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Literature summary for 3.4.11.22 extracted from

  • Giastas, P.; Neu, M.; Rowland, P.; Stratikos, E.
    High-resolution crystal structure of endoplasmic reticulum aminopeptidase 1 with bound phosphinic transition-state analogue inhibitor (2019), ACS Med. Chem. Lett., 10, 708-713 .
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
to 1.6 A resolution, structure of the closed-conformation of ERAP1 with inhibitor Nalpha-(2-[[(1-amino-3-phenylpropyl)(hydroxy)phosphoryl]methyl]pent-4-ynoyl)-D-phenylalaninamide bound in its active site. Inhibitor Nalpha-(2-[[(1-amino-3-phenylpropyl)(hydroxy)phosphoryl]methyl]pent-4-ynoyl)-D-phenylalaninamide is coordinated to the zinc ion via its phosphinic group with a geometry that imitates a transition state analogue Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Nalpha-(2-[[(1-amino-3-phenylpropyl)(hydroxy)phosphoryl]methyl]pent-4-ynoyl)-D-phenylalaninamide potent phosphinic pseudopeptide inhibitor Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NZ08 isoform ERAP1
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