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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BA2178 ArtefenomelSummary: Artefenomel (OZ439) is an orally active, synthetic anti-malarial compound containing an artemisinin pharmacophore with an artemisinin-like mechanism of action. - BA2190 MelarsoprolSummary: Melarsoprol, a trivalent organic arsenic of the melarsoprol-phenylarsine type, is an important drug used for African trypanosomiasis.
- BA2257 GSK3326595Summary: GSK3326595 is a protein arginine methyltransferase 5 inhibitor.
- BA2258 ZotatifinSummary: Zotatifin (eFT226) is a potent, selective and well-tolerated eIF4A inhibitor.
- BA2278 rel-ZotatifinSummary: re-Zotatifin is a racemic isomer of Zotatifin and is less active than Zotatifin as an eIF4A inhibitor.
- BA2305 CnicinSummary: Cnicin is a sesquiterpene lactone.
- 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.