Apoptosis
Apoptosis, also known as programmed cell death, is rigorously controlled process of cell death that leads to phagocytosis of unwanted cell. It is triggered after sufficient cellular damage and activated through extrinsic or intrinsic pathways. The intrinsic pathway is mainly occurs via release of cytochrome c from the mitochondria and regulates mitochondrial outer membrane permeabilization by Bcl-2 family proteins. The extrinsic pathway is induced by ligand binding to death receptor, such as Fas, TNFαR, DR3, DR4, and DR5. Caspases then cleave target proteins and nuclear lamins to promote DNA degradation, resulting apoptotic cells undergo phagocytosis. In addition, p53 has the ability to activate intrinsic and extrinsic pathways of apoptosis by inducing transcription of several proteins like Puma, Bid, Bax, TRAIL-R2, and CD95.
Some Inhibitors of apoptosis proteins (IAPs), such as XIAP/BIRC4 and Bruce/BIRC6, can block casapse activity through direct binding, while other IAPs, such as cIAP1/BIRC2, cIAP2/BIRC3, act as ubiquitin ligases that target caspases for ubiquitin-mediated degradation. Apoptosis is essential for growth, development and aging in multicellular organisms. Any alterations or abnormalities occurring in apoptotic processes contribute to development of human diseases, including cancer.
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BA2754 RMC-6291Summary: RMC-6291 is an orally effective covalent inhibitor. -
BA2755 MilademetanSummary: Milademetan (DS-3032) is a specific, orally active inhibitor for acute myeloid leukemia and solid tumors. -
BA2756 ONC212Summary: ONC212, a fluorinated ONC201 analog, is a promising anticancer agent and selective agonist. -
BA2757 STL127705Summary: STL127705 is a potent inhibitor of Ku70/80 heterodimeric proteins. -
BA2759 BafetinibSummary: Bafetinib is an orally active tyrosine kinase inhibitor. -
BA2760 iCRT3Summary: is an inhibitor of β-cyclin response transcription. -
BA2761 KRIBB11Summary: KRIBB11 is an inhibitor. -
BA2762 GinkgetinSummary: Ginkgetin is a biflavonoid isolated from Ginkgo biloba. -
BA2763 DinoprostSummary: Dinoprost (ProstaglandinF2α) is an orally effective prostaglandin F (PGF) receptor agonist. -
BA2764 MGH-CP1Summary: MGH-CP1 is a potent and orally active and self-palmitoylation inhibitor at 710 nM and 672 nM, respectively.


