venetoclax
Ligand Summary
Venetoclax is a selective and orally bioavailable small-molecule inhibitor of BCL-2, an anti-apoptotic protein. Overexpression of BCL-2 has been demonstrated in CLL cells where it mediates tumor cell survival and has been associated with resistance to chemotherapeutics. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins like BIM, triggering mitochondrial outer membrane permeabilization and the activation of caspases. In nonclinical studies, venetoclax has demonstrated cytotoxic activity in tumor cells that overexpress BCL-2.
UNII: N54AIC43PW
PubChem: 49846579
Guide to Pharmacology: 8318
ChEMBL: CHEMBL3137309
DrugCentral: 5133
LyCHI: 8FJZSPHS5JQ6
Target Activities
26 Activities
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