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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BA2744 TVB-3166Summary: TVB-3166 is an orally effective, reversible and selective fatty acid synthase inhibitor with 42 nM and 81 nM for FASN and cellular palmitate synthesis, respectively. -
BA2745 OctreotideSummary: Octreotide (SMS201-995) is a growth inhibitor receptor agonist and synthetic octapeptide growth inhibitor analog. -
BA2746 Deferoxamine5 CitationSummary: Deferoxamine (DeferoxamineB) is an iron chelator (binding Fe(III) and many other metal cations) that is widely used to reduce iron accumulation and deposition in tissues. -
BA2747 MRT-2359Summary: MRT-2359 is a potent, orally active and selective degrader (>30nM and <300nM) that specifically induces protein translation-dependent apoptosis. -
BA2748 DegarelixSummary: Degarelix is a competitive, reversible gonadotropin-releasing hormone receptor antagonist. -
BA2749 CWI1-2Summary: CWI1-2 is an inhibitor. -
BA2750 MS177Summary: MS177 is an effective and fast acting degradant. -
BA2751 CTBSummary: CTB is an activator of p300 histone acetyltransferase. -
BA2752 AC-4-130Summary: AC-4-130 is a potent structural domain inhibitor. -
BA2753 SD-36Summary: SD-36 is an effective degradant (=~50nM) with high selectivity compared to other members.


