oleclumab   Click here for help

GtoPdb Ligand ID: 9596

Synonyms: MEDI 9447 | MEDI-9447
Immunopharmacology Ligand
Compound class: Antibody
Comment: Oleclumab (MEDI9447) is a monoclonal antibody targeting the ecto-5'-nucleotidase (CD73), which is being investigated for oncology use [1-2]. Functional studies show that MEDI9447 is a high affinity antagonistic mAb, showing non-competitive inhibition of CD73 hydrolysis of AMP[1]. Two modes of action are suggested: prevention of steric conformational change required for catalytic active state, and inter-CD73 dimer cross-linking.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
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Bioactivity Comments
MEDI9447 binds to an epitope in the N-terminal domain of CD73. MEDI9447 binding decreases both the Vmax and Km of CD73 reaction kinetics, indicating a non-competitive mode of inhibition, that does not alter binding of the AMP substrate.
Selectivity at enzymes
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
Ecto-5'-Nucleotidase Primary target of this compound Hs Antibody Binding 11.4 pKd - 1
pKd 11.4 (Kd 4.2x10-12 M) [1]