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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BA3456 UC2288Summary: UC2288 is a novel, cell permeable and orally active attenuating reagent (with relatively selective activity against p21) based on the structural synthesis of sorafenib. -
BA3457 MD-224Summary: MD-224 is a highly efficient small molecule degrader based on protein hydrolysis-targeted chimeras (PROTAC). - BA3458 SulanemadlinSummary: Sulanemadlin (ALRN-6924) is a cell membrane-penetrating, potent p53-based peptidomimetic macrocycle.
- BA3459 MB710Summary: MB710, an aminobenzothiazole derivative, is a stabilizer of the oncogenic p53 mutant Y220C.
- BA3460 MI-773Summary: MI-773 is a potent protein-protein interaction (PPI) inhibitor with high binding affinity for specific (K=8.2nM).
- BA3461 BrigimadlinSummary: Brigimadlin (BI907828) is an orally active E3 ubiquitin protein ligase inhibitor that prevents MDM-2 from negatively regulating the tumor suppressor p53.
- BA3462 P53R3Summary: P53R3 is a potent, sequence-specific DNA binding that restores p53 hotspot mutants, including p53, p53 and p53.
- BA3463 MD-222Summary: MD-222 is a first-of-its-kind, highly effective degradation agent.
- BA3464 PK11007Summary: PK11007 is a mild thiol alkylating agent with anticancer activity.
- BA3466 MDM2-IN-1Summary: MDM2-IN-1 is a synthetic interaction inhibitor.