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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BA3070 Pentagamavunon-1Summary: Pentagamavunon-1 (PGV-1), an analog of Curcumin, is orally active and induces apoptotic signaling through several mechanisms, such as inhibition and. - BA3071 GNE-900Summary: GNE-900 is an ATP-competitive, selective and orally active inhibitor with values of 0.0011, 1.5 μM for ChKl, respectively.
- BA3072 PoncirinSummary: Poncirin is isolated from clover and has anti-inflammatory activity.
- BA3073 FusicoccinSummary: Fusicoccin (FusicoccinA), a fungal septic toxin and stabilizer of protein interactions.
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BA3074 NortriptylineSummary: ortriptyline (Desmethylamitriptyline) is the main active metabolite of mitriptyline, a tricyclic antidepressant. - BA3075 CID5721353Summary: CID5721353 is an inhibitor.
- BA3076 MIR96-IN-1Summary: MIR96-IN-1 targets the Drosha site in the hairpin precursor structure, inhibits its biogenesis, as well as inhibits downstream targets, and triggers apoptosis in breast cancer cells.
- BA3077 JAB-2485Summary: JAB-2485 is a potent and selective aurora kinase A inhibitor.
- BA3078 MPT0E028Summary: MPT0E028 is an orally active, selective inhibitor.
- BA3079 TefinostatSummary: Tefinostat (CHR-2845) is a monocyte/macrophage-targeted histone deacetylase (HDAC) inhibitor.