Apoptosis - Topoisomerases - Bcl-xl - DHFR - MDMX
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.
- A3935 WEHI-53915 CitationTarget: Bcl-xlSummary: 选择性的Bcl-xL抑制剂
- A3237 Betulinic acid中文名: 白桦脂酸,桦木酸Target: Aminopeptidases|Topoisomerases|HIVSummary: 抗HIV和抗肿瘤化合物,五环三萜类化合物
- A4390 Pemetrexed1 Citation中文名: 培美曲塞二钠盐Target: Thymidylate Synthase|DHFR|GARFTSummary: TS、DHFR、GARFT和AICARFT抑制剂
- A4200 Apogossypolone (ApoG2)2 CitationTarget: Bcl-2|Bcl-xl|Mcl-1Summary: Bcl-2的非肽类小分子抑制剂
- A4234 TW-371 CitationTarget: Bcl-2|Bcl-xl|Mcl-1Summary: Bcl-2抑制剂,抑制Bcl-2、Bcl-XL和Mcl-1。
- A4209 NSC 207895 (XI-006)Target: MDMXSummary: MDMX抑制剂,抗癌制剂