efzofitimod   Click here for help

GtoPdb Ligand ID: 13199

Synonyms: ATYR-1923 | ATYR1923 | KRP-R120
Immunopharmacology Ligand
Compound class: Peptide or derivative
Comment: Efzofitimod (ATYR1923) is a Fc fusion protein [1]. The C-terminal 59 amino acids corresponds to the active N-terminal domain of histidyl-tRNA synthetase (HARS), an extracellular non-catalytic isoform that is upregulated by inflammatory cytokine stimulation in the lung. The IgG1 Fc domain extends the peptide's circulating half-life. The HARS domain binds selectively to the cell surface receptor neuropilin 2 (NRP2; O60462, which is an immunomodulatory protein and molecular target for inflammatory diseases [5]. In the airways, NRP2 plays an important role in activation of myeloid cells and their recruitment to inflammatory sites [3]. Efzofitimod was developed as a clinical candidate immunotherpy with potential for immune-mediated fibrotic lung conditions.
Peptide Sequence Click here for help
MDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNST
YRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAV
EWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGKAERAALEELVKL
QGERVRGLKQQKASAELIEEEVAKLLKLKAQLGPDESKQKFVLKTPK
Chemical Modification
This Fc fusion protein forms dimers with the monomers connected by two disulphide bridges between Cys7 and Cys10 on each peptide chain. Intra-chain disulphide bridges form at Cys42-Cys102 and Cys148-Cys206 on each monomer.