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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BA3570 CDC801Summary: CDC801 is a potent inhibitor of phosphodiesterase 4 and tumor necrosis factor-α. - BA2316 InotuzumabSummary: Inotuzumab (HumanizedAnti-CD22RecombinantAntibody) is humanized, κ-antibody targeted to humans.
- BA2326 TaltobulinSummary: Taltobulin (HTI-286) is a synthetic tripeptide cysteine analog, Taltobulin is a potent anti-microtubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.
- BA2331 MaytansinolSummary: Maytansinol (AnsamitocinP-0) is a derivative of Medenin.
- BA2360 MensacarcinSummary: Mensacarcin is a highly complex polyketide that is commonly found in tumor cell lines to strongly inhibit cell growth and may induce apoptosis in melanoma cells.
- BA3594 DantroleneSummary: Dantrolene is an orally active, non-competitive inhibitor.
- BA3677 BOLD-100Summary: BOLD-100 (NKP-1339; IT-139) is a first-in-class ruthenium anticancer reagent developed for solid cancers with few side effects.
- BA3744 OrobolSummary: Orobol is a major soy isoflavone with a variety of pharmacological activities, including anti-skin aging and anti-obesity effects.
- BA3776 BLU-222Summary: BLU-222 is an orally effective and selective inhibitor.
- BA3801 AZ5576Summary: AZ5576 is a potent and highly selective inhibitor (IC:<5nM).