Journal
NATURE CELL BIOLOGY
Volume 3, Issue 2, Pages 173-182Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/35055085
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To study the role of the BH3 domain in mediating pro-apoptotic and anti-apoptotic activities of Bcl-2 family members, we identified a series of novel small molecules (BH3Is) that inhibit the binding of the Bak BH3 peptide to Bcl-x(L). NMR analyses revealed that BH3Is target the BH3-binding pocket of Bcl-x(L). Inhibitors specifically block the BH3-domain-mediated heterodimerization between Bcl-2 family members in vitro and in vivo and induce apoptosis. Our results indicate that BH3-dependent heterodimerization is the key function of anti-apoptotic Bcl-2 family members and is required for the maintenance of cellular homeostasis.
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