Apoptosis - Proteasome - cysteine protease - c-Kit - Caspases
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.
- A1902 Z-VAD-FMK102 CitationTarget: CaspasesSummary: Pan-Caspase抑制剂。
- A8955 Z-YVAD-FMK7 CitationTarget: CaspasesSummary: Caspase-1抑制剂
- A8170 Z-FA-FMKTarget: cysteine proteaseSummary: 半胱氨酸蛋白酶抑制剂
- B3233 Z-LEHD-FMK8 CitationTarget: CaspasesSummary: 不可逆的Caspase-9抑制剂
- B3232 Z-IETD-FMK12 CitationTarget: CaspasesSummary: Caspase-8抑制剂
- A8238 VX-7651 Citation中文名: 贝纳卡森Target: CaspasesSummary: 有效的Caspase-1选择性抑制剂
- A8236 Regorafenib4 Citation中文名: 瑞戈非尼Target: Raf|VEGFR|PDGFR|c-Kit|RETSummary: VEGFR/PDGFR/FGFR/mutant Kit/RET/Raf-1抑制剂
- A4416 AZ 10417808Target: CaspasesSummary: Caspase-3抑制剂
- A3750 Regorafenib hydrochloride中文名: 瑞戈非尼盐酸盐Target: Raf|VEGFR|PDGFR|c-Kit|c-RETSummary: 酪氨酸激酶抑制剂
- A8165 Q-VD(OMe)-OPh6 CitationTarget: CaspasesSummary: Pan-caspase抑制剂