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Abstract
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.
- dipeptidyl peptidase IV (DPP-IV)
- fibroblast activation protein (FAP)
- fibroblast growth factor 21 (FGF21)
- proteolytic cleavage
Abbreviations
- DPP-IV,
- dipeptidyl peptidase IV;
- FAP,
- fibroblast activation protein;
- FGF21,
- fibroblast growth factor 21;
- FGFR1,
- fibroblast growth factor receptor 1;
- GLP-1,
- glucagon-like peptide-1;
- hFGF21,
- human FGF21
- © 2016 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society
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May 2016
Volume: 473 Issue: 9
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