Cancer therapeutics based on BCL-2 functional conversion
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The BCL-2 protein family plays a key role in the regulation of ‘intrinsic’ apoptosis by regulating the integrity of the mitochondrial outer membrane (MOM). The BCL-2 family of proteins consists of both anti-apoptotic and pro-apoptotic members. These proteins possess one to four BCL-2 Homology (BH) domains and fall into three functional groups. The anti-apoptotic proteins include BCL-2, BCL-XLand MCL-1, which possess BH1-4 domains. The pro-apoptotic BCL-2 family members are divided into two subclasses, comprising the BH3 only proteins such as NOXA and PUMA and multi-domain proteins such as BAK and BAX which possess the BH1-3 domains. The balance between the expression of pro- and anti- death BCL-2 proteins determines the cell fate as pro-survival BCL-2 members bind and inhibit the activity of pro-death members. The BH3-only proteins are upregulated upon cellular stress such as DNA damage or oncogene activation and then bind pro-survival proteins, preventing their inhibition of BAX and...
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