Fap sites

Added: Homero Moroney - Date: 11.11.2021 05:29 - Views: 18551 - Clicks: 794

Fibroblast activation protein FAP is a prolyl-cleaving endopeptidase proposed as an anti-cancer drug target. It is necessary to define its cleavage-site specificity to facilitate the identification of its in vivo substrates and to understand its biological functions. Instead, an intracellular protein, SPRY2, is cleavable by FAP and more suitable for investigation of its substrate specificity in the context of the full-length globular protein. FAP prefers uncharged residues, including small or bulky hydrophobic amino acids, but not charged amino acids, especially acidic residue at P1', P3 and P4 sites.

Molecular modelling analysis shows that the substrate-binding site of FAP is surrounded by multiple tyrosine residues and some negatively charged residues, which may exert least preference for substrates with acidic residues. Our study provided new information on FAP cleavage-site specificity, which differs from the data obtained by profiling with a peptide library or with the denatured protein, fap sites, as the substrate. Furthermore, our study suggests that negatively charged residues should be avoided when deing FAP inhibitors.

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RSS Link Copy. Full text links Cite Display options Display options. Abstract Fibroblast activation protein FAP is a prolyl-cleaving endopeptidase proposed as an anti-cancer drug target. Similar articles Using substrate specificity of antiplasmin-cleaving enzyme for fibroblast activation protein inhibitor de. Lee KN, et al. Ala and conserved active site residues promote fibroblast activation protein endopeptidase activity via distinct mechanisms of transition state stabilization. Meadows SA, et al. Epub Mar PMID: Keane FM, et al. FEBS J. Epub Mar 9. Molecular recognition of fibroblast activation protein for diagnostic and fap sites applications.

Biochim Biophys Acta Proteins Proteom. Epub Apr 6. PMID: Review. Kelly T, et al. Int Rev Cell Mol Biol. See all similar articles. Cited by 7 articles The role of fibroblast activation protein in health and malignancy. Fitzgerald AA, et al. Cancer Metastasis Rev. Cop AL, et al. PLoS One. Dunshee DR, et al. J Biol Chem. Epub Jan Circulating FGF21 proteolytic processing mediated by fibroblast activation protein. Zhen EY, et al. Biochem J. Epub Dec 3. Koczorowska MM, et al. Mol Fap sites.

Epub Aug See all "Cited by" articles. Publication types Research Support, Non-U. Gov't Actions. Humans Actions. Models, Molecular Actions. Substrate Specificity Actions. Membrane Proteins Actions. Recombinant Proteins Actions. SPRY2 protein, human Actions. Serine Endopeptidases Actions. Gelatinases Actions. Full text links [x] Silverchair Information Systems. Copy Download.

Fap sites

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Fibroblast activation protein peptide substrates identified from human collagen I derived gelatin cleavage sites