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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BA2852 AGN194204Summary: AGN194204 (IRX4204) is an orally active, selective agonist. - BA2853 MSN-125Summary: MSN-125 is a potent and oligomerization inhibitor.
- BA2854 BTT-3033Summary: BTT-3033 is an orally active conformation-selective (130nM) inhibitor that binds to the α2Idomain.
- BA2855 FasentinSummary: Fasentin is a potent glucose uptake inhibitor that inhibits transport proteins.
- BA2856 MI-1061Summary: MI-1061 is a potent, orally bioavailable, chemically stable (MDM2-p53 interactions) inhibitor.
- BA2857 CurzereneSummary: Curzerene is a sesquiterpene, isolated from the rhizome of Gaertn, which has anticancer activity.
- BA2858 MC4033Summary: MC4033 is a selective, reversible inhibitor of lysine acetyltransferase 8.
- BA2859 BJE6-106Summary: BJE6-106 (B106) is a potent and selective inhibitor.
- BA2861 InecalcitolSummary: Inecalcitol (TX522), a unique vitamin D3 analog, is an orally active vitamin D receptor agonist.
- BA2862 ForodesineSummary: Forodesine (BCX-1777) is a potent, orally active purine nucleoside phosphorylase inhibitor with values ranging from 0.48 to 1.57 nM in humans, mice, rats, monkeys and dogs.