Elongated and Shortened Peptidomimetic Inhibitors of the Proprotein Convertase Furin
نویسندگان
چکیده
منابع مشابه
Sox9-dependent transcriptional regulation of the proprotein convertase furin.
The proprotein convertase furin participates in the maturation/bioactivation of a variety of proproteins involved in chondrogenesis events. These include parathyroid hormone-related peptide (PTHrP), an autocrine/paracrine factor that is crucial to both normal cartilage development and cartilage-related pathological processes. Despite the known importance of furin activity in the bioactivation o...
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Osteocalcin (OCN) is an osteoblast-derived hormone that increases energy expenditure, insulin sensitivity, insulin secretion, and glucose tolerance. The cDNA sequence of OCN predicts that, like many other peptide hormones, OCN is first synthesized as a prohormone (pro-OCN). The importance of pro-OCN maturation in regulating OCN and the identity of the endopeptidase responsible for pro-OCN cleav...
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The proprotein convertase enzyme FURIN processes immature pro-proteins into functional end- products. FURIN is upregulated in activated immune cells and it regulates T-cell dependent peripheral tolerance and the Th1/Th2 balance. FURIN also promotes the infectivity of pathogens by activating bacterial toxins and by processing viral proteins. Here, we evaluated the role of FURIN in LysM+ myeloid ...
متن کاملSynthetic peptides derived from the prosegments of proprotein convertase 1/3 and furin are potent inhibitors of both enzymes.
Proprotein convertases (PCs) are Ca(2+)-dependent serine proteases of the subtilisin/kexin family which are known specifically to cleave propeptide and proprotein substrates at the C-terminal of R-X-(K/R)-R/ to generate the relevant biologically active peptides. PCs are initially synthesized as enzymically inactive proenzyme forms where the prosegments play an important inhibitory role to the r...
متن کاملProprotein convertase models based on the crystal structures of furin and kexin: explanation of their specificity.
In eukaryotes, many secreted proteins and peptide hormones are excised from larger precursors by calcium-dependent serine proteinases, the proprotein/prohormone convertases (PCs). These PCs cleave their protein substrates very specifically following multiple basic residues. The seven mammalian PCs and their yeast orthologue kexin are multi-domain proteinases consisting of a subtilisin-related c...
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ژورنال
عنوان ژورنال: ChemMedChem
سال: 2017
ISSN: 1860-7179
DOI: 10.1002/cmdc.201700108