作者: Sebastian Öther-Gee Pohl , Mark Agostino , Arun Dharmarajan , Shazib Pervaiz
关键词: Cytosol 、 Chromosomal translocation 、 Copy-number variation 、 Chemistry 、 Small molecule 、 Apoptosome assembly 、 Cell biology 、 Cell fate determination 、 Homology (biology) 、 B cell
摘要: Abstract Significance: B cell lymphoma-2 (Bcl-2) was discovered over three decades ago and is the prototype antiapoptotic member of Bcl-2 family that comprises proteins with contrasting effects on fate. First identified as a consequence chromosomal translocation (t 14:18) in human lymphoma, subsequent studies have revealed mutations and/or gene copy number alterations well post-translational modifications variety cancers. The canonical function linked to its ability inhibit mitochondrial membrane permeabilization, thereby regulating apoptosome assembly activation by blocking cytosolic death amplification factors. Of note, identification specific domains within (Bcl-2 homology domains; BH domains) has not only provided mechanistic insight into various interactions between but also been impetus behind design development small molecule inhibitors an...