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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BA2873 LuxeptinibSummary: Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent, potent inhibitor. - BA2874 NHWD-870Summary: NHWD-870 is a potent, orally active and selective inhibitor.
- BA2875 BETd-260Summary: BETd-260 (ZBC260), a PROTAC linked by ligand and ligand-conjugated, was able to reduce protein activity at a low concentration of 30 pM in leukemia cells RS4;11.
- BA2877 SKI-178Summary: SKI-178 is a potent sphingosine kinase-1 and inhibitor.
- BA2879 UBX1325Summary: UBX1325 is an inhibitor that promotes apoptosis in senescent cells.
- BA2880 KinsenosideSummary: Kinsenoside is the main active ingredient isolated from the genus Cleomiscus and possesses a wide range of biological activities and pharmacological effects.
- BA2881 AG-825Summary: AG-825 is a selective, ATP-competitive, inhibitor of tyrosine phosphorylation.
- BA2883 S130Summary: S130 is a high affinity, selective inhibitor of cysteine proteases with a value of 3.24 μM.
- BA2884 TegaserodSummary: Tegaserod is an orally effective 5-hydroxytryptamine receptor 4(;) agonist and receptor antagonist.
- BA2885 ROC-325Summary: ROC-325 is a potent orally active autophagy inhibitor with strong anticancer activity.