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aponermin   Click here for help

GtoPdb Ligand ID: 13293

Synonyms: Shaite® (China)
Approved drug
aponermin is an approved drug (China (2023))
Compound class: Peptide
Comment: Aponermin is an engineered tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) peptide mimetic that was designed to promote apoptosis in tumours by interacting with death receptors (DR) 4 and 5 on the surface of tumour cells [2], whilst sparing normal cells/tissues. This peptide construct comprises the extracellular (soluble) portion of TRAIL and it organises into stable homotrimers in solution. Aponermin has higher binding affinity for DR4/5 and a longer half-life (in rodents and humans) than endogenous wild type TRAIL [1,3].
In the absence of a declared amino acid sequence for aponermin, we generated the sequence presented here from information in [1] and the Uniprot entry for human TRAIL (P50591).
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
death receptor 4 Hs Agonist Agonist - - - 1
⤷ [1]
death receptor 5 Hs Agonist Agonist - - - 1
⤷ [1]