Synonyms: ATYR-1923 | ATYR1923 | KRP-R120
Compound class:
Peptide
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.
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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. |