified in Homo sapiens: The original APAF1 (also called Apaf-1S) is 3585 bp long (it contains 12 WD40 repeats); The APAF1-1M isoform (3618 bp) contains an insertion of 33 nt after position 295 of the first published sequence (11 aa insertion GKDSVSGITSY between aa 98 and 99; it also contains 12 WD40 repeats); The APAF1XS isoform (3516 bp) contains the s...

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apoptotic protease-activating factor 1 (apaf-1) as a liable gene for spontaneous mutations in vitro

the apoptotic protease-activating factor 1 (apaf-1) receives the death signal in the intrinsic ormitochondrial pathway of apoptosis. upon the releasing of cytochrome c from theintermembrane space of mitochondria and binding to apaf-1 molecules, a heptamericapoptosome complex is formed and triggers the downstream cascade of caspases. here, for thefirst time we present spontaneous mutations and r...

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Apoptotic Protease Activating Factor 1 (Apaf-1)–Independent Cell Death Suppression by Bcl-2

Reportedly, antiapoptotic Bcl-2 family proteins suppress apoptosis by binding to and inhibiting members of the CED-4 family of caspase activators. To explore this question, we used embryonic stem (ES) cells in which one (-/+) or both (-/-) copies of the gene encoding apoptotic protease activating factor 1 (Apaf-1), a CED-4 homologue, were disrupted by homologous recombination. Stable clones of ...

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ژورنال

عنوان ژورنال: Scientific Reports

سال: 2016

ISSN: 2045-2322

DOI: 10.1038/srep29820