ArticleEBioMedicine2019
Paracrine-endocrine FGF chimeras as potent therapeutics for metabolic diseases.
Article in EBioMedicine, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 27 citations in OpenAlex.
- Human FGF1Cells · 2026Article
- Engineered fibroblast growth factor 1 variants uncouple glucose-lowering effects from mitogenic activity with therapeutic potential for type 2 diabetes.Molecular biomedicine · 2026Article
- Development of FGF21 Mutant with Potent Cardioprotective Effects in T2D Mice via FGFR1-AMPK-Mediated Inhibition of Oxidative Stress.International journal of molecular sciences · 2025Article
- FGF-based drug discovery: advances and challenges.Nature reviews. Drug discovery · 2025Review
- Pathology and Therapeutic Significance of Fibroblast Growth Factors.Targets (Basel) · 2025Article
- Novel FGF21 analogues through structure-based optimization for therapeutic development.Acta biochimica et biophysica Sinica · 2024Article
- Exploring endocrine FGFs - structures, functions and biomedical applications.International journal of biochemistry and molecular biology · 2024Review
- Targeting FGF21 in cardiovascular and metabolic diseases: from mechanism to medicine.International journal of biological sciences · 2023Review
- Autocrine FGF1 signaling promotes glucose uptake in adipocytes.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Emerging roles of fibroblast growth factor 21 in critical disease.Frontiers in cardiovascular medicine · 2022Review
- The Saga of Endocrine FGFs.Cells · 2021Review
- Label-free methods for opticalPhysical chemistry chemical physics : PCCP · 2021Review
- Glucagon-like peptide-1 receptor co-agonists for treating metabolic disease.Molecular metabolism · 2021Review
- Nutritional Regulation of Hepatic FGF21 by Dietary Restriction of Methionine.Frontiers in endocrinology · 2021Review
- Fibroblast Growth Factor 21 Ameliorates NaFrontiers in pharmacology · 2021Article
- The therapeutic potential of FGF21 in metabolic diseases: from bench to clinic.Nature reviews. Endocrinology · 2020Review
- Systemically Administered, Target-Specific, Multi-Functional Therapeutic Recombinant Proteins in Regenerative Medicine.Nanomaterials (Basel, Switzerland) · 2020Review
- Chronicles of an FGF chimera: The odyssey continues.EBioMedicine · 2019Article
Corrections and comments
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Authors and funding
12 authors at 4 institutions in 2 countries.
Funding
Abstract
backgroundThe development of a clinically useful fibroblast growth factor 21 (FGF21) hormone has been impeded by its inherent instability and weak FGF receptor (FGFR) binding affinity. There is an urgent need for innovative approaches to overcome these limitations.
methodsWe devised a structure-based chimerisation strategy in which we substituted the thermally labile and low receptor affinity core of FGF21 with an HS binding deficient endocrinised core derived from a stable and high receptor affinity paracrine FGF1 (FGF1
findingsThe melting temperature of the engineered chimera (FGF1
interpretationOur study describes a structure-based chimerisation approach that effectively mitigates both the intrinsically weak receptor binding affinities and short half-lives of endocrine FGFs, and advance the development of the FGF21 hormone into a potentially useful drug for Type 2 diabetes.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.