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.
-
BA6289 AfimetoranSummary: Afimetoran is an antagonist. - BA6383 YS-67Summary: YS-67 is a potent inhibitor.
- BA6390 HNPMISummary: HNPMI are inhibitors and have cytotoxic effects on tumor cells.
- BA6422 BruceantinolSummary: Bruceantinol, a bittering agent isolated from the seeds of Crowberry, inhibits the capsicum mottle virus in chili peppers.
- BA6424 C188Summary: C188 is an inhibitor of IL-6-induced STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting the peptide-binding pocket of the STAT3SH2 structural domain.
- BA6439 BIX02188Summary: BIX02188 is a potent and selective inhibitor.
- BA6445 α-AmyrinSummary: α-Amyrin is a pentacyclic triterpenoid with oral activity.
- BA6455 HirsutenoneSummary: Hirsutenone, an active diheptanone contained in alder, has a variety of biological activities including anti-inflammatory, anti-tumor and anti-atopic dermatitis.
- BA6501 NedometinibSummary: Nedometinib is a tyrosine kinase inhibitor that is targeted.
- BA6511 VNPP433-3βSummary: VNPP433-3β is a molecular gel degrader that targets androgen receptor and its splice variants and serine/threonine protein kinases that interact with MAP kinase.