Abstract:
:The programmed cell death or apoptosis plays both physiological and pathological roles in biology. Anomalous activation of apoptosis has been associated with malignancies. The intrinsic mitochondrial pathway of apoptosis activation occurs through a multiprotein complex named the apoptosome. We have discovered molecules that bind to a central protein component of the apoptosome, Apaf-1, and inhibits its activity. These new first-in-class apoptosome inhibitors have been further improved by modifications directed to enhance their cellular penetration to yield compounds that decrease cell death, both in cellular models of apoptosis and in neonatal rat cardiomyocytes under hypoxic conditions.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Mondragón L,Orzáez M,Sanclimens G,Moure A,Armiñán A,Sepúlveda P,Messeguer A,Vicent MJ,Pérez-Payá Edoi
10.1021/jm701195jsubject
Has Abstractpub_date
2008-02-14 00:00:00pages
521-9issue
3eissn
0022-2623issn
1520-4804journal_volume
51pub_type
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