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1State Key Laboratory of Pharmaceutical Biotechnology, The University of Hong Kong, Hong Kong.
2Department of Medicine, The University of Hong Kong, Hong Kong.
3Research Centre for Heart, Brain, Hormone and Healthy Aging, The University of Hong Kong, Hong Kong.
Copyright © 2017 Korean Endocrine Society
This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/4.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
CONFLICTS OF INTEREST: No potential conflict of interest relevant to this article was reported.
Risk factor | Result | Reference |
---|---|---|
Obesity | BMI correlated positively with serum FGF21 | [28] |
T2DM | Elevated plasma FGF21 | [29] |
Elevated plasma FGF21 predicted diabetes development | [30] | |
Hypertension | Independently associated with elevated serum FGF21 | [31] |
Dyslipidaemia | Serum FGF21 correlated positively with serum TG | [37] |
Serum FGF21 correlated positively with total cholesterol | [37] | |
Serum FGF21 correlated negatively with HDL-C | [22] | |
rs2071616 SNP in FGFR2 gene was associated with LDL-C | [38] | |
NAFLD | Elevated hepatic FGF21 expression | [32] |
Elevated serum FGF21 | [33,34] | |
Diabetic nephropathy | Elevated baseline serum FGF21 was associated with and predicted decline of renal function | [35] |
CKD | Elevated serum FGF21 | [36] |
FGF21, fibroblast growth factor 21; BMI, body mass index; T2DM, type 2 diabetes mellitus; TG, triglyceride; HDL-C, high density lipoprotein cholesterol; SNP, single nucleotide polymorphism; FGFR2, FGF receptor 2; LDL-C, low density lipoprotein cholesterol; NAFLD, non-alcohol fatty liver disease; CKD, chronic kidney disease.
CV end-point | Result | Reference |
---|---|---|
CV mortality | Elevated serum FGF21 predicted combined morbidity and mortality in T2DM | [27] |
Total CV outcomes | Elevated plasma FGF21 | [21] |
CHD | Elevated serum FGF21 | [22] |
Carotid artery IMT | Elevated serum FGF21 | [23,24] |
Arterial stiffness | Brachial-ankle pulse wave velocity independently associated with serum FGF21 | [26] |
LEAD | Elevated serum FGF21 | [25] |
Name | Company | Structural feature/Modification | Lipid-lowering effect | Reference |
---|---|---|---|---|
R1MAb | Genentech | β-Klotho-independent agonistic mAb against FGFR1b/c |
↓ Hepatic TC & TG; ↓ serum TC & NEFA (db/db mice) |
[43] |
Fc-FGF21(RG) | Amgen |
L98R (↓ aggregation); P171G (↓ proteolysis); Fusion to Fc (↑ half-life) |
↓ Serum TC & TG (DIO mice) ↓ Fasted serum TG (DIO monkeys) |
[45] |
LY2405319 | Lilly |
L118C, A134C (disulphide bridge); S167A (↓ glycosylation in yeast); HPIP deletion (↓ proteolysis) |
↓ Serum TG, TC & VLDL-C; ↑ serum HDL-C (diabetic rhesus monkeys) ↓ Serum TG, TC, LDL-C & VLDL-C; ↑ serum HDL-C (humans) |
[48,51] |
PF-05231023 | Pfizer |
A129C (linkage to CVX-200); CVX-200 conjugation (↑ half-life) |
↓ Serum TG & VLDL-C; ↑ serum HDL-C (obese cynomolgus monkeys) ↓ Serum TG, TC & LDL-C; ↑ serum HDL-C (humans) |
[53] |
FGF21, fibroblast growth factor 21; R1MAb, FGFR1 with monoclonal anti-FGFR1 antibody; mAb, monoclonal antibody; FGFR1, FGF receptor 1; TC, total cholesterol; TG, triglyceride; NEFA, non-esterified fatty acid; Fc, antibody constant domain; DIO, diet-induced obesity; HPIP, histidine-prolineisoleucine- proline; VLDL-C, very low density lipoprotein cholesterol; HDL-C, high density lipoprotein cholesterol; LDL-C, low density lipoprotein cholesterol; CVX, CovX-body.