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.
- A3007 ABT-263 (Navitoclax)15 CitationTarget: Bcl-2|Bcl-wSummary: Potent Bcl-2 family inhibitor, inhibits Bcl-2, Bcl-xL, and Bcl-w
- A4116 Danusertib (PHA-739358)2 CitationTarget: Aurora KinasesSummary: Pan-aurora kinase inhibitor
- A4208 NSC 319726Target: p53Summary: Reactivator of mutant p53
- A4211 Lenalidomide (CC-5013)Target: angiogenesisSummary: Antineoplastic agent,inhibits angiogenesis
- A4212 Pomalidomide (CC-4047)Summary: Immunomodulator,antumor/anti-angiogenic
- A4234 TW-371 CitationTarget: Bcl-2|Bcl-xl|Mcl-1Summary: Bcl-2 inhibitor, inhibits Bcl-2,Bcl-XL and Mcl-1
- A4204 JNJ-26854165 (Serdemetan)1 CitationTarget: p53|HDM2 ubiquitin ligaseSummary: P53 activator, blocking Mdm2-p53 interaction
- A4194 Obatoclax mesylate (GX15-070)1 CitationTarget: Bcl-2Summary: Potent Bcl-2 inhibitor
- A4200 Apogossypolone (ApoG2)2 CitationTarget: Bcl-2|Bcl-xl|Mcl-1Summary: Bcl-2 inhibitor,nonpeptidic small molecule
- A4199 Sabutoclax2 CitationTarget: Bcl-2|Mcl-1|Bfl-1Summary: pan-Bcl-2 inhibitor