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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BA2776 GSK2256098Summary: GSK2256098 is a selective kinase inhibitor. - BA2777 NU9056Summary: NU9056 is a potent and selective histone acetyltransferase inhibitor.
- BA2778 POMHEXSummary: POMHEX is a racemic mixture of POM precursor active molecules that are cell-permeable and specific inhibitors of HEX.
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BA2779 PROTAC-O4I2Summary: PROTAC-O4I2 is a target of splicing factor 3B1. - BA2780 CR-1-31-BSummary: CR-1-31-B is a synthetic Rocaglate and a potent inhibitor.
- BA2781 MinnelideSummary: Minnelide is a derivative of tretinoin lactone that has shown antitumor activity in many tumor types (especially in pancreatic cancer).
- BA2782 JX06Summary: JX06 is a potent, selective, covalent inhibitor.
- BA2783 BTdCPUSummary: BTdCPU is a heme-regulated inhibitory kinase activator that promotes phosphorylation and induces apoptosis in (Dex)-resistant cancer cells.
- BA2784 FL118Summary: FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a camptothecin (;HY-16560) analog, is an orally effective inhibitor.
- BA2785 BMS-536924Summary: BMS-536924 is an orally active, competitive and selective inhibitor of insulin-like growth factor receptor kinase and insulin receptor at 100nM and 73nM, respectively.