Ontology highlight
ABSTRACT:
SUBMITTER: Nguyen M
PROVIDER: S-EPMC2148320 | biostudies-literature | 2007 Dec
REPOSITORIES: biostudies-literature
Proceedings of the National Academy of Sciences of the United States of America 20071126 49
Elevated expression of members of the BCL-2 pro-survival family of proteins can confer resistance to apoptosis in cancer cells. Small molecule obatoclax (GX15-070), which is predicted to occupy a hydrophobic pocket within the BH3 binding groove of BCL-2, antagonizes these members and induces apoptosis, dependent on BAX and BAK. Reconstitution in yeast confirmed that obatoclax acts on the pathway and overcomes BCL-2-, BCL-XL-, BCL-w-, and MCL-1-mediated resistance to BAX or BAK. The compound pote ...[more]