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kallistatin; kallikrein inhibitor; peptidase inhibitor 4; PI-4; Serpin A4 (SERPINA4, KST, PI4)

Function: - inhibits human amidolytic & kininogenase activities of tissue kallikrein - inhibition is achieved by formation of an equimolar, heat- & SDS-stable complex between the inhibitor & the enzyme, & generation of a small C-terminal fragment of the inhibitor due to cleavage at the reactive site by tissue kallikrein Structure: - the N-terminus is blocked - monomer & some homodimers - belongs to the serpin family Compartment: secreted Expression: - expressed by the liver & secreted into plasma Notes: - heparin blocks kallistatin's complex formation with tissue kallikrein & abolishes its inhibitory effect on tissue kallikrein's activity

Specific

berotralstat (Orladeyo)

General

glycoprotein secreted protein serine protease inhibitor; serpin

Properties

SIZE: entity length = 427 aa MW = 49 kD COMPARTMENT: extracellular compartment MOTIF: signal sequence {1-20} N-glycosylation site {N33} N-glycosylation site {N108} N-glycosylation site {N157} N-glycosylation site {N238} peptide motif {388-389} INHIBITS: kallikrein

Database Correlations

OMIM 147935 UniProt P29622 Pfam PF00079 Entrez Gene 5267 Kegg hsa:5267

References

UniProt :accession P29622