FAP finds FGF21 easy to digest

Fibroblast growth factor 21 (FGF21) is an endocrine hormone that regulates carbohydrate and lipid metabolism. In humans, circulating FGF21 is inactivated by proteolytic cleavage of its C-terminus, thereby preventing signalling through a receptor complex. The mechanism for this cleavage event and the...

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Bibliographic Details
Published inBiochemical journal Vol. 473; no. 9; p. 1125
Main Authors Gillum, Matthew P, Potthoff, Matthew J
Format Journal Article
LanguageEnglish
Published England 01.05.2016
Subjects
Fibroblast Growth Factors - genetics
Fibroblast Growth Factors - metabolism
Gelatinases - genetics
Gelatinases - metabolism
Humans
Membrane Proteins - genetics
Membrane Proteins - metabolism
Protein Domains
Proteolysis
Serine Endopeptidases - genetics
Serine Endopeptidases - metabolism
dipeptidyl peptidase IV (DPP-IV)
fibroblast activation protein (FAP)
fibroblast growth factor 21 (FGF21)
proteolytic cleavage
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Summary:Fibroblast growth factor 21 (FGF21) is an endocrine hormone that regulates carbohydrate and lipid metabolism. In humans, circulating FGF21 is inactivated by proteolytic cleavage of its C-terminus, thereby preventing signalling through a receptor complex. The mechanism for this cleavage event and the factors contributing to the post-translational regulation of FGF21 activity has previously been unknown. In a recent issue of the Biochemical Journal, Zhen et al. have identified fibroblast activation protein (FAP) as the endopeptidase responsible for this site-specific cleavage of human FGF21 (hFGF21), and propose that inhibition of FAP may be a therapeutic strategy to increase endogenous levels of active FGF21.
ISSN:1470-8728
DOI:10.1042/BCJ20160004